Latest advances in hydrogel-based drug delivery systems for optimization of metabolic syndrome treatment
CONCLUSION: The following review aims to evaluate the use of the hydrogel systems in the therapy of diabetes, obesity, hypertension, and dyslipidemia, which are the main components of metabolic syndrome.PMID:33622222 | DOI:10.2174/0929867328666210223141555 (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 24, 2021 Category: Chemistry Authors: Diego Arauna Sekar Vijayakumar Esteban Dur án-Lara Source Type: research

ICP-MS-based approach to determine nanoparticle recovery after hollow fiber flow field flow fractionation
Curr Med Chem. 2021 Feb 21. doi: 10.2174/0929867328666210222094913. Online ahead of print.ABSTRACTCompared to classical chemicals, nanoparticles (NPs) exhibit unique properties, which lead to challenges in sample preparation and analysis. Fractionation techniques and in particular hollow fiber flow field flow fractionation (HF5) have recently become popular in the characterization and quantification of nanomaterials, because of their fine fractionation capability in the nanoscale-range. When dealing with NPs a great drawback during fractionation is the loss of particles in the fractionation devices, tubing and connectors. ...
Source: Current Medicinal Chemistry - February 23, 2021 Category: Chemistry Authors: Fabian L Kriegel Benjamin C Krause Yves U Hachenberger Rafael Fister Philipp Reichardt Jutta Tentschert Ajay-Vikram Singh Harald Jungnickel Peter Laux Andreas Luch Source Type: research

Transcriptional control of the oxidative stress response and implications of using plant derived molecules for therapeutic interventions in cancer
Curr Med Chem. 2021 Feb 17. doi: 10.2174/0929867328666210218110550. Online ahead of print.ABSTRACTOxidative stress response is critical for the malignant cells. It plays dual role by helping cancer cells survive and proliferate but also causing apoptosis and apoptosis like cell death. The oxidative stress response is characterized by a tight regulation of gene expression by a series of transcription factors (OSRts; oxidative stress response transcription factors). In this communication, we review the role of OSRts, notably NRF2 and p53 as well as other transcription factors, that modulate the response. We discuss how the o...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Asim Rizvi Mohd Farhan Faisal Nabi Rizwan Hasan Khan Mohd Adil Aamir Ahmad Source Type: research

Recent Multi-Target Approaches on the Development of Anti-Alzheimer`s Agents Integrating Metal Chelation Activity
Curr Med Chem. 2021 Feb 18. doi: 10.2174/0929867328666210218183032. Online ahead of print.ABSTRACTAlzheimer´s disease (AD) is the most common and severe age-dependent neurodegenerative disorder, worldwide. Notwithstanding the large amount of research dedicated to both the elucidation of this pathology and the development of an effective drug, the multifaceted nature and complexity of the disease are certainly a rationale for the absence of cure so far. Current available drugs are used, mainly, to compensate the decline of the neurotransmitter acetylcholine by acetylcholinesterase (AChE) inhibition, though they only p...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: S ílvia Chaves Katalin V árnagy M Am élia Santos Source Type: research

Current Trends in the Therapeutic Strategies for Diabetes Management
Curr Med Chem. 2021 Feb 18. doi: 10.2174/0929867328666210218183914. Online ahead of print.ABSTRACTDiabetes mellitus is one of the fastest growing noncommunicable disease. Diabetes mellitus is causes due to destruction of pancreatic beta cell or due to insulin resistance and characterised by hyperglycaemia. Diabetes imposes a very serious economic crisis as the diabetic drug market is growing very rapidly. Even after very path breaking scientific discoveries, availability of a better healthcare infrastructure, rise in literacy rates, the diabetes burden is continuously spreading in various sections all over the worlds but m...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Ponnurengam Malliappan Siva Kumar V Prabhawathi Ali Zarrabi Sohail Akthar Pranav Kumar Prabhakar Source Type: research

MicroRNAs in the Management of Heart Failure
CONCLUSION: MicroRNAs are involved in the regulation of multi biological processes involved in the progress of heart failure. More studies are needed to achieve a clinical valuable implementation of microRNAs in the management of HF.PMID:33602070 | DOI:10.2174/0929867328666210218181441 (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Aimilios Kalampogias Gerasimos Siasos Evangelos Oikonomou Konstantinos Mourouzis Evanthia Bletsa Panagiota K Stampouloglou Efstratios Katsianos Konstantinos Vlasis Georgios Marinos Georgios Charalambous Manolis Vavouranakis Dimitris Tousoulis Source Type: research

