Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Opportunities and challenges in phenotypic drug discovery: an industry perspective

JG Moffat, F Vincent, JA Lee, J Eder… - Nature reviews Drug …, 2017 - nature.com
Phenotypic drug discovery (PDD) approaches do not rely on knowledge of the identity of a
specific drug target or a hypothesis about its role in disease, in contrast to the target-based …

Enterococci enhance Clostridioides difficile pathogenesis

AB Smith, ML Jenior, O Keenan, JL Hart, J Specker… - Nature, 2022 - nature.com
Enteric pathogens are exposed to a dynamic polymicrobial environment in the
gastrointestinal tract. This microbial community has been shown to be important during …

Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries

M Kuljanin, DC Mitchell, DK Schweppe… - Nature …, 2021 - nature.com
Current methods used for measuring amino acid side-chain reactivity lack the throughput
needed to screen large chemical libraries for interactions across the proteome. Here we …

Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1

Y Tao, D Remillard, EV Vinogradova… - Journal of the …, 2022 - ACS Publications
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

Recent developments in PROTAC‐mediated protein degradation: from bench to clinic

Z Hu, CM Crews - ChemBioChem, 2022 - Wiley Online Library
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …

Chemistry for covalent modification of endogenous/native proteins: from test tubes to complex biological systems

T Tamura, I Hamachi - Journal of the American Chemical Society, 2018 - ACS Publications
Chemical modification of proteins provides powerful tools to realize a broad range of
exciting biological applications, including the development of new classes of …

Recent advances in activity-based probes (ABPs) and affinity-based probes (A f BPs) for profiling of enzymes

H Fang, B Peng, SY Ong, Q Wu, L Li, SQ Yao - Chemical Science, 2021 - pubs.rsc.org
Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …

Recent advances in identifying protein targets in drug discovery

J Ha, H Park, J Park, SB Park - Cell chemical biology, 2021 - cell.com
Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …

Metabolites of microbiota response to tryptophan and intestinal mucosal immunity: A therapeutic target to control intestinal inflammation

J Zhang, S Zhu, N Ma, LJ Johnston… - Medicinal Research …, 2021 - Wiley Online Library
In a complex, diverse intestinal environment, commensal microbiota metabolizes excessive
dietary tryptophan to produce more bioactive metabolites connecting with kinds of diverse …