Illuminating function of the understudied druggable kinome

Gomez, Shawn M.; Axtman, Alison D.; Willson, Timothy M.; Major, Michael B.; Townsend, Reid R.; Sorger, Peter K.; Johnson, Gary L.

doi:10.1016/j.drudis.2024.103881

Drug Discovery Today

2024

DOI: 10.1016/j.drudis.2024.103881

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Illuminating function of the understudied druggable kinome

Shawn M. Gomez,

Alison D. Axtman,

Timothy M. Willson

et al.

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2024

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Cited by 4 publications

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Illuminating the druggable genome: Pathways to progress

Sharma,

Colvis,

Rodgers

et al. 2024

Drug Discovery Today

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Illuminating the druggable genome: Pathways to progress

Sharma,

Colvis,

Rodgers

et al. 2024

Drug Discovery Today

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Assessing Darkness of the Human Kinome from a Medicinal Chemistry Perspective

Voßen,

Xerxa,

Bajorath

2024

J. Med. Chem.

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In drug discovery, human protein kinases (PKs) represent one of the major target classes due to their central role in cellular signaling, implication in various diseases as a consequence of deregulated signaling, and notable druggability. Individual PKs and their disease biology have been explored to different degrees, giving rise to heterogeneous functional knowledge and disease associations across the human kinome. The U.S. National Institutes of Health previously designated 162 understudied (“dark”) human PKs and lipid kinases due to the lack of functional annotations and high-quality molecular probes for functional investigations. Given the large volumes of available PK inhibitors (PKIs) and activity data, we have systematically analyzed the distribution of PKIs and associated data at different confidence levels across the human kinome and distinguished between chemically explored, underexplored, and unexplored PKs. The analysis provides a medicinal chemistry-centric view of PK exploration and further extends prior assessment of the dark kinome.

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Kinase Drug Discovery: Impact of Open Science and Artificial Intelligence

Miljković,

Bajorath

2024

Mol. Pharmaceutics

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Illuminating function of the understudied druggable kinome

Cited by 4 publications

References 53 publications

Illuminating the druggable genome: Pathways to progress

Illuminating the druggable genome: Pathways to progress

Assessing Darkness of the Human Kinome from a Medicinal Chemistry Perspective

Kinase Drug Discovery: Impact of Open Science and Artificial Intelligence

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