Therapeutic Potential of Coumestan Pks13 Inhibitors for Tuberculosis
Shichun Lun, Shiqi Xiao, Wei Zhang, Shuangshuang Wang, Hendra Gunosewoyo, Li-Fang Yu, William R. Bishai
Abstract
Polyketide synthase 13 (Pks13) is an important enzyme found in Mycobacterium tuberculosis that condenses two fatty acyl chains to produce α-alkyl β-ketoesters, which in turn serve as the precursors for the synthesis of mycolic acids that are essential building blocks for maintaining the cell wall integrity of M. tuberculosis . Coumestan derivatives have recently been identified in our group as a new chemotype that exerts its antitubercular effects via targeting of Pks13.
Topics & Concepts
Mycobacterium tuberculosisTuberculosisBioavailabilityPharmacologyCytotoxicityAntibioticsMicrobiologyPolyketideDrugPharmacokineticsDrug resistanceChemistryEnzymeBiologyMedicineIn vitroBiochemistryBiosynthesisPathologyMicrobial Natural Products and BiosynthesisCancer therapeutics and mechanismsMycobacterium research and diagnosis