The chemistry-medicine continuum: Synthetic, computer, spectroscopic and biological studies on new chemotherapeutic leads

Paul A. Wender, Yolanda Martin-Cantalejo, Andrew J. Carpenter, Anna Chiu, Jef De Brabander, Patrick G. Harran, Juan Miguel Jimenez, Michael F T Koehler, Blaise Lippa, James A. Morrison, Stephan G. Müller, Stephan N. Müller, Cheol Min Park, Makoto Shiozaki, Carsten Siedenbiedel, Donald J. Skalitzky, Masahiro Tanaka, Kazuhiro Irie

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

This lecture provides an overview of investigations directed towards understanding the molecular mechanism of protein kinase C (PKC) activation and function. Central to this effort are studies on the total synthesis of phorbol, the first asymmetric synthesis of phorbol, and the first synthesis of resiniferatoxin, all involving highly effective applications of [5+2] oxidopyrylium-alkene cycloadditions. The synthesis and affinities of the phorbol ester binding domain of PKC are also presented. In addition, a pharmacophore model for agonist binding to PKC is presented in connection with the design of novel PKC activators. Finally, the computer modeling, NMR structure, synthesis, and biological activity of the first fully synthetic bryostatin analogs are described.

Original languageEnglish (US)
Pages (from-to)539-546
Number of pages8
JournalPure and Applied Chemistry
Volume70
Issue number3
StatePublished - Mar 1998

Fingerprint

Medicine
Protein Kinase C
Proteins
Bryostatins
Cycloaddition
Alkenes
Phorbol Esters
Bioactivity
Olefins
Esters
Chemical activation
Nuclear magnetic resonance
phorbol

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Wender, P. A., Martin-Cantalejo, Y., Carpenter, A. J., Chiu, A., De Brabander, J., Harran, P. G., ... Irie, K. (1998). The chemistry-medicine continuum: Synthetic, computer, spectroscopic and biological studies on new chemotherapeutic leads. Pure and Applied Chemistry, 70(3), 539-546.

The chemistry-medicine continuum : Synthetic, computer, spectroscopic and biological studies on new chemotherapeutic leads. / Wender, Paul A.; Martin-Cantalejo, Yolanda; Carpenter, Andrew J.; Chiu, Anna; De Brabander, Jef; Harran, Patrick G.; Jimenez, Juan Miguel; Koehler, Michael F T; Lippa, Blaise; Morrison, James A.; Müller, Stephan G.; Müller, Stephan N.; Park, Cheol Min; Shiozaki, Makoto; Siedenbiedel, Carsten; Skalitzky, Donald J.; Tanaka, Masahiro; Irie, Kazuhiro.

In: Pure and Applied Chemistry, Vol. 70, No. 3, 03.1998, p. 539-546.

Research output: Contribution to journalArticle

Wender, PA, Martin-Cantalejo, Y, Carpenter, AJ, Chiu, A, De Brabander, J, Harran, PG, Jimenez, JM, Koehler, MFT, Lippa, B, Morrison, JA, Müller, SG, Müller, SN, Park, CM, Shiozaki, M, Siedenbiedel, C, Skalitzky, DJ, Tanaka, M & Irie, K 1998, 'The chemistry-medicine continuum: Synthetic, computer, spectroscopic and biological studies on new chemotherapeutic leads', Pure and Applied Chemistry, vol. 70, no. 3, pp. 539-546.
Wender, Paul A. ; Martin-Cantalejo, Yolanda ; Carpenter, Andrew J. ; Chiu, Anna ; De Brabander, Jef ; Harran, Patrick G. ; Jimenez, Juan Miguel ; Koehler, Michael F T ; Lippa, Blaise ; Morrison, James A. ; Müller, Stephan G. ; Müller, Stephan N. ; Park, Cheol Min ; Shiozaki, Makoto ; Siedenbiedel, Carsten ; Skalitzky, Donald J. ; Tanaka, Masahiro ; Irie, Kazuhiro. / The chemistry-medicine continuum : Synthetic, computer, spectroscopic and biological studies on new chemotherapeutic leads. In: Pure and Applied Chemistry. 1998 ; Vol. 70, No. 3. pp. 539-546.
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