Search Results - "Chikhale, Rupesh V"
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Unlocking the potential of PROTACs: A comprehensive review of protein degradation strategies in disease therapy
Published in Bioorganic chemistry (01-10-2023)“…[Display omitted] •PROTACs (PROteolysis TArgeting Chimeras) are a technology used for protein degradation through the use of bifunctional small molecules.•They…”
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Identification of sugar-containing natural products that interact with i-motif DNA
Published in Bioorganic & medicinal chemistry letters (01-10-2022)“…[Display omitted] There are thousands of compounds shown to interact with G-quadruplex DNA, yet very few which target i-motif (iM) DNA. Previous work showed…”
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A Review on Five and Six-Membered Heterocyclic Compounds Targeting the Penicillin-Binding Protein 2 (PBP2A) of Methicillin-Resistant Staphylococcus aureus (MRSA)
Published in Molecules (Basel, Switzerland) (10-10-2023)“…Staphylococcus aureus is a common human pathogen. Methicillin-resistant Staphylococcus aureus (MRSA) infections pose significant and challenging therapeutic…”
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Structural insights into i-motif DNA structures in sequences from the insulin-linked polymorphic region
Published in Nature communications (20-08-2024)“…The insulin-linked polymorphic region is a variable number of tandem repeats region of DNA in the promoter of the insulin gene that regulates transcription of…”
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Rutin from Begonia roxburghii modulates iNOS and Sep A activity in treatment of Shigella flexneri induced diarrhoea in rats: An in vitro, in vivo and computational analysis
Published in Microbial pathogenesis (01-11-2023)“…In developing countries, diarrhoea is a major issue of concern, where consistent use of antibiotics has resulted in several side effects along with development…”
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Current biomarkers and treatment strategies in Alzheimer disease: An overview and future perspectives
Published in IBRO neuroscience reports (01-06-2024)“…Alzheimer's disease (AD), a progressive degenerative disorder first identified by Alois Alzheimer in 1907, poses a significant public health challenge. Despite…”
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Identification of Mycobacterium tuberculosis transcriptional repressor EthR inhibitors: Shape-based search and machine learning studies
Published in Heliyon (15-03-2024)“…Tuberculosis has been a challenge to the world since prehistoric times, and with the advent of drug-resistant strains, it has become more challenging to treat…”
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Covalent drug – An emerging framework for targeted drug development
Published in Results in Chemistry (01-06-2024)“…[Display omitted] •Historical overview traces covalent drugs since the 20th century, spotlighting safety concerns that hindered their…”
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Determination and Pharmacokinetic Study of Pirfenidone in Rat Serum by High-Performance Thin-Layer Chromatography
Published in Journal of chromatographic science (01-08-2016)“…A rapid, sensitive and selective high-performance thin-layer chromatography (HPTLC) method was developed and validated for the determination and…”
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Generation of Phenothiazine with Potent Anti-TLK1 Activity for Prostate Cancer Therapy
Published in iScience (25-09-2020)“…Through in vitro kinase assays and docking studies, we report the synthesis and biological evaluation of a phenothiazine analog J54 with potent TLK1 inhibitory…”
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Design, synthesis and evaluation of novel enzalutamide analogues as potential anticancer agents
Published in Heliyon (01-03-2021)“…The androgen receptor inhibitor, Enzalutamide, proved effective against castration resistance prostate cancer, has demonstrated clinical benefits and increased…”
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Vitamin-anticancer drug conjugates: A new era for cancer therapy
Published in Istanbul journal of pharmacy (01-12-2020)“…Background: Following cardiovascular diseases, cancer is the world's second leading cause of death. Chemotherapy is the conventional gold technique for…”
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Computational and network pharmacology studies of Phyllanthus emblica to tackle SARS-CoV-2
Published in Phytomedicine Plus : International journal of phytotherapy and phytopharmacology (01-08-2021)“…•Emblica officinalis is used as rejuvenator in Traditional Systems of Medicine.•Docking, MD and network pharmacology demonstrated antiviral & adjuvant…”
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Overview of the Development of DprE1 Inhibitors for Combating the Menace of Tuberculosis
Published in Journal of medicinal chemistry (11-10-2018)“…Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), a vital enzyme for cell wall synthesis, plays a crucial role in the formation of lipoarabinomannan and…”
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Mycobacterial Membrane Protein Large 3 (MmpL3) Inhibitors: A Promising Approach to Combat Tuberculosis
Published in ChemMedChem (15-10-2021)“…Tuberculosis is a prominent aliment throughout the world and a leading cause of mortality among infectious diseases. Drug development for multi‐drug resistance…”
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Mycobacterium enoyl acyl carrier protein reductase (InhA): A key target for antitubercular drug discovery
Published in Bioorganic chemistry (01-10-2021)“…[Display omitted] •InhA remains a novel target for development of antitubercular drugs.•High throughput screening and encoded library technology helped…”
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Evolution and Impact of Nucleic Acid Amplification Test (NAAT) for Diagnosis of Coronavirus Disease
Published in Analytical chemistry (Washington) (21-05-2024)Get full text
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Identification of potential anti-TMPRSS2 natural products through homology modelling, virtual screening and molecular dynamics simulation studies
Published in Journal of biomolecular structure & dynamics (22-11-2021)“…Recent outbreak of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has led to a pandemic of COVID-19. The absence of a therapeutic drug and…”
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Sars-cov-2 host entry and replication inhibitors from Indian ginseng: an in-silico approach
Published in Journal of biomolecular structure & dynamics (13-08-2021)“…COVID-19 has ravaged the world and is the greatest of pandemics in modern human history, in the absence of treatment or vaccine, the mortality and morbidity…”
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DNA G‑Quadruplex and i‑Motif Structure Formation Is Interdependent in Human Cells
Published in Journal of the American Chemical Society (09-12-2020)“…Guanine- and cytosine-rich nucleic acid sequences have the potential to form secondary structures such as G-quadruplexes and i-motifs, respectively. We show…”
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