Bioorganic and Medicinal Chemistry Letters p. 1508 - 1512 (2017)
Update date:2022-07-29
Topics:
Meyners, Christian
Wolff, Benjamin
Kleinschek, Alexander
Kr?mer, Andreas
Meyer-Almes, Franz-Josef
A series of perfluorinated SAHA (PFSAHA) was prepared and profiled against a panel of human and bacterial members of the Histone deacetylase (HDAC) family. Some of the active substances show nanomolar inhibitory activity and several hundred fold selectivity for the HDAC like enzyme PA3774 from P. aeruginosa. The extraordinary selectivity against human HDACs results from the distinct oligomeric state of PA3774 which consists of two head-to-head dimers. The binding pocket is defined by the surface of both opposite monomers confining the access of ligands to the active site. In addition, the aromatic cap group of PFSAHA undergoes an edge-to-face aromatic interaction with phenylalanine from the opposite monomer.
View MoreLIANYUNGANG YC FINE CHEMICAL CO., LTD
Contact:+86-518-858 99188
Address:Shangdong Modern Bldg, South Greenpark Road, Lianyungang, Jiangsu Pro. China
Contact:+86-10-83993285
Address:Rm.1708, Haobai Tower, Building 6, No.50, North Road, West Third Ring, Haidian District, Beijing, China
Ji'an Hairui Natural Plant Co. Ltd.
Contact:0796-8105528
Address:Meilin industry park, Qingyuan district Ji'an City, Jiangxi Province
Contact:+86-21-56338808
Address:799 Dunhuang Road, Putuo
Jinhua Haoyuan Chemical CO., LTD(expird)
Contact:86-579-82465583
Address:Jinhua,Zhejiang
Doi:10.1016/S0022-328X(01)01210-4
(2002)Doi:10.1021/ja2081907
(2012)Doi:10.1016/j.bmcl.2011.08.055
(2011)Doi:10.1055/s-0030-1260253
(2011)Doi:10.1016/S0040-4020(00)00408-7
(2000)Doi:10.1002/chem.200700178
(2007)