Selective Inhibition of Bruton's Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors

Autor: Sousa, Bárbara B., de Almeida, Cátia Rebelo, Barahona, Ana F., Lopes, Raquel, Martins-Logrado, Ana, Cavaco, Marco, Neves, Vera, Carvalho, Luís A.R., Labaõ-Almeida, Carlos, Coelho, Ana R., Bento, Marta Leal, Lopes, Ricardo M.R.M., Oliveira, Bruno L., Castanho, Miguel A.R.B., Neumeister, Peter, Deutsch, Alexander, Vladimer, Gregory I., Krall, Nikolaus, Joaõ, Cristina, Corzana, Francisco, Seixas, Joaõ D., Fior, Rita, Bernardes, Gonçalo J.L., 0000-0002-0938-9038, 0000-0002-2989-7208, 0000-0001-7891-7562, 0000-0003-4205-7585, 0000-0001-5597-8127, 0000-0001-6594-8917

Bruton's tyrosine kinase (BTK) is a member of the TEC-family kinases and crucial for the proliferation and differentiation of B-cells. We evaluated the therapeutic potential of a covalent inhibitor (JS25) with nanomolar potency against BTK and with a

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https://www.repository.cam.ac.uk/handle/1810/343251

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Selective Inhibition of Bruton's Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors.

Autor: Sousa BB; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., de Almeida CR; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Barahona AF; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Lopes R; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Martins-Logrado A; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Cavaco M; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Neves V; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Carvalho LAR; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K., Labão-Almeida C; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Coelho AR; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Leal Bento M; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal.; Centro Hospitalar Lisboa Norte, Department of Hematology and Bone Marrow Transplantation, Avenida Prof. Egas Moniz, 1649-035 Lisbon, Portugal., Lopes RMRM; Research Institute for Medicines (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1600-277 Lisbon, Portugal., Oliveira BL; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Castanho MARB; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal., Neumeister P; Division of Hematology, Medical University of Graz, Auenbruggerplatz 38, 8036 Graz, Austria., Deutsch A; Division of Hematology, Medical University of Graz, Auenbruggerplatz 38, 8036 Graz, Austria., Vladimer GI; Exscientia, The Schrödinger Building, Oxford Science Park, Oxford OX4 4GE, U.K., Krall N; Exscientia, The Schrödinger Building, Oxford Science Park, Oxford OX4 4GE, U.K., João C; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Corzana F; Centro de Investigación en Síntesis Química, Departamento de Química, Universidad de La Rioja, 26006 Logroño, Spain., Seixas JD; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal.; TARGTEX S.A., Avenida Tenente Valadim, N°17, 2F, 2560-275 Torres Vedras, Portugal., Fior R; Champalimaud Foundation, Avenida de Brasília, 1400-038, Lisbon, Portugal., Bernardes GJL; Instituto de Medicina Molecular João Lobo Antunes, Faculdade de Medicina, Universidade de Lisboa, Avenida Prof. Egas Moniz, 1649-028, Lisbon, Portugal.; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K.

Publikováno v: ACS pharmacology & translational science [ACS Pharmacol Transl Sci] 2022 Nov 02; Vol. 5 (11), pp. 1156-1168. Date of Electronic Publication: 2022 Nov 02 (Print Publication: 2022).