Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase.
Authors:Baltgalvis KA,Lamb KN,Symons KT,Wu CC,Hoffman MA,Snead AN,Song X,Glaza T,Kikuchi S,Green JC,Rogness DC,Lam B,Rodriguez-Aguirre ME,Woody DR,Eissler CL,Rodiles S,Negron SM,Bernard SM,Tran E,Pollock J,Tabatabaei A,Contreras V,Williams HN,Pastuszka MK,Sigler JJ,Pettazzoni P,Rudolph MG,Classen M,Brugger D,Claiborne C,Plancher JM,Cuartas I,Seoane J,Burgess LE,Abraham RT,Weinstein DS,Simon GM,Patricelli MP,Kinsella TM
Journal:Nature
PubMed ID:38658751
WRN helicase is a promising target for treatment of cancers with microsatellite instability (MSI) due to its essential role in resolving deleterious non-canonical DNA structures that accumulate in cells with faulty mismatch repair mechanisms(1-5). Currently there are no approved drugs directly targeting human DNA or RNA helicases, in part owing ... More