The Discovery of Novel Protein Kinase Inhibitors by Using Fragment‐Based High‐Throughput X‐ray Crystallography | Zendy

Gill Adrian | Zendy; Cleasby Anne | Zendy; Jhoti Harren | Zendy

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The Discovery of Novel Protein Kinase Inhibitors by Using Fragment‐Based High‐Throughput X‐ray Crystallography

Author(s) -

Gill Adrian,

Cleasby Anne,

Jhoti Harren

Publication year - 2005

Publication title -

chembiochem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.05

H-Index - 126

eISSN - 1439-7633

pISSN - 1439-4227

DOI - 10.1002/cbic.200400188

Subject(s) - fragment (logic) , throughput , kinase , protein kinase a , computational biology , high throughput screening , chemistry , small molecule , biochemistry , biology , computer science , algorithm , telecommunications , wireless

This article describes the application of a high‐throughput X‐ray crystallographic fragment‐based screening methodology to identify low‐molecular‐weight leads for structure‐based optimisation into protein kinase inhibitors. The identification of two novel p38α MAP kinase inhibitors (with IC 50 =65 and 150 n M ) starting from low‐molecular‐weight fragments is described.

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