Viral Envelope Membrane: A Special Entry Pathway and a Promising Drug Target
Curr Med Chem. 2021 Feb 18. doi: 10.2174/0929867328666210218182203. Online ahead of print.ABSTRACTEnveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 pandemic. Thanks to their outer membrane, consisting essentially of host lipids, enveloped viruses are more resistant to enzymes, and are also less susceptible to host immune defenses than their naked counterparts. Therefore, the development of effective approaches to combat en...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Nastasja Palombi Annalaura Brai Martina Gerace Salvatore Di Maria Francesco Orofino Federico Corelli Source Type: research

Advances of Inorganic Materials in the Detection and Therapeutic Uses Against Coronaviruses
Curr Med Chem. 2021 Feb 19. doi: 10.2174/0929867328666210219142208. Online ahead of print.ABSTRACTCoronaviruses (CoVs) are enveloped viruses with particle-like characteristics and a diameter of 60-140 nm, positively charged, and single-stranded RNA genomes which produce a major outbreak of human fatal pneumonia since the beginning of the 21st century. COVID-19 is currently considered as a continuous potential pandemic threat across the globe. Therefore, considerable efforts have been made to develop innovative methods and technologies for suppressing the spread of viruses as well as inactivating the viruses but COVID-19 va...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Sathish Veerasamy Manivannan Chandrakumar Malathi Balasubramaniyan Ramesh Kumar Arumugam Thanasekaran Pounraj Source Type: research

The link between bacterial inflammagens, leaky gut syndrome and colorectal cancer
Curr Med Chem. 2021 Feb 19. doi: 10.2174/0929867328666210219142737. Online ahead of print.ABSTRACTThere is a causal relationship between cancer (including colorectal cancer), chronic systemic inflammation and persistent infections, and the presence of dysregulated circulating inflammatory markers. It is known that aberrant clot formation and coagulopathies occur in systemic inflammation. In colorectal cancer, there is close link between gut dysbiosis and an inflammatory profile. In this review we present evidence of the connection between gut dysbiosis, the entry of bacteria into the internal environment and the presence o...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Greta M de Waal Willem Js de Villiers Etheresia Pretorius Source Type: research

Advances of Inorganic Materials in the Detection and Therapeutic Uses Against Coronaviruses.
Abstract Coronaviruses (CoVs) are enveloped viruses with particle-like characteristics and a diameter of 60-140 nm, positively charged, and single-stranded RNA genomes which produce a major outbreak of human fatal pneumonia since the beginning of the 21st century. COVID-19 is currently considered as a continuous potential pandemic threat across the globe. Therefore, considerable efforts have been made to develop innovative methods and technologies for suppressing the spread of viruses as well as inactivating the viruses but COVID-19 vaccines are still in the development phase. This perspective focuses on the sensi...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: Veerasamy S, Chandrakumar M, Balasubramaniyan M, Arumugam RK, Pounraj T Tags: Curr Med Chem Source Type: research

The link between bacterial inflammagens, leaky gut syndrome and colorectal cancer.
Abstract There is a causal relationship between cancer (including colorectal cancer), chronic systemic inflammation and persistent infections, and the presence of dysregulated circulating inflammatory markers. It is known that aberrant clot formation and coagulopathies occur in systemic inflammation. In colorectal cancer, there is close link between gut dysbiosis and an inflammatory profile. In this review we present evidence of the connection between gut dysbiosis, the entry of bacteria into the internal environment and the presence of their highly potent inflammagenic molecules, such as lipopolysaccharide and li...
Source: Current Medicinal Chemistry - February 19, 2021 Category: Chemistry Authors: de Waal GM, de Villiers WJ, Pretorius E Tags: Curr Med Chem Source Type: research

Recent Multi-Target Approaches on the Development of Anti-Alzheimer`s Agents Integrating Metal Chelation Activity.
os MA Abstract Alzheimer´s disease (AD) is the most common and severe age-dependent neurodegenerative disorder, worldwide. Notwithstanding the large amount of research dedicated to both the elucidation of this pathology and the development of an effective drug, the multifaceted nature and complexity of the disease are certainly a rationale for the absence of cure so far. Current available drugs are used, mainly, to compensate the decline of the neurotransmitter acetylcholine by acetylcholinesterase (AChE) inhibition, though they only provide temporary symptomatic benefits and cannot stop AD progression. Alth...
Source: Current Medicinal Chemistry - February 18, 2021 Category: Chemistry Authors: Chaves S, Várnagy K, Santos MA Tags: Curr Med Chem Source Type: research

