Cheminformatics Toolboxes and Workflows within KNIME Analytics.
PMID: 33222663 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 25, 2020 Category: Chemistry Authors: Afantitis A, Melagraki G Tags: Curr Med Chem Source Type: research

Using a hybrid radioenhancer to realize tumor cell-targeted treatment for osteosarcoma: an in vitro study.
In this study, we developed an innovative method for treating osteosarcoma by using a novel radiation-enhancer (i.e., carboxymethyl-hexanoyl chitosan-coated selfassembled Au@Fe3O4 nanoparticles; CSAF NPs). CSAF NPs were employed together with 5-aminolevulinic acid (5-ALA) to achieve tumor cell-targeted radiotherapy. In this study, osteosarcoma cells (MG63) and normal cells (MC3T3-E1) were used for an in vitro investigation, in which a reactive oxygen species (ROS) assay, cell viability assay, clonogenic assay, and western blot were used to confirm the treatment efficiency. The ROS assay showed that the combination of CSAF ...
Source: Current Medicinal Chemistry - November 18, 2020 Category: Chemistry Authors: Tung FI, Chen LC, Wang YC, Chen MH, Shueng PW, Liu TY Tags: Curr Med Chem Source Type: research

Vitamin D/VDR in acute kidney injury: a potential therapeutic target.
Abstract Despite many strategies and parameters used in clinical practice, the incidence and mortality of acute kidney injury (AKI) are still high with poor prognosis. With the development of molecular biology, the role of vitamin D and vitamin D receptor (VDR) in AKI is drawing increasing attention. Accumulated researches have suggested that Vitamin D deficiency is a risk factor of both clinical and experimental AKI, and vitamin D/VDR could be a promising therapeutic target against AKI. However, more qualitative clinical researches are needed to provide stronger evidence for clinical application of vitamin D and ...
Source: Current Medicinal Chemistry - November 18, 2020 Category: Chemistry Authors: Jiang S, Huang L, Zhang W, Zhang H Tags: Curr Med Chem Source Type: research

Exosome-mediated drug delivery for cell-free therapy of osteoarthritis.
Abstract Osteoarthritis (OA) is a degenerative disease of cartilage and bones, which results in severely compromised quality of life in the aged population. However, currently no ideal treatment strategies have been developed to prevent the OA progression. Cell therapies such as chondrocyte and MSC transplantation have been extensively tested and evaluated in clinical trials. Yet, until to date, the clinical efficacy of articular injection of stem cells in OA has not been convincingly demonstrated. Recent studies have indicated that exosomes, one type of Extracellular Vesicles (EVs) play an important regulatory ro...
Source: Current Medicinal Chemistry - November 18, 2020 Category: Chemistry Authors: Duan L, Xu X, Xu L, Chen H, Li X, Alahdal M, Xiao Y, Liang Y, Xia J Tags: Curr Med Chem Source Type: research

Recent advances in small molecule PROTACs for the treatment of cancer.
Abstract The PROTAC (PROteolysis TArgeting Chimera) technology is a target protein degradation strategy, based on the ubiquitin-proteasome system, which has been gradually developed into a potential means of targeted cancer therapy in recent years. This strategy has already shown significant advantages over traditional small-molecule inhibitors in terms of pharmacodynamics, selectivity, and drug resistance. Several small molecule PROTACs have been in a Phase I clinical trial. Herein, we introduced the mechanism, characteristics, and advantages of PROTAC strategy. And we summarize the recent advances in the develop...
Source: Current Medicinal Chemistry - November 17, 2020 Category: Chemistry Authors: Li W, Elhassan RM, Hou X, Fang H Tags: Curr Med Chem Source Type: research

Artificial Intelligence for epigenetics: towards personalized medicine.
Abstract Epigenetics is a field of biological sciences focused on the study of reversible, heritable changes in gene function not due to modifications of the genomic sequence. These changes are the result of a complex cross-talk between several molecular mechanisms, that is in turn orchestrated by genetic and environmental factors. The epigenetic profile captures the unique regulatory landscape and the exposure to environmental stimuli of an individual. It thus constitutes a valuable reservoir of information for personalized medicine, which is aimed at customizing health-care interventions based on the unique char...
Source: Current Medicinal Chemistry - November 17, 2020 Category: Chemistry Authors: De Riso G, Cocozza S Tags: Curr Med Chem Source Type: research

