Single site-modified congeners of vinblastine dissociate its various anti-microtubule actions.
New C-20' alkyl congeners of vinblastine (VBL) were examined for their reaction with purified microtubule protein or steady-state microtubules in vitro. We found that each of the three typical activities of VBL with this system was amenable to alteration through structural modification of the molecule at this single site. The activity profiles were congener-specific, and they establish the dissociable nature of the various actions that characterize the parent molecule, VBL.
Borman
L S
LS
Department of Pharmacology, University of Vermont, Burlington.
Kuehne
M E
ME
Matson
P A
PA
Marko
I
I
Zebovitz
T C
TC
D000818:Animals; D001921:Brain / Q000378:metabolism; D002417:Cattle; D008868:Microtubule Proteins / Q000378:metabolism*; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure; D013329:Structure-Activity Relationship; D014747:Vinblastine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D008868:Microtubule Proteins; D014747:Vinblastine