Current Trends in the Therapeutic Strategies for Diabetes Management.
Abstract Diabetes mellitus is one of the fastest growing noncommunicable disease. Diabetes mellitus is causes due to destruction of pancreatic beta cell or due to insulin resistance and characterised by hyperglycaemia. Diabetes imposes a very serious economic crisis as the diabetic drug market is growing very rapidly. Even after very path breaking scientific discoveries, availability of a better healthcare infrastructure, rise in literacy rates, the diabetes burden is continuously spreading in various sections all over the worlds but more especially in low- and middle-income countries. The recent development in sc...
Source: Current Medicinal Chemistry - February 18, 2021 Category: Chemistry Authors: Siva Kumar PM, Prabhawathi V, Zarrabi A, Akthar S, Prabhakar PK Tags: Curr Med Chem Source Type: research

MicroRNAs in the Management of Heart Failure.
CONCLUSION: MicroRNAs are involved in the regulation of multi biological processes involved in the progress of heart failure. More studies are needed to achieve a clinical valuable implementation of microRNAs in the management of HF. PMID: 33602070 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 18, 2021 Category: Chemistry Authors: Kalampogias A, Siasos G, Oikonomou E, Mourouzis K, Bletsa E, Stampouloglou PK, Katsianos E, Vlasis K, Marinos G, Charalambous G, Vavouranakis M, Tousoulis D Tags: Curr Med Chem Source Type: research

Viral Envelope Membrane: A Special Entry Pathway and a Promising Drug Target.
Abstract Enveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 pandemic. Thanks to their outer membrane, consisting essentially of host lipids, enveloped viruses are more resistant to enzymes, and are also less susceptible to host immune defenses than their naked counterparts. Therefore, the development of effective approaches to combat enveloped virus infections represents a major challenge for antiviral therapy in t...
Source: Current Medicinal Chemistry - February 18, 2021 Category: Chemistry Authors: Palombi N, Brai A, Gerace M, Di Maria S, Orofino F, Corelli F Tags: Curr Med Chem Source Type: research

An overview of the α4β1 integrin and the potential therapeutic role of its antagonists.
This article presents a simplified view of integrins with emphasis on the α4 (α4β1/VLA-4) integrin. Integrins are heterodimeric proteins expressed on the cell surface of leukocytes that participate in a wide variety of functions, such as survival, growth, differentiation, migration, inflammatory responses, tumour invasion, among others. When the extracellular matrix is degraded or deformed, cells are forced to undergo responsive changes that influence remodelling during physiological and pathological events. Integrins recognize these changes and trigger a series of cellular responses, forming a physical co...
Source: Current Medicinal Chemistry - February 17, 2021 Category: Chemistry Authors: Ferreira EFB, Silva LB, Cruz JV, Araújo PHF, Kimani NM, Leite FHA, Campos JM, Santos CBR Tags: Curr Med Chem Source Type: research

Transcriptional control of the oxidative stress response and implications of using plant derived molecules for therapeutic interventions in cancer.
Abstract Oxidative stress response is critical for the malignant cells. It plays dual role by helping cancer cells survive and proliferate but also causing apoptosis and apoptosis like cell death. The oxidative stress response is characterized by a tight regulation of gene expression by a series of transcription factors (OSRts; oxidative stress response transcription factors). In this communication, we review the role of OSRts, notably NRF2 and p53 as well as other transcription factors, that modulate the response. We discuss how the oxidative stress response is hierarchal and controls 'live or die' signals. This ...
Source: Current Medicinal Chemistry - February 17, 2021 Category: Chemistry Authors: Rizvi A, Farhan M, Nabi F, Khan RH, Adil M, Ahmad A Tags: Curr Med Chem Source Type: research

Antimicrobial activity of 5-membered nitroheteroaromatic compounds beyond nitrofurans and nitroimidazoles: recent progress.
Abstract The last decade has been characterized by the development and approval of pretomanid and delamanid, which are nitroimidazole based drugs for multidrug resistant tuberculosis. This attracted renewed attention to the nitroheterocyclic scaffolds as a source of safe and efficient antimicrobial agents. While the primary focus is still on nitrofurans and nitroimidazoles, well known as bioreducible prodrugs, a number of studies have been published on other 5-membered nitroheteroaromatic compounds. The latter not only show promising antimicrobial activity, but also demonstrate modes of action different from the c...
Source: Current Medicinal Chemistry - February 15, 2021 Category: Chemistry Authors: Kalinin S, Vedekhina T, Paramonova P, Krasavin M Tags: Curr Med Chem Source Type: research

Design and Synthesis of Novel Aminoalkanamides Targeting Neurodegeneration and Symptoms of Alzheimer's Disease.
CONCLUSION: This study revealed a new class of compounds that may be useful in the search for an effective drug in the alleviation of neurodegeneration and symptoms of Alzheimer's disease. PMID: 33588717 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 14, 2021 Category: Chemistry Authors: Jankowska A, Satała G, Latacz G, Partyka A, Lubelska A, Pociecha K, Świerczek A, Wilczyńska N, Mordyl B, Bojarski AJ, Wyska E, Chłoń-Rzepa G Tags: Curr Med Chem Source Type: research