The association between migraine and depression based on miRNA biomarkers and cohort studies.
CONCLUSIONS: The evidence based on both molecular and epidemiological data reveals the significant association between MD and migraine. This result can help investigate the correlated underlying mechanism of these two diseases. PMID: 33208058 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 16, 2020 Category: Chemistry Authors: Chen YH, Wang H Tags: Curr Med Chem Source Type: research

Potential use of RNA-based therapeutics for breast cancer treatment.
Abstract Breast cancer is one of the most lethal cancers in women worldwide, and the development of efficient treatments faces several challenges. Breast cancer is characterized by histological and functional heterogeneity in aspects such as tumorigenesis, metastasis and drug resistance. RNA therapy has emerged as highly attractive classes of drugs for the treatment and prevention of breast cancer. It might play remarkable regulatory roles in the treatment of targeted cells by either increasing or silencing expressions of specific proteins, and such features of RNA-based drugs cause high selectivity and low risk o...
Source: Current Medicinal Chemistry - November 16, 2020 Category: Chemistry Authors: Song Y, Ke X, Leilei PC Tags: Curr Med Chem Source Type: research

An Overview of the Compounds Tested In Vivo for Leishmania spp. of the Last 5 Years.
CONCLUSION: Drug repurposing and new formulations of already-known drugs are worthwhile approaches to promptly introduce new treatment schemes to Leishmaniasis. Nevertheless, the interest in new synthetic compounds and new formulations brings light to new treatment proposals and are notable lines of research. PMID: 33198609 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 16, 2020 Category: Chemistry Authors: de Barros Dias MCH, Freitas LAB, Dos Santos IR, de Almeida VS, do Amaral E Melo RT, de Melo Silva VG, de Santana BFM, da Conceição JM, Lima Leite AC Tags: Curr Med Chem Source Type: research

Evaluation of the Therapeutic Effect of Lycoramine on Alzheimer's Disease in Mouse Model.
CONCLUSION: Lycoramine shows therapeutic potential to halt and reverse cognitive decline at the late stages of disease progression, and holds great promise for the treatment of Alzheimer's disease. PMID: 33200692 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 16, 2020 Category: Chemistry Authors: Kiris I, Basar MK, Sahin B, Gurel B, Coskun J, Mroczek T, Baykal AT Tags: Curr Med Chem Source Type: research

EndMT: Potential Target of H2S Against Atherosclerosis.
Abstract Atherosclerosis is a chronic arterial wall illness that forms atherosclerotic plaques within the arteries. Plaque formation and endothelial dysfunction are atherosclerosis' characteristics. It is believed that the occurrence and development of atherosclerosis mainly include endothelial cell damage, lipoprotein deposition, inflammation and fibrous cap formation, but its molecular mechanism has not been elucidated. Therefore, protecting the vascular endothelium from damage is one of the key factors against atherosclerosis. The factors and processes involved in vascular endothelial injury are complex. Findin...
Source: Current Medicinal Chemistry - November 16, 2020 Category: Chemistry Authors: Liu HT, Zhou ZX, Ren Z, Yang S, Liu LS, Wang Z, Wei DH, Ma XF, Ma Y, Jiang ZS Tags: Curr Med Chem Source Type: research

Recent development of novel HDAC6 isoform-selective inhibitors.
Abstract As an important posttranscription modification, histone deacetylation plays significant roles in chromatin remodeling and gene expression. The aberrant modification of histone deacetylation leads to various diseases. As a critical member of histone deacetylase (HDAC), HDAC6 serves as a key modulator in many physiological processes. Abnormal expression of HDAC6 gives rise to cancer, neurodegeneration and other diseases. Here, we reviewed recent advances in physiological, protein structure and development of HDAC6 selective inhibitors. PMID: 33176627 [PubMed - as supplied by publisher] (Source: Current...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Zhao Y, Liang T, Hou X, Fang H Tags: Curr Med Chem Source Type: research

High-Intensity Focused Ultrasound in the Treatment of Breast Cancer.
Abstract High-intensity focused ultrasound (HIFU) is a noninvasive method of ablating malignant tumors. This paper will review the current clinical application of HIFU specially in the treatment of breast cancer. In addition to clinical studies, this review will also look into some basic studies that could address the technical issues related to this modality. In general, HIFU is considered to be safe being noninvasive and non-ionizing. Complication occurrence rate is low and repeated treatment is possible, making it an attractive option for some patients. However, for more than two decades since it was first used...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Feril LB, Fernan RL, Tachibana K Tags: Curr Med Chem Source Type: research

