Journal of Medicinal Chemistry

Emerging New Targets for the Treatment of Resistant Fungal Infections (Tue, 16 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01413
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Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate (Tue, 16 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01466
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Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection (Tue, 16 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01249
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Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma (Thu, 11 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01051
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Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides (Thu, 11 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01678
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Correction to Synthesis of Potent and Selective Inhibitors of Aldo-Keto Reductase 1B10 and Their Efficacy against Proliferation, Metastasis, and Cisplatin Resistance of Lung Cancer Cells (Thu, 11 Jan 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01911
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Neutral Porphyrin Derivative Exerts Anticancer Activity by Targeting Cellular Topoisomerase I (Top1) and Promotes Apoptotic Cell Death without Stabilizing Top1-DNA Cleavage Complexes (Thu, 11 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01297
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Systematic Tuning of Fluoro-galectin-3 Interactions Provides Thiodigalactoside Derivatives with Single-Digit nM Affinity and High Selectivity (Thu, 11 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01626
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Fluorescently Labeled Morphine Derivatives for Bioimaging Studies (Wed, 10 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01811
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In Silico Fragment-Based Design Identifies Subfamily B1 Metallo-β-lactamase Inhibitors (Wed, 10 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01728
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Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent (Wed, 10 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01288
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Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy? (Tue, 09 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00901
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Effect of Structural Modifications to Glyoxal-bis(thiosemicarbazonato)copper(II) Complexes on Cellular Copper Uptake, Copper-Mediated ATP7A Trafficking, and P-Glycoprotein Mediated Efflux (Mon, 08 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01158
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Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure (Mon, 08 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01474
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Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01654
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Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01547
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Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766) (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01406
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“Seriously Sweet”: Acesulfame K Exhibits Selective Inhibition Using Alternative Binding Modes in Carbonic Anhydrase Isoforms (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01470
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High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01136
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Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01411
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Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3) (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01674
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Structure-Guided Synthesis and Mechanistic Studies Reveal Sweetspots on Naphthyl Salicyl Hydrazone Scaffold as Non-Nucleosidic Competitive, Reversible Inhibitors of Human Ribonucleotide Reductase (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00530
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Insights into the Impact of a Membrane-Anchoring Moiety on the Biological Activities of Bivalent Compounds As Potential Neuroprotectants for Alzheimer’s Disease (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01284
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Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01607
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Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis (Fri, 05 Jan 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01339
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Targeting Transcriptional Enhanced Associate Domains (TEADs) (Thu, 28 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00879
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Inhibit or Evade Multidrug Resistance P-Glycoprotein in Cancer Treatment (Thu, 28 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01457
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The Rise and Fall of a Scaffold: A Trend Analysis of Scaffolds in the Medicinal Chemistry Literature (Wed, 27 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00954
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Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497) (Wed, 27 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01375
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Discovery of Peptidomimetic Antibody–Drug Conjugate Linkers with Enhanced Protease Specificity (Thu, 21 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01430
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Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy (Wed, 20 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01019
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Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones? (Tue, 19 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01272
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Small Molecule Mitochondrial Uncouplers and Their Therapeutic Potential (Fri, 08 Dec 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01182
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Importance of Rigidity in Designing Small Molecule Drugs To Tackle Protein–Protein Interactions (PPIs) through Stabilization of Desired Conformers (Tue, 28 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01120
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Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer (Mon, 27 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01310
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Inducing Protein Degradation as a Therapeutic Strategy (Wed, 22 Nov 2017)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01333
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Relevance of Half-Life in Drug Design (Fri, 17 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00969
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Pharmacophore Hybridization To Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity (Thu, 09 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01388
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Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs (Thu, 09 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00772
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Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds (Wed, 01 Nov 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00718
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Fragment-to-Lead Medicinal Chemistry Publications in 2016 (Tue, 31 Oct 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01298
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Modulators of 14-3-3 Protein–Protein Interactions (Thu, 19 Oct 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00574
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Chemical Approaches to Modulating Complement-Mediated Diseases (Wed, 18 Oct 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00882
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Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA) (Thu, 28 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00935
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Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection (Wed, 27 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00717
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Modulation of Glycine-Mediated Spinal Neurotransmission for the Treatment of Chronic Pain (Fri, 22 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00956
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Carbon Monoxide and Its Controlled Release: Therapeutic Application, Detection, and Development of Carbon Monoxide Releasing Molecules (CORMs) (Wed, 20 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01153
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Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298) (Mon, 18 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00675
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Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry (Fri, 08 Sep 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00315
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Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges (Fri, 25 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01827
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The ProTide Prodrug Technology: From the Concept to the Clinic (Thu, 24 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00734
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Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD) (Tue, 22 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00115
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Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies (Fri, 18 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00498
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Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts (Fri, 18 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00762
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Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors (Fri, 11 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00404
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The Current State of Peptide Drug Discovery: Back to the Future? (Fri, 11 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00318
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BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer’s Disease (Tue, 08 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00393
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Free Energy Methods in Drug Design: Prospects of “Alchemical Perturbation” in Medicinal Chemistry (Fri, 04 Aug 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00681
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Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1 (Mon, 10 Jul 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00635
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Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00168
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Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds (Fri, 23 Jun 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01912
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Interrogating the Roles of Post-Translational Modifications of Non-Histone Proteins (Wed, 24 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01817
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Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins (Wed, 10 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00413
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Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ERα and ERβ Activity (Mon, 01 May 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01917
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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01921
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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01872
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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01781
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Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1 (Thu, 13 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01911
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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression (Fri, 24 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01816
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Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site (Tue, 28 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01346
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