Click chemistry for drug development and diverse chemical–biology applications

P Thirumurugan, D Matosiuk, K Jozwiak - Chemical reviews, 2013 - ACS Publications
Chemistry, traditionally being the science of synthesis and structural manipulations of
molecules, has gradually undertaken the more challenging task of biology-oriented …

Chemical proteomics approaches for identifying the cellular targets of natural products

MH Wright, SA Sieber - Natural product reports, 2016 - pubs.rsc.org
Covering: 2010 up to 2016 Deconvoluting the mode of action of natural products and drugs
remains one of the biggest challenges in chemistry and biology today. Chemical proteomics …

Bacterial proteases, untapped antimicrobial drug targets

E Culp, GD Wright - The Journal of antibiotics, 2017 - nature.com
Bacterial proteases are an extensive collection of enzymes that have vital roles in cell
viability, stress response and pathogenicity. Although their perturbation clearly offers the …

Enzyme inhibitor discovery by activity-based protein profiling

MJ Niphakis, BF Cravatt - Annual review of biochemistry, 2014 - annualreviews.org
Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes.
Selective inhibitors offer powerful probes for assigning functions to enzymes in native …

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

DS Johnson, E Weerapana… - Future medicinal …, 2010 - Taylor & Francis
This article presents several covalent inhibitors, including examples of successful drugs, as
well as highly selective, irreversible inhibitors of emerging therapeutic targets, such as fatty …

Covalent protein modification: the current landscape of residue-specific electrophiles

DA Shannon, E Weerapana - Current opinion in chemical biology, 2015 - Elsevier
Highlights•Electrophiles can show distinct amino-acid selectivities in proteomes.•The
judicious selection of an electrophile is critical to various chemical-proteomic applications.•A …

Small-molecule inhibition of APT1 affects Ras localization and signaling

FJ Dekker, O Rocks, N Vartak, S Menninger… - Nature chemical …, 2010 - nature.com
Cycles of depalmitoylation and repalmitoylation critically control the steady-state localization
and function of various peripheral membrane proteins, such as Ras proto-oncogene …

Electrophilic natural products and their biological targets

M Gersch, J Kreuzer, SA Sieber - Natural product reports, 2012 - pubs.rsc.org
Covering: 1900 to 2011 The study of biologically active natural products has resulted in
seminal contributions to our understanding of living systems. In the case of electrophilic …

Biosynthesis and chemical diversity of β-lactone natural products

SL Robinson, JK Christenson, LP Wackett - Natural product reports, 2019 - pubs.rsc.org
Covering: up to 2018 β-Lactones are strained rings that are useful organic synthons and
pharmaceutical warheads. Over 30 core scaffolds of β-lactone natural products have been …

Advances in the research on the targets of anti-malaria actions of artemisinin

J Yang, Y He, Y Li, X Zhang, YK Wong, S Shen… - Pharmacology & …, 2020 - Elsevier
Malaria has been a global epidemic health threat since ancient times. It still claims roughly
half a million lives every year in this century. Artemisinin and its derivatives, are frontline …