Recent Advances on Paclitaxel-based Self-Delivery Nanomedicine for Cancer Therapy.
Abstract Paclitaxel (PTX) is the first natural plant-derived chemotherapeutic drug approved by the Food and Drug Administration. However, the clinical applications of PTX are limited by some drawbacks, such as poor water solubility, rapid blood clearance, nonspecific distribution, and adverse side effects. Nanocarriers have made important contributions for drug delivery and cancer therapy in recent years. However, low drug loading capacity, nanocarrier excipients-induced toxicity or immunogenicity, and complicated synthesis technologies pose a challenge for the clinical application of nanocarriers. To address thes...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Zhou M, Han S, An F Tags: Curr Med Chem Source Type: research

New Perspectives of Machine Learning in Drug Discovery.
Abstract Artificial intelligence methods, in particular, machine learning, has been playing a pivotal role in drug development, from structural design to clinical trial. This approach is harnessing the impact of computer-aided drug discovery thanks to large available data sets for drug candidates and its new and complex manner of information interpretation to identify patterns for the study scope. In the present review, recent applications related to drug discovery and therapies are assessed, and limitations and future perspectives are analyzed. PMID: 33176630 [PubMed - as supplied by publisher] (Source: Curr...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Musella S, Verna G, Fasano A, Di Micco S Tags: Curr Med Chem Source Type: research

Harnessing phage display for the discovery of peptide-based drugs and monoclonal antibodies.
Abstract Phage display is a powerful high-throughput screening technology that presents a large and diverse selection of functional peptides, proteins, or antibody fragments on phage capsid surfaces for affinity determination towards a target of interest. Due to its advantages of a large screening capacity, mass production through fermentation, and straightforward execution, phage display has been widely used in bioengineering and biomedicine, especially for diagnostics and therapeutics. With the advent of next-generation sequencing and microfluidics technologies, phage display has become an even more powerful and...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Li Y, Liu M, Xie S Tags: Curr Med Chem Source Type: research

Anti-tumor Effects of Curcuminoids in Glioblastoma Multiforme: An Updated Literature Review.
This study reviews the observations regarding the impact of curcumin and its derivatives on GBM and the potential of translating the research findings into the clinic. PMID: 33176632 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Afshari AR, Jalili-Nik M, Abbasinezhad-Moud F, Javid H, Karimi M, Mollazadeh H, Jamialahmadi T, Sathyapalan T, Sahebkar A Tags: Curr Med Chem Source Type: research

E6 and E7 oncoproteins: Potential targets of cervical cancer.
Abstract Cervical cancer (CC) is the fourth leading cancer in women in the age group 15-44 globally. Experimental as well as epidemiological studies identified that type16 and 18 HPV cause 70% of precancerous cervical lesions as well as cervical cancer worldwide by bringing about genetic as well as epigenetic changes in the host genome. The insertion of the HPV genome triggers various defense mechanisms including the silencing of tumor suppressor genes as well as activation of oncogenes associated with cancer metastatic pathway. E6 and E7 are small oncoproteins consisting of 150 and 100 amino acids respectively. T...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Malla R, Kamal MA Tags: Curr Med Chem Source Type: research

Polyisoprenylated Cysteinyl Amide Inhibitors: A Novel Approach to Controlling Cancers with Hyperactive Growth Signaling.
Abstract Aberrant activation of monomeric G-protein signaling pathways drives some of the most aggressive cancers. Suppressing these hyperactivities has been the focus of efforts to obtain targeted therapies. Polyisoprenylated methylated protein methyl esterase (PMPMEase) is overexpressed in various cancers. Its inhibition induces the death of cancer cells that harbor the constitutively active K-Ras proteins. Furthermore, the viability of cancer cells driven by factors upstream of KRas, such as overexpressed growth factors and their receptors or the mutationally-activated receptors is also susceptible to PMPMEase ...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Lamango NS, Nkembo AT, Ntantie E, Tawfeeq N Tags: Curr Med Chem Source Type: research

