Search Results - "Nag, Partha"
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1
A substrate-driven allosteric switch that enhances PDI catalytic activity
Published in Nature communications (30-08-2016)“…Protein disulfide isomerase (PDI) is an oxidoreductase essential for folding proteins in the endoplasmic reticulum. The domain structure of PDI is a – b – b′ –…”
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A small-molecule allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase
Published in Nature chemical biology (01-09-2017)“…High-throughput screening identifies an inhibitor of the interaction between α- and β-subunits of the Mycobacterium tuberculosis (Mtb) tryptophan synthase,…”
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3
Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes
Published in Cell (23-03-2017)“…Type 2 diabetes (T2D) is a worldwide epidemic with a medical need for additional targeted therapies. Suppression of hepatic glucose production (HGP)…”
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4
Allosteric inhibitors of Mycobacterium tuberculosis tryptophan synthase
Published in Protein science (01-03-2020)“…Global dispersion of multidrug resistant bacteria is very common and evolution of antibiotic‐resistance is occurring at an alarming rate, presenting a…”
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5
Cell-specific transcriptional control of mitochondrial metabolism by TIF1γ drives erythropoiesis
Published in Science (American Association for the Advancement of Science) (14-05-2021)“…Transcription and metabolism both influence cell function, but dedicated transcriptional control of metabolic pathways that regulate cell fate has rarely been…”
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6
Stereocontrolled Synthesis of the Tricyclic ABC Ring System of Daphnicyclidin A
Published in Organic letters (04-04-2014)“…An enantiocontrolled synthesis pathway has been developed to provide formation of tricyclic amine 7, representing the ABC ring system of the complex alkaloid…”
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7
Identification of Novel Inhibitors of Nonreplicating Mycobacterium tuberculosis Using a Carbon Starvation Model
Published in ACS chemical biology (18-10-2013)“…During Mycobacterium tuberculosis infection, a population of bacteria is thought to exist in a nonreplicating state, refractory to antibiotics, which may…”
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8
Small-molecule probe for IBD risk variant GPR65 I231L alters cytokine signaling networks through positive allosteric modulation
Published in Science advances (19-07-2024)“…The proton-sensing heterotrimeric guanine nucleotide-binding protein-coupled receptor GPR65 is expressed in immune cells and regulates tissue homeostasis in…”
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9
Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects
Published in ACS chemical biology (15-07-2016)“…The mood stabilizer lithium, the first-line treatment for bipolar disorder, is hypothesized to exert its effects through direct inhibition of glycogen synthase…”
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Conservation of the structure and function of bacterial tryptophan synthases
Published in IUCrJ (01-07-2019)“…Tryptophan biosynthesis is one of the most characterized processes in bacteria, in which the enzymes from and serve as model systems. Tryptophan synthase…”
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Discovery of bisamide-heterocycles as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake
Published in Bioorganic & medicinal chemistry letters (15-06-2015)“…[Display omitted] A new series of potent inhibitors of cellular lipid uptake from HDL particles mediated by scavenger receptor, class B, type I (SR-BI) was…”
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12
Identification of a selective small molecule inhibitor of breast cancer stem cells
Published in Bioorganic & medicinal chemistry letters (15-05-2012)“…A high-throughput screen (HTS) with the National Institute of Health–Molecular Libraries Small Molecule Repository (NIH–MLSMR) compound collection identified a…”
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13
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells
Published in Bioorganic & medicinal chemistry letters (15-03-2013)“…A high-throughput screen (HTS) was conducted against stably propagated cancer stem cell (CSC)-enriched populations using a library of 300,718 compounds from…”
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14
Phenotypic high-throughput screening elucidates target pathway in breast cancer stem cell-like cells
Published in Journal of biomolecular screening (01-10-2012)“…Cancer stem cells (CSCs) are resistant to standard cancer treatments and are likely responsible for cancer recurrence, but few therapies target this…”
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15
Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies
Published in ACS medicinal chemistry letters (11-10-2012)“…Macrocyclic Hedgehog (Hh) pathway inhibitors have been discovered with improved potency and maximal inhibition relative to the previously reported macrocycle…”
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16
Indolinyl-Thiazole Based Inhibitors of Scavenger Receptor-BI (SR-BI)-Mediated Lipid Transport
Published in ACS medicinal chemistry letters (09-04-2015)“…A potent class of indolinyl-thiazole based inhibitors of cellular lipid uptake mediated by scavenger receptor, class B, type I (SR-BI) was identified via a…”
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17
ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
Published in Beilstein journal of organic chemistry (26-07-2013)“…The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to…”
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18
Studies of the Generation and Pericyclic Behavior of Cyclic Pentadienyl Carbanions. Alkylation Reactions as an Efficient Route to Functionalized cis-Bicyclo[3.3.0]octenes
Published in Journal of the American Chemical Society (20-09-2006)“…Carbolithiation has been studied with alkyllithium reagents in a series of six- through nine-membered 3-methylene-1,4-cycloalkadienes, efficiently producing…”
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19
Target-Based Identification of Whole-Cell Active Inhibitors of Biotin Biosynthesis in Mycobacterium tuberculosis
Published in Chemistry & biology (22-01-2015)“…Biotin biosynthesis is essential for survival and persistence of Mycobacterium tuberculosis (Mtb) in vivo. The aminotransferase BioA, which catalyzes the…”
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Samarium Barbier Reactions of α-Iodomethyloxazoles and Thiazoles with Aliphatic Aldehydes
Published in Organic letters (15-09-2005)“…The reductive coupling of substituted α-iodomethyloxazoles and thiazoles with aliphatic aldehydes under Barbier conditions provides an effective method for the…”
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