European Journal of Medicinal Chemistry p. 537 - 549 (1994)
Update date:2022-08-03
Topics:
Young
Downes
Jones
Milliner
Rana
Ward
Analogues of phosphatidylinositol (PtdIns, 1) have been synthesized to investigate the structural requirements for inhibition of a PtdIns 4-kinase obtained from human erythrocyte membranes. While the presence of either D-1 or D-3 stereochemistry in the inositol moiety greatly influences the degree of inhibition produced by PtdIns analogues, the stereochemistry of the glycerol moiety is of little consequence. Neither structural feature however, makes a significant contribution to binding affinity. Competitive inhibitory activity was found to be retained (or even enhanced) in substantially simpler analogues consisting of 1 or 2 hydrocarbon chains attached to a charged phosphate head group, such as in the phosphatidic acids, 24 and 26. The observation that the phosphatidylinositol 4-phosphate (PtdIns 4P) and phosphatidic acid analogues (eg, 16 or 17, and 26 respectively) inhibit PtdIns 4-kinase may suggest that such species have a regulatory role in PtdIns turnover.
View MoreShanghai Zhihua ChemTech Co., Ltd.
Contact:+86-13774313779
Address:Room 817 Suite B 3333 Shenjiang Road
Zipont chem(wuhan)Tech co.,Ltd
Contact:+86-27-87587198
Address:wuhan
Qingdao Pana-Life Biochem Co.,Ltd.
Contact:86-532-87683902
Address:No.967 Dalao Road, Licang Zone, Qingdao City,Shandong, China 266021
Contact:+86-21-38122007
Address:2, Lane 1123, Kangqiao Road, Pudong New Area, Shanghai
Contact:86-21-50966856
Address:Building 5,300 Chuanzhan Road,Pudong New District,Shanghai
Doi:10.1016/S0040-4039(00)85157-6
(1986)Doi:10.1007/s10870-009-9622-0
(2009)Doi:10.3987/COM-08-S(N)99
(2008)Doi:10.1021/jm00395a014
(1987)Doi:10.1016/j.dyepig.2010.06.006
(2011)Doi:10.1002/ejic.200700602
(2007)