Current Status and Future Prospects of C1 Domain Ligands as Drug Candidates

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http://hdl.handle.net/10138/161200

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Boije af Gennäs , G , Talman , V , Yli-Kauhaluoma , J , Tuominen , R K & Ekokoski , E 2011 , ' Current Status and Future Prospects of C1 Domain Ligands as Drug Candidates ' , Current Topics in Medicinal Chemistry , vol. 11 , no. 11 , pp. 1370-1392 .

Title: Current Status and Future Prospects of C1 Domain Ligands as Drug Candidates
Author: Boije af Gennäs, Gustav; Talman, Virpi; Yli-Kauhaluoma, Jari; Tuominen, Raimo K.; Ekokoski, Elina
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
Date: 2011
Language: eng
Number of pages: 23
Belongs to series: Current Topics in Medicinal Chemistry
ISSN: 1568-0266
URI: http://hdl.handle.net/10138/161200
Abstract: The second messenger diacylglycerol (DAG) plays a central role in the signal transduction of G-protein coupled receptors and receptor tyrosine kinases by binding to C1 domain of effector proteins. C1 domain was first identified in protein kinase C (PKC) which comprises a family of ten isoforms that play roles in diverse cellular processes such as proliferation, apoptosis and differentiation. Aberrant signaling through PKC isoforms and other C1 domain-containing proteins has been implicated in several pathological disorders. Drug discovery concerning C1 domains has exploited both natural products and rationally designed compounds. Currently, molecules from several classes of C1 domain-binding compounds are in clinical trials; however, still more have the potential to enter the drug development pipeline. This review gives a summary of the recent developments in C1 domain-binding compounds.
Subject: Protein kinase C
C1 domain
drug discovery
cancer
Alzheimer's disease
bryostatins
ingenol-3-angelate
DAG-lactones
PROTEIN-KINASE-C
CONFORMATIONALLY CONSTRAINED ANALOGS
CHRONIC LYMPHOCYTIC-LEUKEMIA
ACTIVATOR-BINDING DOMAIN
PHORBOL ESTER RECEPTOR
CELLS IN-VITRO
NF-KAPPA-B
NEURONAL ELAV PROTEINS
LACTONES DAG-LACTONES
PROSTATE-CANCER CELLS
317 Pharmacy
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