Enzastaurin: A Lesson in Drug Development

Highlights • The development of the proposed anticancer drug Enzastaurin is reviewed. • Protein Kinase C structure and function are discussed with a focus on isozyme specific inhibitors. • Enzastaurin’s molecular mechanisms are examined. • Enzastaurin’s preclinical and clinical efficacies are scruti...

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Bibliographic Details
Published in:Critical reviews in oncology/hematology 2017-04, Vol.112, p.72-79
Main Authors: Bourhill, T, Narendran, A, Johnston, R.N
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - pharmacology
Drug Design
Drug development
Enzastaurin
Hematology, Oncology and Palliative Medicine
Humans
Indoles - pharmacology
Neoplasms - drug therapy
Protein kinase C
Protein Kinase C beta - antagonists & inhibitors
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Summary:Highlights • The development of the proposed anticancer drug Enzastaurin is reviewed. • Protein Kinase C structure and function are discussed with a focus on isozyme specific inhibitors. • Enzastaurin’s molecular mechanisms are examined. • Enzastaurin’s preclinical and clinical efficacies are scrutinized. • Challenges associated with drug development are explored.
ISSN:1040-8428
1879-0461
DOI:10.1016/j.critrevonc.2017.02.003