title: Facile synthesis of SAM-peptide conjugates through alkyl linkers targeting proteinN-terminal methyltransferase 1.
abstract: We report the first chemical synthesis of SAM-peptide conjugates through alkyl linkers to prepare bisubstrate analogs for protein methyltransferases. We demonstrate its application by developing a series of bisubstrate inhibitors for proteinN-terminal methyltransferase 1 and the most potent one exhibits aKivalue of 310 ± 55 nM.
authors: Department of Medicinal Chemistry, Institute for Structural Biology, Drug Discovery & Development, Virginia Commonwealth University, Richmond, VA, 23219, USA.
authors: Gang
authors: G
authors: Zhang
authors: Department of Medicinal Chemistry, Institute for Structural Biology, Drug Discovery & Development, Virginia Commonwealth University, Richmond, VA, 23219, USA.
authors: Rong
authors: R
authors: Huang