From Nucleic Acids to Drug Discovery: Nucleobases as Emerging Templates for Drug Candidates.
Abstract Nucleobases represent key structural motif in biologically active molecules including synthetic and natural products. Molecular modifications made on nucleobases or their isolation from natural sources are being widely investigated for the development of drugs with improved potency for the treatment of different diseases, such as cancer, as well as viral and bacterial infections. This review article focuses on the nucleobase analogue drug developments of the past 20 years (2000-2020). Various pharmacological and medicinal aspects of nucleobases and their analogues are discussed. The current state and limi...
Source: Current Medicinal Chemistry - February 14, 2021 Category: Chemistry Authors: Wong XK, Yeong KY Tags: Curr Med Chem Source Type: research

Trefoil Factor Family (TFF) Peptides and their Different Roles in the Mucosal Innate Immune Defense and More: An Update.
Abstract Mucous epithelia are protected by complex mucus barrier layers, which are part of the innate immune defense. Trefoil factor family peptides TFF1, TFF2, and TFF3 have lectin activities and are predominantly co-secreted together with mucins from these epithelia. TFF1 and TFF2 are mainly expressed in the gastric mucosa; whereas TFF3 is rather widely secreted from most mucous epithelia and their glands. TFF1 and TFF3 consist of a single TFF domain and an additional free 7th cysteine residue; whereas TFF2 contains two TFF domains. Systematic analyses of the molecular forms of TFFs gave new insights into their ...
Source: Current Medicinal Chemistry - February 14, 2021 Category: Chemistry Authors: Hoffmann W Tags: Curr Med Chem Source Type: research

Nuclear long non-coding RNAs as epigenetic regulators in cancer.
Abstract BACKGROUND: Transcriptome analyses have revealed the presence of numerous long non-coding RNAs (lncRNAs) in mammalian cells. Many lncRNAs are expressed in development-, differentiation-, and disease-specific manners, suggesting their importance as cell regulators. Some nuclear lncRNAs are bound to specific genomic loci, either near or distant from their own transcription sites, and regulate gene expression in cis or trans. These lncRNAs recruit epigenetic factors, including the DNA methyl transferase and histone modification complex, and mediate both the 3D genome structure and nuclear domains. LncRNAs ar...
Source: Current Medicinal Chemistry - February 14, 2021 Category: Chemistry Authors: Tachiwana H, Saitoh N Tags: Curr Med Chem Source Type: research

Renin Angiotensin System in Central Nervous System diseases and its interaction with COVID-19.
CONCLUSION: Although there are limitations and controversies, the analysis of RAS mechanisms in the CNS certainly represents an interesting field of research. However, further investigation is necessary to support the noteworthy interactions and provide a better comprehension of the cross-talk between RAS and the CNS. Investigations in this research field may shed lights to novel therapeutic targets. PMID: 33583366 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 11, 2021 Category: Chemistry Authors: Lanza K, Dias R, Dos Santos Oliveira R, Belotto L, Miranda AS, Simões E Silva AC Tags: Curr Med Chem Source Type: research

Novel biomarkers for lupus nephritis in the "OMICS" era.
Novel biomarkers for lupus nephritis in the "OMICS" era. Curr Med Chem. 2021 Feb 11;: Authors: Dias R, Hasparyk UG, Peres ML, de Barros JLVM, Simões E Silva AC Abstract Lupus nephritis (LN) is a severe renal comorbidity associated with systemic lupus erythematosus (SLE), a complex autoimmune disorder with high morbidity and mortality. Diagnosis and monitoring of LN patients still rely on renal biopsy, a procedure that exposes patients to a variety of risks and is not capable of providing longitudinally information about disease prognosis. In this review, we summarized current data of ...
Source: Current Medicinal Chemistry - February 11, 2021 Category: Chemistry Authors: Dias R, Hasparyk UG, Peres ML, de Barros JLVM, Simões E Silva AC Tags: Curr Med Chem Source Type: research

Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives Based on 5-Fluorouracil.
ez-Malule H Abstract Cancer still continues as an important cause of death worldwide. Thus, several conventional anticancer treatments are widely used, however, most of them display low selectivity against malignant cells and induce many adverse side effects. Among these, the use of therapies based on 5-Fluorouracil (5-FU) has been one of the most efficient, with a broad-spectrum. Due to these circumstances, various modifications of 5-FU have been developed to improve drug delivery and reduce side effects. Among the optimization strategies, modifications of 5-FU at N1 or N3 position are made, usually including inc...
Source: Current Medicinal Chemistry - February 11, 2021 Category: Chemistry Authors: Cardona-G W, Herrera-R A, Castrillón-L W, Ramírez-Malule H Tags: Curr Med Chem Source Type: research

