A New Class of Simplified Phorbol Ester Analogues: Synthesis and Binding to PKC and ηPKC-C1B (ηPKC-CRD2)
Paul A. Wender, Thorsten Kirschberg, Peter Williams, H. M. M. BASTIAANS, Kazuhiro Irie
Abstract
Paul A. Wender, Thorsten Kirschberg, Peter Williams, H. M. M. BASTIAANS, Kazuhiro Irie
Abstract
[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.
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[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.
Key concepts: Protein kinase C, Phorbol ester, Phorbol, Chemistry, Stereochemistry, Ring (chemistry), Kinase, Biochemistry