Review-Recent Advancements in Electrochemical Biosensors for Alzheimer's Disease Biomarkers Detection.
CONCLUSIONS: The article focuses on various strategies of biosensor chemical surface modifications to immobilize biorecognition molecules, enabling specific, quantitative AD biomarker detection in synthetic and clinical samples. In addition, this is the first review that presents innovative single-platform systems for simultaneous detection of multiple biomarkers and other important AD-associated biological species based on electrochemical techniques. The importance of these platforms in disease diagnosis is discussed. PMID: 33176635 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Mikuła E Tags: Curr Med Chem Source Type: research

A critical transcription factor NF- κB as a cancer therapeutic target and its inhibitors as cancer treatment options.
A critical transcription factor NF-κB as a cancer therapeutic target and its inhibitors as cancer treatment options. Curr Med Chem. 2020 Nov 11;: Authors: Suhail M, Tarique M, Muhammad N, Naz H, Hafeez A, Zughaibi TA, Kamal MA, Rehan M Abstract Nuclear Factor-κappa B (NF-κB) is a family of critical transcription factors of inflammatory pathway and plays an imperative role in the progression of various cancers such as breast, lung, liver, pancreatic, prostate and multiple types of lymphoma. NF-κB develops an inherent relationship between inflammation and cancer. It is a crucial ...
Source: Current Medicinal Chemistry - November 11, 2020 Category: Chemistry Authors: Suhail M, Tarique M, Muhammad N, Naz H, Hafeez A, Zughaibi TA, Kamal MA, Rehan M Tags: Curr Med Chem Source Type: research

mTor Targeting by Different Flavonoids for Cancer Prevention.
Abstract Over the past several decades, plant-derived products (phytochemicals) have been suggested to possess immense therapeutic potential. Among these phytochemicals, different flavonoids have been reported for their potent anticancer activity. To exhibit their anticancer potential, these flavonoids modulate different signaling pathways. Among these pathways, the mammalian target of rapamycin (mTOR) and associated phosphatidyl-inositiol 3-kinase (PI3K)/protein kinase B (Akt) signaling cascade has been suggested as a pivotal modulator of cell survival, proliferation, and death/apoptosis. Hence, targeting this ca...
Source: Current Medicinal Chemistry - November 9, 2020 Category: Chemistry Authors: Badar Ul Islam, Khan MS, Husain FM, Rehman MT, Alzughaibi TA, Abuzenadah AM, Urooj M, Kamal MA, Tabrez S Tags: Curr Med Chem Source Type: research

Cell-to-cell transmission of the unfolded protein response - is it a real phenomenon?
PMID: 33153417 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 5, 2020 Category: Chemistry Authors: Bozko M, Bozko P Tags: Curr Med Chem Source Type: research

Targeted Delivery of Natural Bioactives and Lipid-nanocargos against Signaling Pathways Involved in Skin Cancer.
Abstract At present, skin cancer is a widespread malignancy in human beings. Among diverse population types, Caucasian populations are much more prone in comparison to darker skin populations due to the comparative lack of skin pigmentation. Skin cancer is divided into malignant and non-melanoma skin cancer, which is additionally categorized as basal and squamous cell carcinoma. The exposure to ultraviolet radiation, chemical carcinogen (polycyclic aromatic hydrocarbons, arsenic, tar, etc.), and viruses (herpes virus, human papillomavirus, and human T-cell leukemia virus type-1) are major contributing factors of s...
Source: Current Medicinal Chemistry - November 4, 2020 Category: Chemistry Authors: Iqubal MK, Chaudhuri A, Iqubal A, Saleem S, Gupta MM, Ahuja A, Ali J, Baboota S Tags: Curr Med Chem Source Type: research

The role of MIF in hepatic function, oxidative stress, and inflammation in thioacetamide-induced liver injury in mice: Protective effects of betaine.
CONCLUSION: MIF is mediator in hepatotoxic, pro-oxidative and proinfammatory effects of TAA-induced liver injury. MIFtargeted therapy could potentially mitigate the oxidative stress and inflammation in the liver, but the exact mechanism of its action requires further investigation. Betaine increases antioxidative defense and attenuates hepatotoxic effects of MIF, suggesting that betaine can be used for the prevention and treatment of liver damage. PMID: 33148149 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 4, 2020 Category: Chemistry Authors: Vukićević D, Rovčanin B, Gopčević K, Stanković S, Vučević D, Jorgačević B, Mladenović D, Vesković M, Samardžić J, Ješić R, Radosavljević T Tags: Curr Med Chem Source Type: research

