Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1

Author:

Lucas Simon C. C.1ORCID,Milbradt Alexander G.2,Blackwell J. Henry1,Bonomo Silvia1,Brierley Andrew3,Cassar Doyle J.4ORCID,Freeman Jared5,Hadfield Thomas E.1,Morrill Lucas A.6,Riemens Rick7,Sarda Sunil3,Schiesser Stefan8ORCID,Wiktelius Daniel9ORCID,Ahmed Samiyah10,Bostock Mark J.2,Börjesson Ulf11,De Fusco Claudia1ORCID,Guerot Carine4,Hargreaves David2,Hewitt Sarah2,Lamb Michelle L.6ORCID,Su Nancy12,Whatling Ryan2,Wheeler Matthew2ORCID,Kettle Jason G.4ORCID

Affiliation:

1. Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

2. Mechanistic and Structural Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

3. Compound Synthesis and Management, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

4. Medicinal Chemistry, Oncology R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

5. Medicinal Chemistry, Research and Early Development, Cardiovascular, Renal and Metabolic Disorders (CVRM), Biopharmaceuticals R&D, AstraZeneca, Gothenburg, SE-43183, Sweden

6. Medicinal Chemistry, Oncology R&D, AstraZeneca, Waltham, Massachusetts 02451, United States

7. Medicinal Chemistry, Oncology R&D, Acerta B. V., a Part of the AstraZeneca Group, Oss 5349, The Netherlands

8. Medicinal Chemistry, Research and Early Development, Respiratory and Immunology (R&I), Biopharmaceuticals R&D, AstraZeneca, Gothenburg, SE-43183, Sweden

9. Compound Synthesis and Management, Discovery Sciences, R&D, AstraZeneca, Gothenburg, SE-43183, Sweden

10. Discovery Biology, Discovery Sciences, R&D, AstraZeneca, Cambridge CB2 0AA, U.K.

11. Hit Discovery, Discovery Sciences, R&D, AstraZeneca, Gothenburg, SE-43183, Sweden

12. Mechanistic and Structural Biology, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States

Publisher

American Chemical Society (ACS)

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