Journal
CHEMMEDCHEM
Volume 14, Issue 9, Pages 889-906Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201900107
Keywords
acetylcholinesterase; caspase; cathepsin; covalent inhibitors; protein kinases; RAS proteins
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Funding
- US National Institutes of Health [R01GM121584, R01GM127575]
- Cancer Prevention & Research Institute of Texas [RP170797]
- Welch Foundation [A1715]
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Although covalent inhibitors have been used as therapeutics for more than a century, there has been general resistance in the pharmaceutical industry against their further development due to safety concerns. This inclination has recently been reverted after the development of a wide variety of covalent inhibitors to address human health conditions along with the US Food and Drug Administration (FDA) approval of several covalent therapeutics for use in humans. Along with this exciting resurrection of an old drug discovery concept, this review surveys enzymes that can be targeted by covalent inhibitors for the treatment of human diseases. We focus on protein kinases, RAS proteins, and a few other enzymes that have been studied extensively as targets for covalent inhibition, with the aim to address challenges in designing effective covalent drugs and to provide suggestions in the area that have yet to be explored.
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