New insights on Fak and Fak inhibitors.
CONCLUSION: All reported results evidenced that additional studies are necessary to design and synthesize new selective and more active compounds, although promising informations have been obtained from associations between Fak inhibitors and other different anti-cancer drugs. In addition, the other important roles evidenced, both at nuclear level and in non-cancerous cells, make this protein an increasingly important target in pharmaceutical chemistry. PMID: 33143618 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 3, 2020 Category: Chemistry Authors: Brullo C, Tasso B Tags: Curr Med Chem Source Type: research

Rediscovery of caffeine: an excellent drug for improving patient outcomes while fighting WARS.
Abstract The COVID-19 (here specifically called Worldwide Acute Respiratory Syndrome, WARS) pandemic is surging worldwide. Unfortunately, no specific drug meets the urgent need to fight this pandemic, leading to thousands of deaths. The theory of host-directed therapies (HDTs) is viewed as the ideal means to rephrase the treatment of infectious diseases. However, related drugs based on this theory have not been identified. Previously, we realized that caffeine is the ligand of type 2 taste receptors (TAS2Rs), which play a critical role in host defense. Here we gathered data on caffeine acting as an immunomodulator...
Source: Current Medicinal Chemistry - November 3, 2020 Category: Chemistry Authors: Liu L, Zhang C, Chen J, Li X Tags: Curr Med Chem Source Type: research

Conventional and non-conventional targets of natural products in the management of diabetes mellitus and associated complications.
CONCLUSION: The information amassed in this review is anticipated to provide useful scientific baseline information to support advanced research in natural antidiabetic drug development. PMID: 33138749 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 2, 2020 Category: Chemistry Authors: Mahomoodally MF, Lobine D, Picot-Allain MCN, Sadeer N, Jugreet S, Zengin G Tags: Curr Med Chem Source Type: research

Experimental approaches to identify selective picomolar inhibitors for carbonic anhydrase IX.
CONCLUSIONS: Novel CA IX inhibitors are promising derivatives for in vivo explorations. Furthermore, the simultaneous targeting of several proteins involved in proton flux upon tumor acidosis and the disruption of transport metabolons might improve cancer management. PMID: 33138744 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 1, 2020 Category: Chemistry Authors: Kazokaitė-Adomaitienė J, Becker HM, Smirnovienė J, Dubois LJ, Matulis D Tags: Curr Med Chem Source Type: research

Intracellular calcium homeostasis and kidney disease.
Abstract Kidney disease is a serious health problem that burdens our healthcare system. It is crucial to find the accurate pathogenesis of various types of kidney disease to provide guidance for precise therapies for patients suffered from these diseases. However,the exact molecular mechanisms underlying these diseases have not been fully understood. Disturbance of calcium homeostasis in renal cells plays a fundamental role in the development of various types of kidney disease,such as primary glomerular disease, diabetic nephropathy, acute kidney injury and polycystic kidney disease,through promoting cell prolifer...
Source: Current Medicinal Chemistry - November 1, 2020 Category: Chemistry Authors: Song N, Yang M, Zhang H, Yang SK Tags: Curr Med Chem Source Type: research

Synthesis and Biological Activities of Natural Functionalized Polyamines: An Overview.
el JM Abstract Recently, extensive researches have emphasized the fact that polyamines conjugates are becoming important in all the biological and medicinal fields. In this review we will focus our attention on natural polyamines and highlight recent progress in both fundamental mechanism studies and interest for the development and application for a therapeutic human use of polyamine derivatives. PMID: 33138746 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 1, 2020 Category: Chemistry Authors: Négrel S, Brunel JM Tags: Curr Med Chem Source Type: research

Indole and Indoline Scaffolds in Antimicrobials: Overview, Synthesis, and Recent Advances in Antimicrobial Research.
Abstract In our current society, a pandemic of antibiotic-resistant infectious diseases is an ever-growing threat. The need for new antibiotics and ways to combat antibiotic resistance is glaring. This review will focus on two different privileged scaffolds, the indole and the indoline, as useful nuclei for novel antibacterial compounds. The indole, a moiety found in numerous approved drugs for many disease states, has recently been studied for its usefulness as a scaffold for compounds that have activity against antibiotic-resistant bacteria, especially against methicillin-resistant Staphylococcus aureus (MRSA). ...
Source: Current Medicinal Chemistry - November 1, 2020 Category: Chemistry Authors: Nieto MJ, Lupton HK Tags: Curr Med Chem Source Type: research

