Peter Rosston

Joint Center for Structural Genomics

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Panagiotis Prinos

University of Toronto

David H. Drewry

University of North Carolina at Chapel Hill

Brian Anderson

Joint Center for Structural Genomics

Alison D. Axtman

University of North Carolina at Chapel Hill

Han Wee Ong

University of North Carolina at Chapel Hill

Capener J.L

Jacob L. Capener

University of North Carolina at Chapel Hill

Flax R.G

Raymond G. Flax

Joint Center for Structural Genomics

Drewry D.H.

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University of North Carolina at Chapel Hill

Joint Center for Structural Genomics

Structural Genomics Consortium

McGill University

Svenskt Gastekniskt Center

International Drug Development

University of North Carolina Health Care

Montreal Neurological Institute and Hospital

Discovery Centre

Communities In Schools of Orange County

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How many kinases are druggable? A review of our current understanding

Biochemical Journal (2023)

Brian Anderson Peter Rosston Han Wee Ong Mohammad Anwar Hossain Zachary W. Davis‐Gilbert

There are over 500 human kinases ranging from very well-studied to almost completely ignored. Kinases are tractable and implicated in many diseases, making them ideal targets for medicinal chemistry campaigns, but is it possible to discover a drug for each individual kinase? For every human kinase, we gathered data on their citation count, availability of chemical probes, approved and investigational drugs, PDB structures, and biochemical and cellular assays. Analysis of these factors highlights which kinase groups have a wealth of information available, and which groups still have room for progress. The data suggest a disproportionate focus on the more well characterized kinases while much of the kinome remains comparatively understudied. It is noteworthy that tool compounds for understudied kinases have already been developed, and there is still untapped potential for further development in this chemical space. Finally, this review discusses many of the different strategies employed to generate selectivity between kinases. Given the large volume of information available and the progress made over the past 20 years when it comes to drugging kinases, we believe it is possible to develop a tool compound for every human kinase. We hope this review will prove to be both a useful resource as well as inspire the discovery of a tool for every kinase.

Kinome

Druggability

10.1042/bcj20220217

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Citations (19)

Illumination of understudied ciliary kinases

Frontiers in Molecular Biosciences (2024)

Raymond G. Flax Peter Rosston Cecilia Rocha Brian Anderson Jacob L. Capener

Cilia are cellular signaling hubs. Given that human kinases are central regulators of signaling, it is not surprising that kinases are key players in cilia biology. In fact, many kinases modulate ciliogenesis, which is the generation of cilia, and distinct ciliary pathways. Several of these kinases are understudied with few publications dedicated to the interrogation of their function. Recent efforts to develop chemical probes for members of the cyclin-dependent kinase like (CDKL), never in mitosis gene A (NIMA) related kinase (NEK), and tau tubulin kinase (TTBK) families either have delivered or are working toward delivery of high-quality chemical tools to characterize the roles that specific kinases play in ciliary processes. A better understanding of ciliary kinases may shed light on whether modulation of these targets will slow or halt disease onset or progression. For example, both understudied human kinases and some that are more well-studied play important ciliary roles in neurons and have been implicated in neurodevelopmental, neurodegenerative, and other neurological diseases. Similarly, subsets of human ciliary kinases are associated with cancer and oncological pathways. Finally, a group of genetic disorders characterized by defects in cilia called ciliopathies have associated gene mutations that impact kinase activity and function. This review highlights both progress related to the understanding of ciliary kinases as well as in chemical inhibitor development for a subset of these kinases. We emphasize known roles of ciliary kinases in diseases of the brain and malignancies and focus on a subset of poorly characterized kinases that regulate ciliary biology.

Ciliogenesis

Ciliopathies

10.3389/fmolb.2024.1352781

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Illumination of understudied ciliary kinases

Carolina Digital Repository (University of North Carolina at Chapel Hill) (2024)

Flax R.G Peter Rosston Clarissa Araújo Gurgel Rocha B. J. Anderson Capener J.L

10.17615/bvdg-w241

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