Search Results - "Noe, Mark C"
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Delineating the role of cooperativity in the design of potent PROTACs for BTK
Published in Proceedings of the National Academy of Sciences - PNAS (31-07-2018)“…Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that simultaneously bind to a target protein and an E3 ligase, thereby leading…”
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Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors
Published in Journal of medicinal chemistry (11-12-2014)“…Interest in drugs that covalently modify their target is driven by the desire for enhanced efficacy that can result from the silencing of enzymatic activity…”
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Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections
Published in Journal of medicinal chemistry (26-01-2012)“…In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel…”
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Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes
Published in Nature chemical biology (01-02-2021)Get full text
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Inducing protein-protein interactions with molecular glues
Published in Bioorganic & medicinal chemistry letters (15-08-2018)“…[Display omitted] •Molecular glues promote the unnatural association of proteins to produce a therapeutic effect.•Molecular glues alter the surface of proteins…”
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An Asymmetric Synthesis of (2S,5S)-5-Substituted Azepane-2-Carboxylate Derivatives
Published in Journal of organic chemistry (18-03-2011)“…To facilitate a drug discovery project, we needed to develop a robust asymmetric synthesis of (2S,5S)-5-substituted-azepane-2-carboxylate derivatives. Two key…”
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Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes
Published in Nature chemical biology (01-02-2021)“…Heterobifunctional chimeric degraders are a class of ligands that recruit target proteins to E3 ubiquitin ligases to drive compound-dependent protein…”
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Linezolid, the first oxazolidinone antibacterial agent
Published in Annals of the New York Academy of Sciences (01-03-2011)“…Linezolid (Zyvox™) is the first member of an entirely new class of antibiotics to reach the market in over 35 years; it was approved for use in 2000. A member…”
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A Critical Analysis of the Mechanistic Basis of Enantioselectivity in the Bis-Cinchona Alkaloid Catalyzed Dihydroxylation of Olefins
Published in Journal of the American Chemical Society (13-11-1996)“…This paper presents a critical analysis of two transition state models for the bis-cinchona alkaloid catalyzed enantioselective dihydroxylation of olefins…”
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Ultra-High-Throughput Acoustic Droplet Ejection-Open Port Interface-Mass Spectrometry for Parallel Medicinal Chemistry
Published in ACS medicinal chemistry letters (11-06-2020)“…High-throughput experimentation (HTE) has emerged as an important tool in drug discovery, providing a platform for preparing large compound libraries and…”
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The application of a mechanistic model leads to the extension of the Sharpless asymmetric dihydroxylation to allylic 4-methoxybenzoates and conformationally related amine and homoallylic alcohol derivatives
Published in Journal of the American Chemical Society (01-11-1995)Get full text
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Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections
Published in Journal of medicinal chemistry (23-02-2012)“…The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this…”
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Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity
Published in Journal of medicinal chemistry (11-07-2013)“…Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity…”
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Discovery of Dap‑3 Polymyxin Analogues for the Treatment of Multidrug-Resistant Gram-Negative Nosocomial Infections
Published in Journal of medicinal chemistry (27-06-2013)“…We report novel polymyxin analogues with improved antibacterial in vitro potency against polymyxin resistant recent clinical isolates of Acinetobacter…”
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X-ray Crystal and NMR Structure of a Highly Reactive Bidentate 1,2-Diamine−OsO4 Complex, Formally a 20-Electron Outer Valence Shell Species. Mechanistic Implications for the 1,2-Diamine-Accelerated Dihydroxylation of Olefins by OsO4
Published in Journal of the American Chemical Society (21-08-1996)Get full text
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