scholarly journals Introductory Chapter: Protein Kinases as Promising Targets for Drug Design against Cancer

2021 ◽  
Author(s):  
Rohit Bhatia ◽  
Rajesh K. Singh
Keyword(s):  
Drug Design ◽  
Protein Kinases

scholarly journals Evolution of kinase polypharmacology across HSP90 drug discovery

2020 ◽  
Author(s):  
Albert A. Antolin ◽  
Paul A. Clarke ◽  
Ian Collins ◽  
Paul Workman ◽  
Bissan Al-Lazikani
Keyword(s):  
Drug Discovery ◽  
Drug Design ◽  
Small Molecules ◽  
Protein Kinases ◽  
Experimental Methods ◽  
Experimental Characterization ◽  
Hsp90 Inhibitors ◽  
Target Drug ◽  
Clinical Candidate

AbstractMost small molecules interact with several target proteins but this polypharmacology is seldom comprehensively investigated or explicitly exploited during drug discovery. Here, we use computational and experimental methods to systematically characterize the kinase cross-pharmacology of representative HSP90 inhibitors. We demonstrate that the resorcinol clinical candidates ganetespib and, to a lesser extent, luminespib, display unique off-target kinase pharmacology as compared to other HSP90 inhibitors. We also demonstrate that polypharmacology evolved during the optimisation to discover luminespib and that the hit, leads and clinical candidate all have different polypharmacological profiles. We conclude that the submicromolar target inhibition of protein kinases by ganetespib may have potential clinical significance and we recommend the computational and experimental characterization of polypharmacology earlier in drug discovery projects to unlock new multi-target drug design opportunities.

Bacterial Eukaryotic Type Serine-Threonine Protein Kinases: From Structural Biology to Targeted Anti-Infective Drug Design

2011 ◽  
Vol 11 (11) ◽  
pp. 1352-1369 ◽  
Author(s):  
Valery N. Danilenko ◽  
Dmitry I. Osolodkin ◽  
Sergey A. Lakatosh ◽  
Maria N. Preobrazhenskaya ◽  
Alexander A. Shtil
Keyword(s):  
Drug Design ◽  
Protein Kinases ◽  
Structural Biology

Peptides Targeting Protein Kinases: Strategies and Implications

Physiology ◽  
2006 ◽  
Vol 21 (6) ◽  
pp. 411-418 ◽  
Author(s):  
Oksana Kaidanovich-Beilin ◽  
Hagit Eldar-Finkelman
Keyword(s):  
Drug Design ◽  
Signaling Pathways ◽  
Protein Kinases ◽  
Human Diseases ◽  
Biological Processes ◽  
Potential Drug ◽  
Therapeutic Implications ◽  
Active Peptides ◽  
Drug Compounds

Protein kinases are important key regulators in most, if not all, biological processes and are linked with many human diseases. Protein kinases thus became attractive targets for drug design. Intracellularly active peptides that selectively interfere with kinase function and or kinase-mediated signaling pathways are potential drug compounds with therapeutic implications.

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