Article
Contribution of Noncovalent Recognition and Reactivity to the Optimization of Covalent Inhibitors: A Case Study on KRasG12C.
ACS chemical biology - 16 Aug 2024
Péczka Nikolett, Ranđelović Ivan, Orgován Zoltán, Csorba Noémi, Egyed Attila, Petri László, Ábrányi-Balogh Péter, Gadanecz Márton, Perczel András, Tóvári József, Schlosser Gitta, Takács Tamás, Mihalovits Levente M, Ferenczy György G, Buday László, Keserű György M
Abstract excerpt
Covalent drugs might bear electrophiles to chemically modify their targets and have the potential to target previously undruggable proteins with high potency. Covalent binding of drug-size molecules includes a noncovalent recognition provided by secondary interactions and a chemical reaction leading to covalent complex formation. Optimization of their covalent mechanism of action should involve both types of...
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