Privileged Electrophile Sensors: A Resource for Covalent Drug Development
Open accessAbstract
This Perspective delineates how redox signaling affects the activity of specific enzyme isoforms and how this property may be harnessed for rational drug design. Covalent drugs have resurged in recent years and several reports have extolled the general virtues of developing irreversible inhibitors. Indeed, many modern pharmaceuticals contain electrophilic appendages. Several invoke a warhead that hijacks active-site nucleophiles whereas others take advantage of spectator nucleophilic side chains that do not participate in enzymatic chemistry, but are poised to bind/react with electrophiles. The latest data suggest that innate electrophile sensing-which enables rapid reaction with an endogenous signaling electrophile-is a quintessential resource for the development of covalent drugs. For instance, based on recent work documenting isoform-specific electrophile sensing, isozyme non-specific drugs may be converted to isozyme-specific analogs by hijacking privileged first-responder electrophile-sensing cysteines. Because this approach targets functionally relevant cysteines, we can simultaneously harness previously untapped moonlighting roles of enzymes linked to redox sensing.
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Covalent inhibitors have potentially more durable inhibition at the PPI site, leading to improved pharmacology in vivo.
“For covalent inhibitors, one of their chief advantages is potentially more durable inhibition at the PPI site leading to improved pharmacology in vivo [117, 118].”
From The design and development of covalent protein-protein interaction inhibitors for cancer treatment (2020) · cites this paper as [117]
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- Authors
- Long, M. J. C., & Aye, Y.
- Affiliations
- Cornell University (US)
- Corresponding author
- Aye, Yimon
- Venue
- Cell Chemical Biology
- Publisher
- Elsevier BV
- Published
- 2017-07
- Volume
- 24
- Issue
- 7
- Pages
- 787-800
- ISSN
- 2451-9448 (ISSN-L)
- 2451-9456
- PMC
- PMC5528179
- OpenAlex
- W2705421977
- Cited by
- 81
- References
- 86
- Citations by year
- 2026: 7 · 2025: 6 · 2024: 6 · 2023: 2 · 2022: 14 · 2021: 15 · 2020: 12 · 2019: 9 · 2018: 8 · 2017: 2
- FWCI
- 0.82
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Cell chemical biology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- NSF CAREER (CHE-1351400)
- NIH-New-Innovator (1DP2GM114850)
- ONR (N00014-17-1-2529)
- Burroughs Wellcome CRTG (R01 NS026539)
- Sloan (FG-2016-6379)
- NIH (1S10RR025502)
- NSF MRI (CHE-1531632)
- NIH SIG (1S10RR025449-01)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Redox biology and oxidative stress
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics, phytochemicals, and oxidative stress
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- redox signaling, isozymes, irreversible inhibitors, electrophilic warheads, moonlighting enzymes, rational drug design
- MeSH terms
- Acrylamides, Aniline Compounds, Animals, Cysteine, Enzyme Inhibitors, Humans, Indoles, Isoenzymes, Piperazines, Pyrimidines, Drug Design, Reactive Oxygen Species, Catalytic Domain, Proto-Oncogene Proteins c-akt, ErbB Receptors
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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