The Impact of CrystallographicData for the Development of Machine Learning Models to Predict Protein-Ligand Binding Affinity.
CONCLUSION: The rapid increase in the number of crystal structures of protein-ligand complexes created a favorable scenario for developing machine learning models to predict binding affinity. These models rely on experimental data from two sources, the structural and the affinity data. The combination of experimental data generates computational models that outperform classical scoring functions. PMID: 33568025 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 10, 2021 Category: Chemistry Authors: Veit-Acosta M, de Azevedo Junior WF Tags: Curr Med Chem Source Type: research

The Yin and Yang of High-density Lipoprotein and Atherosclerotic Cardiovascular Disease: Focusing on Functionality and Cholesterol Efflux to Reframe the HDL Hypothesis.
Abstract The inverse relationship between low plasma high-density lipoprotein cholesterol (HDL-C) concentrations and increased risk of Atherosclerotic Cardiovascular Disease (ASCVD) is well-known. However, plasma HDL-C concentrations are highly variable in subjects with ASCVD. In clinical outcome trials, pharmacotherapies that increase HDL-C concentrations are not associated with a reduction in ASCVD events. A causal relationship between HDL-C and ASCVD has also been questioned by Mendelian randomization studies and genome-wide association studies of genetic variants associated with plasma HDL-C concentrations. Th...
Source: Current Medicinal Chemistry - February 8, 2021 Category: Chemistry Authors: Ganjali S, Watts GF, Banach M, Reiner Ž, Nachtigal P, Sahebkar A Tags: Curr Med Chem Source Type: research

Nucleoside Inhibitors of Coronaviruses.
Abstract Coronaviruses (CoVs) belong to a large family of zoonotic supercapsid viruses, including about 40 species of RNA-containing viruses with several strains capable of causing damage to the lungs and respiratory tract. The severe acute respiratory syndrome coronavirus (SARS-CoV) was responsible for the worldwide SARS outbreak in 2003. The rapid global spread of SARS-CoV-2 has been the cause of significant health concern and thousands of deaths in 2019-2020 and outlined the need for novel antivirals. The present review is devoted to the development of effective and selective nucleoside drugs for the treatment ...
Source: Current Medicinal Chemistry - February 8, 2021 Category: Chemistry Authors: Zenchenko AA, Drenichev MS, Mikhailov SN Tags: Curr Med Chem Source Type: research

Current phthalocyanines delivery systems in photodynamic therapy: an updated review.
Abstract Photodynamic therapy has emerged as an effective therapeutic alternative to treat oncological, cardiovascular, dermatological, infectious, and ophthalmic diseases. Photodynamic therapy combines the action of a photosensitizer with light in the presence of oxygen to generate reactive oxygen species capable of reacting with cellular components resulting in injury and, consequently, inducing cellular death. Phthalocyanines are considered good photosensitizers, although most of them are lipophilic, difficulting their administration for clinical use. A strategy to overcome the lack of solubility of phthalocyan...
Source: Current Medicinal Chemistry - February 7, 2021 Category: Chemistry Authors: Miretti M, Prucca CG, Tempesti TC, Baumgartner MT Tags: Curr Med Chem Source Type: research

Advancements within modern machine learning methodology: Impacts and prospects for biomarker discovery.
Conclusion The use of machine learning methodologies for biomarker discovery is critical to the analysis of various types of data used for biomarker discovery, such as mass spectrometry, nucleotide and protein sequencing, and image (e.g. CT-scan) data. Further studies containing more standardized techniques for evaluation, and the use of cutting-edge machine learning architectures may lead to more accurate and specific results. PMID: 33557728 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 7, 2021 Category: Chemistry Authors: Ledesma D, Symes S, Richards S Tags: Curr Med Chem Source Type: research

A Review of Water-Resistant Cellulose-Based Materials in Pharmaceutical and Biomedical Application.
CONCLUSION: Currently, water-resistant cellulose-based materials were mainly applied in water-insoluble drugs delivery carriers, wound dressing and medical diagnosis and presented great application prospects. However, the contradiction between hydrophobicity and mechanical properties of these reported water-resistant cellulose-based materials limited their wider application in biomedicine such as tissue engineering. In the future, attention will be focused on the higher hydrophobicity of water-resistant cellulose-based materials with excellent mechanical properties. In addition, clinical medical research of water-resistant...
Source: Current Medicinal Chemistry - February 7, 2021 Category: Chemistry Authors: He B, Liu X, Qi S, Zheng R, Chang M, Lin Q, Ren J Tags: Curr Med Chem Source Type: research