Dysregulation of HOX as a Potential Therapeutic Target in Breast Cancer.
Abstract HOX genes belong to the highly conserved homeobox superfamily, responsible for the regulation of various cellular processes that control cell homeostasis, from embryogenesis to carcinogenesis. The abnormal expression of HOX genes is observed in various cancers, including breast cancer; they act as oncogenes or as suppressors of cancer, according to context. In this review, we analyze HOX gene expression patterns in breast cancer and examine their relationship, based on the three-dimensional genome structure of the HOX locus. The presence of non-coding RNAs, embedded within the HOX cluster, and the role of...
Source: Current Medicinal Chemistry - November 1, 2020 Category: Chemistry Authors: Lee JY, Kim MH Tags: Curr Med Chem Source Type: research

CypA: a Potential Target of Tumor Radiotherapy and/or Chemotherapy.
Abstract Cyclophilin A (CypA) is a ubiquitous and highly conserved protein. CypA, the intracellular target protein for the immunosuppressant cyclosporine A (CsA), plays important cellular roles through peptidyl-prolyl cis-trans isomerase (PPIase). Increasing evidence shows that CypA is up-regulated in a variety of human cancers. In addition to being involved in the occurrence and development of multiple tumors, overexpression of CypA also has been shown to be strongly associated with malignant transformation. Surgery, chemotherapy and radiotherapy are the three main treatments for cancer. Chemotherapy and radiothe...
Source: Current Medicinal Chemistry - October 29, 2020 Category: Chemistry Authors: Chu MY, Huang HC, Li EM, Xu LY Tags: Curr Med Chem Source Type: research

COVID-19 vaccine race: analysis of age-dependent immune responses against SARS-CoV-2 indicates that more than just one strategy may be needed.
Abstract In December 2019, a novel respiratory coronavirus named SARS-CoV-2 appeared in China, causing the disease termed COVID-19 that has caused millions of infections worldwide. In this article we have analyzed existing evidence on the immune response against SARS coronaviruses in order to understand the possible outcome of a vaccine for COVID-19. From our analysis it becomes clear that there is a big difference in the immune response against SARS in children, young adults and the elderly, both at the innate and adaptive levels. Taking this information into account, we have studied the strategies that are being...
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Campillo NE, Jimenez M, Canelles M Tags: Curr Med Chem Source Type: research

Recent Advances towards Drug Design Targeting the Protease of 2019 novel coronavirus (2019-nCoV).
CONCLUSION: In conclusion, this review summarizes recent progress in developing protease inhibitors for SARS-CoV-2. PMID: 33109027 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Bano S, Hameed A, Al-Rashida M, Iftikhar S, Iqbal J Tags: Curr Med Chem Source Type: research

Natural Products in Mitigation of SARS CoV Infections.
Abstract The severe acute respiratory syndrome (SARS) is a critical respiratory disease caused by coronaviruses (CoV). The available antiviral agents or host-specific anti-inflammatory therapies are the principal treatment modalities, with drugrepurposing as the most viable approach to timely tackle the CoV pandemic. Though these approaches are successful to some extent in reducing the mortality rate, however, it is too far to see a complete escape from the current CoV-2 pandemic. Plants are the primary source of diet, dietary supplements, botanical drugs, and natural products (NPs). It has been well accepted and ...
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Sharma V, Sharma A, Bharate SB Tags: Curr Med Chem Source Type: research

MALDI-ToF Mass spectra phenomic analysis for human disease diagnosis enabled by cutting-edge data processing pipelines and bioinformatic tools.
Abstract Currently, methodologies of human disease diagnosis are still far from capable of rapidly and accurately screening for multiple diseases, simultaneously in a large population, at affordable costs. MALDI-ToF mass spectrometry is an ultra-sensitive, ultra-fast and low-cost high-throughput technology which has a huge potential in clinical laboratory medicine to achieve this goal. Such clinical analysis is starting the first steps towards human phenotype detection and hence phenomic screening for multiple disease states. In this review, we will discuss the main advances achieved so far; putting forward target...
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Pais RJ, Iles RK, Zmuidinaite R Tags: Curr Med Chem Source Type: research

