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Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton’s tyrosine kinase inhibitors

Brian T. Hopkins, Eris Bame, Noah Bell, Tonika Bohnert, Jon K. Bowden-Verhoek, Minna Bui, Mark T. Cancilla, Patrick R. Conlon, Patrick Cullen, Daniel A. Erlanson,

Bioorganic & Medicinal Chemistry · 2021 · 11 citations · 23 references

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Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

Frank Lovering, Jack Bikker, Christine Humblet · Journal of Medicinal Chemistry · 2009 · 4.4K citations

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The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

Lee Honigberg, Ashley M. Smith, Mint Sirisawad et al. · Proceedings of the National Academy of Sciences · 2010 · 1.5K citations · Full text

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The gene involved in X-linked agammaglobulinaemia is a member of the src family of protein-tyrosine kinases

David Vetrie, Igor Vořechovský, Paschalis Sideras et al. · Nature · 1993 · 1.5K citations

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Deficient expression of a B cell cytoplasmic tyrosine kinase in human X-linked agammaglobulinemia

Satoshi Tsukada, Douglas C. Saffran, David J. Rawlings et al. · Cell · 1993 · 1.3K citations

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Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

Jennifer A. Woyach, Richard R. Furman, Ta-Ming Liu et al. · New England Journal of Medicine · 2014 · 1.3K citations · Full text

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