Novel nitrogen containing steroid derivatives for prostate cancer treatment.
Abstract This mini review focuses on the investigation of novel nitrogen containing steroid derivatives potentially applicable for prostate cancer treatment. It covers last decade of literature with highlights on the structure of new steroid compounds exhibiting significant activity in prostate cancer cells and possessing pharmacological potency. New derivatives of known anti-prostate cancer agents: abiraterone and galeterone, new derivatives of androstane and pregnane modified with nitrogen containing heterocycles, and some related steroid derived compounds are discussed in the review. PMID: 33557730 [PubMed...
Source: Current Medicinal Chemistry - February 7, 2021 Category: Chemistry Authors: Latysheva AS, Zolottsev VA, Pokrovsky VS, Khan II, Misharin AY Tags: Curr Med Chem Source Type: research

Development of Novel Rhodacyanine-Based Heat Shock Protein 70 Inhibitors.
CONCLUSION: Together with the finding that compounds 1 and 6 showed improved microsomal stability, these results suggest the translational potential of these putative Hsp70 inhibitors to foster new strategies for cancer therapy. However, whether these benzo-fused rhodacyanines act on kinases or other targets remains unclear, which is currently under investigation. PMID: 33538660 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 3, 2021 Category: Chemistry Authors: Chang CS, Kumar V, Lee DY, Chen Y, Wu YC, Gao JY, Chu PC Tags: Curr Med Chem Source Type: research

Monoamineoxidase-B (MAO-B) Inhibitors in theTreatment of Alzheimer's and Parkinson's Disease.
CONCLUSION: Many studies demonstrate that MAO-B activity increases with age in brain tissue, cerebrospinal fluid (CSF), and platelets in Alzheimer's patients. This suggests that MAO-B inhibitor drugs, which may be effective in the treatment of Parkinson's disease, may also be effective in the treatment of Alzheimer's disease. This article was written to explain the multifaceted MAO-B inhibitor molecules. PMID: 33538661 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 3, 2021 Category: Chemistry Authors: Özdemir Z, Alagöz MA, Bahçecioğlu ÖF, Gök S Tags: Curr Med Chem Source Type: research

Artificial Intelligence: the "Trait D'Union" in Different Analysis Approaches of Autism Spectrum Disorder Studies.
Artificial Intelligence: the "Trait D'Union" in Different Analysis Approaches of Autism Spectrum Disorder Studies. Curr Med Chem. 2021 Feb 03;: Authors: Marciano F, Venutolo G, Ingenito CM, Verbeni A, Terracciano C, Plunk E, Garaci F, Cavallo A, Fasano A Abstract Autistic Spectrum Disorder (ASD) is a neurodevelopmental condition affecting approximately 1 out of 70 (range 1:59 - 1:89) children worldwide. It is characterized by a delay in cognitive capabilities, repetitive and restricted behaviors and deficit in communication and social interaction. Several factors seem to be associated with A...
Source: Current Medicinal Chemistry - February 3, 2021 Category: Chemistry Authors: Marciano F, Venutolo G, Ingenito CM, Verbeni A, Terracciano C, Plunk E, Garaci F, Cavallo A, Fasano A Tags: Curr Med Chem Source Type: research

Application of Microfluidics in Single-cell Manipulation, Omics and Drug Development.
CONCLUSION: Microfluidics is a robust platform technology which is able to accomplish rare cell separation, efficient single-cell omics analysis and provide a platform for drug development and drug delivery. PMID: 33538663 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 3, 2021 Category: Chemistry Authors: Abdulla A, Maboyi N, Ding X Tags: Curr Med Chem Source Type: research

Recent Progress in Small Molecular Inhibitors of DNA Gyrase.
CONCLUSION: We briefly summed up the current situation and future challenges on this topic. Through the discussion of the design strategies and drug effect, we hope that this review can provide focused direction for future researches. PMID: 33530900 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - February 1, 2021 Category: Chemistry Authors: Man RJ, Zhang XP, Yang YS, Jiang AQ, Zhu HL Tags: Curr Med Chem Source Type: research