COVID-19: innovative antiviral drugs required for long-term prevention and control of coronavirus diseases.
lo CB Abstract The COVID-19 pandemic has had catastrophic Global effects on financial markets, jobs and peoples' lives. Future prevention/therapy of COVID-19 will rely heavily on vaccine development and attempts to repurpose drugs previously used for other microbial diseases. Little attention, however, has been paid to possible difficulties and delays in producing these drugs. Sometimes, unfortunately, these endeavours have been politicized and if these two approaches founder in any way or resistance subsequently occurs then the World will be left once again to the mercy of these devastating viral pandemics. This ...
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Ratcliffe NA, Castro HC, Paixão IC, Mello CB Tags: Curr Med Chem Source Type: research

Development of aldose reductase inhibitors for the treatment of inflammatory disorders and cancer: current drug design strategies and future directions.
Abstract Aldose Reductase (AR) is an enzyme that converts glucose to sorbitol during the polyol pathway of glucose metabolism. AR has been shown to be involved in the development of secondary diabetic complications due to its involvement in causing osmotic stress as well as oxidative stress. Various AR inhibitors have been tested for their use to treat secondary diabetic complications such as retinopathy, neuropathy, and nephropathy in clinical studies. Recent studies also suggest the potential role of AR in mediating various inflammatory complications. Therefore, the studies on the development and potential use o...
Source: Current Medicinal Chemistry - October 27, 2020 Category: Chemistry Authors: Sonowal H, Ramana KV Tags: Curr Med Chem Source Type: research

A comprehensive overview of colon cancer- a grim reaper of the 21st century.
Abstract A few decades ago, the incidence of colorectal cancer (CRC) was low and is now the fourth in the list of deadly cancers producing nearly a million deaths annually. A population that is aging along with risk factors such as smoking, obesity, sedentary lifestyle with little or no physical activity, and non-healthy food habits of developed countries can increase the risk of colorectal cancer. The balance in gut microbiota and the metabolites produced during bacterial fermentation within the host play a significant role in regulating intestinal diseases as well as colorectal cancer development. Recent progres...
Source: Current Medicinal Chemistry - October 26, 2020 Category: Chemistry Authors: Kumar R, Harilal S, Carradori S, Mathew B Tags: Curr Med Chem Source Type: research

Recent advances on the synthesis of the antidepressant Paroxetine.
omingues HS Abstract Paroxetine is a potent inhibitor of serotonin reuptake and is widely prescribed for the treatment of depression and other neurological disorders. The synthesis of paroxetine and the possibility to prepare derivatives with a specific substitution pattern that may allow their use as biological probes, is an attractive topic especially for medicinal chemists engaged in neurosciences research. Considering the extensive work that was developed in the last decade on the total synthesis of paroxetine, this review summarizes the most important contributions in this field, organized according to the re...
Source: Current Medicinal Chemistry - October 26, 2020 Category: Chemistry Authors: Santos J, Proença MF, Rodrigues AJ, Patrício P, Domingues HS Tags: Curr Med Chem Source Type: research

Evidence and the main adverse effects regarding drug therapies in the war against COVID-19.
CONCLUSION: At present, despite the enormous medical effort for publishing several trials or case reports, we have not yet discovered a definitive therapy against the COVID-19 infection. This brief review aims to prompt identification of risk factors and main adverse effects in a systematic view related to therapy with partial evidence proposed to date. PMID: 33106134 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 26, 2020 Category: Chemistry Authors: Mora-Ramírez M, Melgoza-Hernández P, Toledo-Ramírez SE, Aranguré JMM Tags: Curr Med Chem Source Type: research

Marine Natural Products as A Source of Drug Leads against Respiratory Viruses: Structural and Bioactive Diversity.
This report reviews marine natural products with activities against respiratory viruses, the emphasis of which was put on structures and antiviral activities of these natural products. This review has described 167 marine-derived secondary metabolites with activities against respiratory viruses published during 1981 to 2019. Altogether 102 references are cited in this review article. PMID: 33106135 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 26, 2020 Category: Chemistry Authors: Sun TT, Zhu HJ, Cao F Tags: Curr Med Chem Source Type: research

