A new class of simplified phorbol ester analogues: synthesis and binding to PKC and eta PKC-C1B (eta PKC-CRD2).
[formula: see text] A unique class of simplified phorbol ester analogues is described for the first time. A highly efficient retro-annelation sequence was developed in order to remove the five-membered ring from the phorbol diterpene core, allowing access to BCD ring analogues of the phorbol esters. The binding of these analogues to protein kinase C (PKC) and the truncated peptide eta PKC-C1B (eta PKC-CRD2) is also reported.
Wender
P A
PA
Department of Chemistry, Stanford University, California 94305, USA. wenderp@leland.stanford.edu
Kirschberg
T A
TA
Williams
P D
PD
Bastiaans
H M
HM
Irie
K
K
D000818:Animals; D051379:Mice; D010703:Phorbol Esters / Q000138:chemical synthesis* / Q000378:metabolism; D011493:Protein Kinase C / Q000378:metabolism*; D051381:Rats; D013379:Substrate Specificity
D010703:Phorbol Esters; D011493:Protein Kinase C