Structure-based virtual screening of chemical libraries as potential MELK inhibitors and their therapeutic evaluation against breast cancer
Chem Biol Interact. 2023 Mar 7:110443. doi: 10.1016/j.cbi.2023.110443. Online ahead of print.ABSTRACTNew targeted therapy for triple negative breast cancer (TNBC) is an urgent need, as advanced disease responds poorly to conventional chemotherapy. Genomic and proteomic studies are currently investigating new genes and proteins as promising therapeutic targets. One of such therapeutic targets is a cell cycle regulatory kinase; Maternal Embryonic Leucine Zipper Kinase (MELK), overexpressed in TNBC and correlated with cancer development. We performed molecular docking for virtual screening of chemical libraries (phytochemical...
Source: Chemico-Biological Interactions - March 9, 2023 Category: Molecular Biology Authors: Amiya Das Anita Prajapati Amarnath Karna Hitesh Kumar Sharma Sheetal Uppal Viney Lather Deepti Pandita Pallavi Agarwal Source Type: research
Structure-based virtual screening of chemical libraries as potential MELK inhibitors and their therapeutic evaluation against breast cancer
Chem Biol Interact. 2023 Mar 7:110443. doi: 10.1016/j.cbi.2023.110443. Online ahead of print.ABSTRACTNew targeted therapy for triple negative breast cancer (TNBC) is an urgent need, as advanced disease responds poorly to conventional chemotherapy. Genomic and proteomic studies are currently investigating new genes and proteins as promising therapeutic targets. One of such therapeutic targets is a cell cycle regulatory kinase; Maternal Embryonic Leucine Zipper Kinase (MELK), overexpressed in TNBC and correlated with cancer development. We performed molecular docking for virtual screening of chemical libraries (phytochemical...
Source: Chemico-Biological Interactions - March 9, 2023 Category: Molecular Biology Authors: Amiya Das Anita Prajapati Amarnath Karna Hitesh Kumar Sharma Sheetal Uppal Viney Lather Deepti Pandita Pallavi Agarwal Source Type: research
Molecules, Vol. 28, Pages 2352: Development of a Rapid LC-MS/MS Method for Simultaneous Quantification of Donepezil and Tadalafil in Rat Plasma: Its Application in a Pharmacokinetic Interaction Study after Oral Administration in Rats
This study aimed to establish a simple and sensitive analytical method to simultaneously quantify donepezil (DPZ) and tadalafil (TAD) in rat plasma using lansoprazole (LPZ) as an internal standard (IS) by using liquid chromatography tandem mass spectrometry. The fragmentation pattern of DPZ, TAD, and IS was elucidated using multiple reaction monitoring in electrospray ionization positive ion mode for the quantification of precursor to production at m/z 380.1 → 91.2 for DPZ, m/z 390.2 → 268.1 for TAD, and m/z 370.3 → 252.0 for LPZ. The extracted DPZ and TAD from plasma using acetonitri...
Source: Molecules - March 3, 2023 Category: Chemistry Authors: Jiyoung Yoon Doowon Choi Wang-Seob Shim Sanghee Choi Yeo Jin Choi Soo-Heui Paik Kyung-Tae Lee Tags: Article Source Type: research
Why the Vonoprazan Helicobacter pylori Therapies in the US-European Trial Produced Unacceptable Cure Rates
ConclusionThe most likely reason for failure was failure to achieve high intragastric concentrations of antibiotics or to achieve an intragastric pH conducive for amoxicillin to be active. Importantly, vonoprazan triple therapy resulted in > 10 tons of unneeded clarithromycin/million courses of vonoprazan triple therapy. Antibiotic misuse combined with low cure rates suggest that vonoprazan–clarithromycin triple therapies should not be prescribed forH. pylori infection. Dual vonoprazan –amoxicillin therapy has proven effective elsewhere and after optimization may eventually prove useful in the U.S./Europe. (So...
Source: Digestive Diseases and Sciences - March 1, 2023 Category: Gastroenterology Source Type: research
Lansoprazole attenuates cyclophosphamide-induced cardiopulmonary injury by modulating redox-sensitive pathways and inflammation
Mol Cell Biochem. 2023 Jan 31. doi: 10.1007/s11010-023-04662-x. Online ahead of print.ABSTRACTCyclophosphamide (CPA) is a classical chemotherapeutic drug widely used as an anticancer and immunosuppressive agent. However, it is frequently associated with significant toxicities to the normal cells of different organs, including the lung and heart. Lansoprazole (LPZ), a proton pump inhibitor (PPI), possesses antioxidant and anti-inflammatory properties. The current study investigated how LPZ protects against CPA-induced cardiac and pulmonary damage, focusing on PPARγ, Nrf2, HO-1, cytoglobin, PI3K/AKT, and NF-κB signaling. A...
