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Literature DB >> 33492229

Disrupting enzyme fluidity.

Abstract

A combination of X-ray crystallography, NMR, and mass spectrometry has revealed how diverse small-molecule inhibitors bind Bruton's tyrosine kinase and alter the conformation of this enzyme.

Entities: Chemical

Keywords: allostery; bruton tyrosine kinase; drug resistance; hydrogen/deuterium exchange mass spectrometry; kinase inhibitor; molecular biophysics; none; nuclear magnetic resonance; structural biology

Mesh：

Substances：

Year: 2021 PMID： 33492229 PMCID： PMC7834015 DOI： 10.7554/eLife.65221

Source DB: PubMed Journal: Elife ISSN： 2050-084X Impact factor: 8.140

10 in total

Review 1. Theory of protein folding.

Authors: José Nelson Onuchic; Peter G Wolynes
Journal: Curr Opin Struct Biol Date: 2004-02 Impact factor: 6.809

2. Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures.

Authors: Andreas Kuglstatter; April Wong; Stan Tsing; Simon W Lee; Yan Lou; Armando G Villaseñor; J Michael Bradshaw; David Shaw; Jim W Barnett; Michelle F Browner
Journal: Protein Sci Date: 2011-02 Impact factor: 6.725

Review 3. Dynamic personalities of proteins.

Authors: Katherine Henzler-Wildman; Dorothee Kern
Journal: Nature Date: 2007-12-13 Impact factor: 49.962

Review 4. Development of BTK inhibitors for the treatment of B-cell malignancies.

Authors: Hyung-Ook Kim
Journal: Arch Pharm Res Date: 2019-01-31 Impact factor: 4.946

Review 5. Allostery and population shift in drug discovery.

Authors: Gozde Kar; Ozlem Keskin; Attila Gursoy; Ruth Nussinov
Journal: Curr Opin Pharmacol Date: 2010-09-29 Impact factor: 5.547

6. Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases.

Authors: Douglas J Marcotte; Yu-Ting Liu; Robert M Arduini; Catherine A Hession; Konrad Miatkowski; Craig P Wildes; Patrick F Cullen; Victor Hong; Brian T Hopkins; Elisabeth Mertsching; Tracy J Jenkins; Michael J Romanowski; Darren P Baker; Laura F Silvian
Journal: Protein Sci Date: 2010-03 Impact factor: 6.725

Disrupting enzyme fluidity.

Review 1. Theory of protein folding.

2. Insights into the conformational flexibility of Bruton's tyrosine kinase from multiple ligand complex structures.

Review 3. Dynamic personalities of proteins.

Review 4. Development of BTK inhibitors for the treatment of B-cell malignancies.

Review 5. Allostery and population shift in drug discovery.

6. Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases.

Review 7. cAMP-dependent protein kinase defines a family of enzymes.

Review 8. The role of dynamic conformational ensembles in biomolecular recognition.

Review 9. Bruton's TK inhibitors: structural insights and evolution of clinical candidates.

10. Differential impact of BTK active site inhibitors on the conformational state of full-length BTK.