Dynamics of Toll-like receptors signaling in skeletal muscle atrophy.
Abstract Skeletal muscle atrophy has been characterizedas a state of uncontrolled inflammation and oxidative stress that escalates the protein catabolism. Recent advancement supportsthat impinging signaling molecules in the muscle fibers controlled throughtoll-like receptors (TLR). Activated TLR signalingpathways have been identified as inhibitors of muscle mass and provoke the settings for muscle atrophy. Among them, mainly TLR2 and TLR4 manifest their presence to exacerbate the release of the pro-inflammatory cytokine to deform the synchronized muscle programming. The present review enlightens the TLR signaling ...
Source: Current Medicinal Chemistry - February 1, 2021 Category: Chemistry Authors: Yadav A, Dahuja A, Dabur R Tags: Curr Med Chem Source Type: research

A Review of Light Sources and Enhanced Targeting for Photodynamic Therapy.
Abstract Photodynamic Therapy (PDT), as a clinically approved modality for the treatment of various disordered diseases including cancer, has received great advances in recent years. By preferentially accumulating non-toxic Photosensitizers (PSs) in the pathological area, and in situ generation of cytotoxic reactive oxygen species (ROS) under local irradiation by a light source with appropriate wavelength, PDT works in a dual-selective manner. Over the past decades, numerous studies and reviews on PDT mainly focused on activable PSs and the newly emerging PSs in PDT. However, to the best of our knowledge, there ar...
Source: Current Medicinal Chemistry - January 21, 2021 Category: Chemistry Authors: Xiang M, Zhou Q, Shi Z, Wang X, Li M, Jia Y, Li S, Yang F, Wang W, Sharma B, Nie Y, Xiao Q, Gao L, Chen T, Xu X Tags: Curr Med Chem Source Type: research

Ethnomedicinal plants for the management of diabetes worldwide: A systematic review.
CONCLUSION: This review is the first to provide a compiled list of traditional medicinal plants used worldwide against diabetes. PMID: 33475054 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 21, 2021 Category: Chemistry Authors: Aumeeruddy MZ, Mahomoodally MF Tags: Curr Med Chem Source Type: research

NAD precursors, mitochondria targeting compounds and ADPribosylation inhibitors in treatment of inflammatory diseases and cancer.
Abstract Mitochondrial dysfunction and oxidative stress are prominent features of a plethora of human disorders. Dysregulation of mitochondrial functions represents a common pathogenic mechanism of diseases such as neurodegenerative disorders and cancer. The maintenance of the Nicotinamide adenine dinucleotide (NAD+ ) pool, and a positive NAD+ /NADH ratio, are essential for mitochondrial and cell functions. The synthesis and degradation of NAD+ and transport of its key intermediates among cell compartments play an important role to maintain optimal NAD levels, for regulation of NAD+ -utilizing enzymes, such as sir...
Source: Current Medicinal Chemistry - January 18, 2021 Category: Chemistry Authors: Poltronieri P, Mezzolla V, Farooqi AA, Di Girolamo M Tags: Curr Med Chem Source Type: research

Preparation and formulation optimization of methotrexate-loaded human serum albumin nanoparticles modified by mannose.
CONCLUSION: This targeting drug delivery system laid a promising foundation for the treatment of RA. PMID: 33461449 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 17, 2021 Category: Chemistry Authors: Chen Z, Luo Z, Lyu J, Wang J, Liu Z, Wei J, Lin Y, Zhong Z Tags: Curr Med Chem Source Type: research

Recent advances in small-molecule HIV-1 integrase inhibitors.
Abstract HIV-1 integrase catalyzed the insertion of the viral DNA into the genome of human cells in the process of retrotranscription. Integrase is an attractive target for HIV-1 treatment due to the lack of its homologue in human cells and its vital role in HIV-1 replication. Although a major progress about the development of HIV-1 integrase inhibitors has been made, some thorny problems, such as the drug resistance, led to the further study of HIV-1 integrase inhibitors. This review briefly discussed the structure, function and mechanism of catalysis of HIV-1 integrase and made a further conclusion for recent ad...
Source: Current Medicinal Chemistry - January 14, 2021 Category: Chemistry Authors: Zhang C, Xie Q, Wan CC, Jin Z, Hu C Tags: Curr Med Chem Source Type: research

Extracellular Vesicles in the Treatment of Parkinson's Disease: A Review.
CONCLUSION: PD is a heterogeneous disease that can be treated by using pharmacologic approaches (e.g., dopamine agonists and levodopa) and nonpharmacologic approaches (e.g., music), based on symptoms and progression level in patients. Even though current treatments have demonstrated effectiveness, clinical challenges remain because the BBB reduces medication received and lowers the efficacy of drug delivery, which impairs the treatment's effect. Therefore, EVs, as an emerging delivery platform, are highly promising for PD treatment since they can readily cross the BBB with high therapeutic efficiency through the loading or...
Source: Current Medicinal Chemistry - January 13, 2021 Category: Chemistry Authors: Yang X, Ma Y, Xie H, Dong S, Rao G, Yang Z, Zhang J, Wu Q Tags: Curr Med Chem Source Type: research

