Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl.
The cytotoxic macrolide kendomycin was identified as a ligand of Bcl-xl, an anti-apoptotic member of the Bcl-2 protein family. Hydrolysis-stable and protonable semi-synthetic analogues have been obtained that retain cytotoxicity and Bcl-xl binding.
Janssen
Christian O
CO
MerLion Pharmaceuticals Pte Ltd, Medicinal Chemistry, Singapore Science Park II, Singapore 117528, Singapore.
Lim
Stephanie
S
Lo
Ee Peng
EP
Wan
Kah Fei
KF
Yu
Victor C
VC
Lee
May Ann
MA
Ng
Siew Bee
SB
Everett
Martin J
MJ
Buss
Antony D
AD
Lane
David P
DP
Boyce
Rustum S
RS
D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D006801:Humans; D017828:Rifabutin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D051020:bcl-X Protein / Q000737:chemistry*
D051020:bcl-X Protein; C485395:kendomycin; D017828:Rifabutin