Peptide-Modified Nanoparticles for Tumor Targeting and Molecular Imaging.
Abstract Nanoparticles hold great promise in tumor targeting and molecular imaging because they can co-deliver therapeutic drugs and imaging agents to the tumor site with a single entity. Nanoparticles modified with ligands against moieties overexpressed on tumor tissues have gained increasing attention due to their active targeting mechanisms. Peptides are well suited for nanoparticle targeting modifications because they are small, easy to synthesize and typically non-immunogenic. Herein, we review the peptide-modified nanoparticles used for tumor targeting therapy and molecular imaging based on the classificatio...
Source: Current Medicinal Chemistry - October 22, 2020 Category: Chemistry Authors: Lu L, Zhang Q, Wang Z, Gao L, Shen J Tags: Curr Med Chem Source Type: research

Chalcones acting as inhibitors of cholinesterases, β-secretase and βamyloid aggregation and other targets for Alzheimer's disease: a critical review.
CONCLUSION: The most important characteristic of these molecules,is the given that many of the examples mentioned here act on more than one target, characterizing them as multi-target compounds. Regarding predicted properties, solubility stands out as the most problematic one, however these structures can incorporate functional groups that circumvent this problem of solubility without interfering in the biological activity. PMID: 33081667 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 20, 2020 Category: Chemistry Authors: Antoniolli G, Almeida WP, Frias CC, de Oliveira TB Tags: Curr Med Chem Source Type: research

Clinical therapy of patients contaminated with Polonium or Plutonium.
Abstract Although most of the harmful radionuclides are of anthropogenic origin and released from military or industrial processes, radioactive substances also occur naturally in the environment, e.g. uranium. Low standards of nuclear facilities can lead to contamination of employees with radionuclides due to inhalation of gases or dust, or contamination of skin or wounds. Various sources for radionuclide exposure may represent concerns for radioactive polonium or plutonium exposure, for instance terrorist actions on the infrastructure such as on drinking water basins. Early health effects after extensive radiatio...
Source: Current Medicinal Chemistry - October 20, 2020 Category: Chemistry Authors: Aaseth J, Nurchi VM, Andersen O Tags: Curr Med Chem Source Type: research

The Mitochondrion-targeted Antioxidants in Kidney Disease.
Abstract Mitochondria are potent source of cellular reactive oxygen species (ROS) and are vulnerable to oxidative damage. Mitochondria dysfunction could result in adenosine triphosphate (ATP) decrease and cell death. The kidney is an ATPconsuming organ, and the relationship between mitochondrial dysfunction and renal disease has been long noted. Mitochondrial targeting is a novel strategy for kidney diseases. At present, there are several ways to target mitochondria such as the addition of a triphenylphosphonium cation, mitochondria-targeted peptides, and nanocarrier. There are also a variety of choices for the pa...
Source: Current Medicinal Chemistry - October 20, 2020 Category: Chemistry Authors: Li X, Ma L, Fu P Tags: Curr Med Chem Source Type: research

Electrochemical and Electrochemiluminescence Dendrimer-based Nanostructured Immunosensors for Tumor Marker Detection: A review.
Abstract The usage of dendrimers or cascade molecules in the biomedical area can be recently attracted much attention worldwide. Also, dendrimers are interesting in the field of clinical and pre-clinical applications due to their unique characteristics. Cancer is one of the most widespread challenges and important diseases, which has the highest mortality rate. In this review, the recent advances and developments (from 2009 up to 2019) in the field of electrochemical and electroluminescence immunosensors for detection of the cancer markers are presented. Also, this review covers the basic fabrication principles an...
Source: Current Medicinal Chemistry - October 19, 2020 Category: Chemistry Authors: Filik H, Avan AA Tags: Curr Med Chem Source Type: research

Irinotecan or Oxaliplatin: Which is the First Move for the Mate?
CONCLUSIONS: OXA and IRI are indispensable drugs for mCRC treatment and their selection must be as careful as that of targeted agents. We suggest to take into consideration the interaction between known genomic alterations and OXA and IRI activity to personalize chemotherapy in mCRC patients. PMID: 33069191 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 16, 2020 Category: Chemistry Authors: Morelli C, Formica V, Riondino S, Russo A, Ferroni P, Guadagni F, Roselli M Tags: Curr Med Chem Source Type: research