Search Results - "King, Bryan W"
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RIP3 Induces Apoptosis Independent of Pronecrotic Kinase Activity
Published in Molecular cell (20-11-2014)“…Receptor-interacting protein kinase 3 (RIP3 or RIPK3) has emerged as a central player in necroptosis and a potential target to control inflammatory disease…”
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Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
Published in Journal of medicinal chemistry (23-02-2017)“…RIP1 regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated…”
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The Identification and Pharmacological Characterization of 6‑(tert-Butylsulfonyl)‑N‑(5-fluoro‑1H‑indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase
Published in Journal of medicinal chemistry (26-05-2016)“…RIP2 kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1…”
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Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening
Published in Nature communications (17-07-2017)“…The identification and prioritization of chemically tractable therapeutic targets is a significant challenge in the discovery of new medicines. We have…”
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Asymmetric Aldol Additions: Use of Titanium Tetrachloride and (−)-Sparteine for the Soft Enolization of N-Acyl Oxazolidinones, Oxazolidinethiones, and Thiazolidinethiones
Published in Journal of organic chemistry (09-02-2001)“…Asymmetric aldol additions using chlorotitanium enolates of N-acyloxazolidinone, oxazolidinethione, and thiazolidinethione propionates proceed with high…”
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DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors
Published in Journal of medicinal chemistry (10-03-2016)“…The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to its emergence…”
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Structural characterization of dicyanopyridine containing DNMT1-selective, non-nucleoside inhibitors
Published in Structure (London) (02-06-2022)“…DNMT1 maintains the parental DNA methylation pattern on newly replicated hemimethylated DNA. The failure of this maintenance process causes aberrant DNA…”
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Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2‑((4-(Benzo[d]thiazol-5-ylamino)-6‑(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases
Published in Journal of medicinal chemistry (25-07-2019)“…RIP2 kinase has been identified as a key signal transduction partner in the NOD2 pathway contributing to a variety of human pathologies, including…”
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Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement
Published in Bioorganic & medicinal chemistry (15-02-2024)“…[Display omitted] •P1 analogues with aldehyde warhead prepared and tested against 3CLpro in SARS-CoV-2.•Discovery of 2-THF as P1 residue with potent inhibition…”
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DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry
Published in ACS medicinal chemistry letters (08-07-2021)“…DNA-encoded library (DEL) technology is a powerful platform for hit identification in academia and the pharmaceutical industry. When conducting off-DNA…”
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Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity
Published in Bioorganic & medicinal chemistry (01-11-2015)“…[Display omitted] Receptor interacting protein 2 (RIP2) is an intracellular kinase and key signaling partner for the pattern recognition receptors NOD1 and…”
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Regioselectivity in the Palladium-Catalyzed Addition of Carbon Nucleophiles to Carbocyclic Derivatives
Published in Journal of organic chemistry (25-01-2002)“…The regioselectivity of Pd-catalyzed malonate additions and arylations to cycloalkenyl esters can be predicted by completing a stereochemical analysis of the…”
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Synthesis of the C1−C13 Fragment of Leucascandrolide A
Published in Organic letters (09-03-2000)“…The synthesis of the C1−C13 fragment 3 of leucascandrolide A has been completed utilizing a stereoselective and regioselective reductive cleavage of a highly…”
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Correction: Author Correction: Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening
Published in Nature communications (13-07-2018)“…Nature Communications 8: Article number: 16081 (2017); Published: 17 July 2017, Updated: 13 July 2018 The original version of this Article omitted the…”
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An Efficient, General Asymmetric Synthesis of Carbocyclic Nucleosides: Application of an Asymmetric Aldol/Ring-Closing Metathesis Strategy
Published in Journal of organic chemistry (15-12-2000)“…A general and efficient synthesis of carbocyclic and hexenopyranosyl nucleosides has been developed. The strategy combines three key transformations: an…”
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Asymmetric Total Synthesis of Callystatin A: Asymmetric Aldol Additions with Titanium Enolates of Acyloxazolidinethiones
Published in Journal of the American Chemical Society (09-09-1998)Get full text
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Understanding the Origins of Time-Dependent Inhibition by Polypeptide Deformylase Inhibitors
Published in Biochemistry (Easton) (09-08-2011)“…The continual bacterial adaptation to antibiotics creates an ongoing medical need for the development of novel therapeutics. Polypeptide deformylase (PDF) is a…”
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Author Correction: Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening
Published in Nature communications (13-07-2018)“…This corrects the article DOI: 10.1038/ncomms16081…”
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