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Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase by Ron Grey; Albert C. Pierce; Guy W. Bemis; Marc D. Jacobs; Cameron Stuver Moody; Rahul Jajoo; Narinder Mohal; Jeremy Green is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase about?

A series of substituted 3-aryl-6-amino-triazolo[4,3-b]pyridazines were identified as highly selective inhibitors of Pim-1 kinase. Initial exploration identified compound 24 as a potent, selective inhibitor, limited in its utility by poor solubility and permeability. Understanding the unusual ATP-binding site of the Pim kinases and X-ray crystallographic data on compound 24 led to design improvements in this class of inhibitor. This resulted in compound 29, a selective, soluble and permeable inhibitor of Pim-1.

Who reads Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase?

Author

Ron Grey; Albert C. Pierce; Guy W. Bemis; Marc D. Jacobs; Cameron Stuver Moody; Rahul Jajoo; Narinder Mohal; Jeremy Green

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)