Small heterocycles in multicomponent reactions

BH Rotstein, S Zaretsky, V Rai, AK Yudin - Chemical reviews, 2014 - ACS Publications
Small-ring heterocycles have found many applications both as useful starting materials in
the synthesis of more elaborate structures and as valuable targets of synthesis. Our review …

All roads lead to PP 2A: exploiting the therapeutic potential of this phosphatase

J Sangodkar, CC Farrington, K McClinch… - The FEBS …, 2016 - Wiley Online Library
Protein phosphatase 2A (PP 2A) is a serine/threonine phosphatase involved in the
regulation of many cellular processes. A confirmed tumor suppressor protein, PP 2A is …

[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology

CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors

BR Lanning, LR Whitby, MM Dix, J Douhan… - Nature chemical …, 2014 - nature.com
Kinases are principal components of signal transduction pathways and the focus of intense
basic and drug discovery research. Irreversible inhibitors that covalently modify non-catalytic …

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 …

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

MD Hall, A Yasgar, T Peryea, JC Braisted… - … and applications in …, 2016 - iopscience.iop.org
The sensitivity of fluorescence polarization (FP) and fluorescence anisotropy (FA) to
molecular weight changes has enabled the interrogation of diverse biological mechanisms …

The metabolic serine hydrolases and their functions in mammalian physiology and disease

JZ Long, BF Cravatt - Chemical reviews, 2011 - ACS Publications
Serine hydrolases (SHs) consist of> 200 enzymes in humans characterized by the presence
of an active site serine that is used for the hydrolysis of substrates. The membership of this …

Therapeutic targeting of PP2A

CM O'Connor, A Perl, D Leonard, J Sangodkar… - The international journal …, 2018 - Elsevier
Abstract Protein phosphatase 2A (PP2A) is a major serine/threonine phosphatase that
regulates many cellular processes. Given the central role of PP2A in regulating diverse …

A chemoproteomic platform to quantitatively map targets of lipid-derived electrophiles

C Wang, E Weerapana, MM Blewett, BF Cravatt - Nature methods, 2014 - nature.com
Cells produce electrophilic products with the potential to modify and affect the function of
proteins. Chemoproteomic methods have provided a means to qualitatively inventory …

The pharmacological landscape and therapeutic potential of serine hydrolases

DA Bachovchin, BF Cravatt - Nature reviews Drug discovery, 2012 - nature.com
Serine hydrolases perform crucial roles in many biological processes, and several of these
enzymes are targets of approved drugs for indications such as type 2 diabetes, Alzheimer's …