Neurokinin-1 receptor (NK-1R) antagonists: potential targets in the treatment of glioblastoma multiforme.
Abstract The current standard of care in glioblastoma multiforme (GBM), as the most morbid brain tumor, is not adequate, despite substantial progress in cancer therapy. Among patients receiving current standard treatments, including surgery, irradiation, and chemotherapy, the overall survival (OS) period with GBM is less than one year. The high mortality frequency of GBM is due to its aggressive nature, including accelerated growth, deregulated apoptosis, and invasion into surrounding tissues. The understanding of the molecular pathogenesis of GBM is, therefore, crucial for identifying, designing, and repurposing ...
Source: Current Medicinal Chemistry - January 13, 2021 Category: Chemistry Authors: Afshari AR, Motamed-Sanaye A, Sabri H, Soltani A, Karkon-Shayan S, Radvar S, Javid H, Mollazadeh H, Sathyapalan T, Sahebkar A Tags: Curr Med Chem Source Type: research

Deep learning in the quest for compound nomination for fighting COVID-19.
Abstract The current COVID-19 pandemic gave rise to an unprecedented response from clinicians and the scientific community in all relevant biomedical fields. This created an incredible multidimensional data-rich framework in which deep learning proved instrumental to make sense of the data and build models used in prediction-validation workflows that in a matter of months have already produced results in assessing the spread of the outbreak, its taxonomy, population susceptibility, in diagnostics or drug discovery and repurposing. More is expected to come in the near future from using such advanced machine learnin...
Source: Current Medicinal Chemistry - January 13, 2021 Category: Chemistry Authors: Mernea M, Martin EC, Petrescu AJ, Avram S Tags: Curr Med Chem Source Type: research

Machine Learning Approaches in Parkinson's Disease.
CONCLUSION: Machine learning algorithms are computer-based statistical approaches which can be trained and are able to find common patterns from big amounts of data. The machine learning approaches can help clinicians in classifying patients according to several variables at the same time. PMID: 33430721 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 11, 2021 Category: Chemistry Authors: Landolfi A, Ricciardi C, Donisi L, Cesarelli G, Troisi J, Vitale C, Barone P, Amboni M Tags: Curr Med Chem Source Type: research

Recent Advances in the Synthesis and Development of Curcumin, its Combinations, Formulations and Curcumin-like Compounds as Antiinfective Agents.
Abstract Infectious diseases are caused by pathogenic microorganisms, such as bacteria, fungi, parasites and viruses. Such diseases mostly develop in tropical and sub-tropical climates and represent major health challenges. The pathogens of these diseases are able to multiply in human hosts, warranting their continual survival. Treatment is becoming extremely difficult, due to the absence of effective vaccines and the emergence of resistance by their causative pathogens to existing drugs. Several currently available drugs employ oxidative stress, resulting from the generation of reactive oxygen nitrogen species (R...
Source: Current Medicinal Chemistry - January 10, 2021 Category: Chemistry Authors: Kannigadu C, N'Da DD Tags: Curr Med Chem Source Type: research

Alport Syndrome: a comprehensive review on genetics, pathophysiology, histology, clinical, and therapeutic perspectives.
CONCLUSION: AS is still a greatly under and misdiagnosed disorder. The pathophysiology is still not fully unnderstand and genetics of the disease have also some gaps. Up to know, there is no specific and effective treatment for AS. Further studies are necessary to establish novel and effective therapeutic protocols. PMID: 33423643 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 7, 2021 Category: Chemistry Authors: Pedrosa AL, Bitencourt L, Paranhos RM, Leitão CA, Ferreira GC, Simões E Silva AC Tags: Curr Med Chem Source Type: research

Machine Intelligence Techniques for the Identification and Diagnosis of COVID-19.
Abstract COVID-19, an infectious disease caused by a newly discovered enveloped virus (SARS-CoV-2), was first reported in Wuhan, China, in December 2019 and affected the whole world. The infected individual may develop symptoms such as high fever, cough, myalgia, lymphopenia, respiratory distress syndrome etc. or remain completely asymptomatic after the incubation period of two to fourteen days. As the virus is transmitted by inhaling infectious respiratory droplets that are produced by sneezing or coughing, so early and rapid diagnosis of the disease can prevent infection and transmission. In the current pandemic...
Source: Current Medicinal Chemistry - January 6, 2021 Category: Chemistry Authors: Zaib S, Rana N, Noor A, Khan I Tags: Curr Med Chem Source Type: research