Source: Molecular and Cellular Biochemistry - January 30, 2023 Category: Biochemistry Authors: Emad H M Hassanein Esam O Kamel Wail M Gad-Elrab Mohammed A Ahmed Zuhair M Mohammedsaleh Fares E M Ali Source Type: research
Lansoprazole attenuates cyclophosphamide-induced cardiopulmonary injury by modulating redox-sensitive pathways and inflammation
Mol Cell Biochem. 2023 Jan 31. doi: 10.1007/s11010-023-04662-x. Online ahead of print.ABSTRACTCyclophosphamide (CPA) is a classical chemotherapeutic drug widely used as an anticancer and immunosuppressive agent. However, it is frequently associated with significant toxicities to the normal cells of different organs, including the lung and heart. Lansoprazole (LPZ), a proton pump inhibitor (PPI), possesses antioxidant and anti-inflammatory properties. The current study investigated how LPZ protects against CPA-induced cardiac and pulmonary damage, focusing on PPARγ, Nrf2, HO-1, cytoglobin, PI3K/AKT, and NF-κB signaling. A...
Source: Molecular and Cellular Biochemistry - January 30, 2023 Category: Biochemistry Authors: Emad H M Hassanein Esam O Kamel Wail M Gad-Elrab Mohammed A Ahmed Zuhair M Mohammedsaleh Fares E M Ali Source Type: research
Pembrolizumab, radiotherapy, and an immunomodulatory five-drug cocktail in pretreated patients with persistent, recurrent, or metastatic cervical or endometrial carcinoma: Results of the phase II PRIMMO study
In conclusion, PRIMMO did not meet its primary objective in both cohorts; pembrolizumab, radiotherapy, and an IDC had modest but durable antitumor activity with acceptable but not negligible toxicity.Trial registration ClinicalTrials.gov (identifier NCT03192059) and EudraCT Registry (number 2016-001569-97). (Source: Cancer Immunology, Immunotherapy)
Source: Cancer Immunology, Immunotherapy - January 23, 2023 Category: Cancer & Oncology Source Type: research
The Association of Proton Pump Inhibitors and QT Interval Prolongation in Critically Ill Patients
ConclusionIn ICU patients, the association between PPI prescription and increased risk of QT interval prolongation was independent of known QT-prolonging factors; pantoprazole and lansoprazole had a higher risk compared with omeprazole. The combination of PPIs and other QT-prolonging drugs should be avoided. (Source: Cardiovascular Drugs and Therapy)
Source: Cardiovascular Drugs and Therapy - January 10, 2023 Category: Cardiology Source Type: research
The Case | Hyperammonemia in a non-cirrhotic hemodialysis patient
A 78-year-old woman presented with recurrent encephalopathy after hemodialysis initiation. Her medical history included end-stage renal disease, congestive heart failure, and cerebral infarction. Her medication included aspirin, losartan, carvedilol, pravastatin, and lansoprazole. Maintenance hemodialysis was initiated because of refractory volume overload. Two days after dialysis initiation, she was noted to be comatose with hyperammonemia (205 μg/dl). Branched-chain amino acid infusion was administered, resulting in improvement of her mental status. (Source: Kidney International)
Source: Kidney International - January 1, 2023 Category: Urology & Nephrology Authors: Tomoki Taniguchi, Mayumi Tomita, Noriyuki Iehara Tags: Make Your Diagnosis Source Type: research
Changes in bone turnover markers in adolescents with gastroesophageal reflux disease treated with lansoprazole
CONCLUSIONS: The results of this study reveal that eight weeks of treatment with 30 mg lansoprazole daily increased the bone turnover markers of CTX, NTX, DPD and osteocalcin in adolescents aged 16-18.PMID:36566365 | DOI:10.51821/85.4.10906 (Source: Acta Gastro-Enterologica Belgica)
Source: Acta Gastro-Enterologica Belgica - December 25, 2022 Category: Gastroenterology Authors: A Islek N Erol Kizilelma H Keskin N Ozturk Source Type: research
