From Functional Fatty Acids to Potent and Selective Natural-Product-Inspired Mimetics via Conformational Profiling.

Autor: Markham LE; Department of Chemistry, Dartmouth College, 6128 Burke Laboratory, Hanover, New Hampshire 03755, United States., Koelblen T; University of Florida Genetics Institute, P.O. Box 103610, 2033 Mowry Road, Gainesville, Florida 32610, United States., Chobanian HR; ROME Therapeutics, 201 Brookline Avenue, Suite 1001, Boston, Massachusetts 02215, United States., Follis AV; ROME Therapeutics, 201 Brookline Avenue, Suite 1001, Boston, Massachusetts 02215, United States., Burris TP; University of Florida Genetics Institute, P.O. Box 103610, 2033 Mowry Road, Gainesville, Florida 32610, United States., Micalizio GC; Department of Chemistry, Dartmouth College, 6128 Burke Laboratory, Hanover, New Hampshire 03755, United States.

Publikováno v: ACS central science [ACS Cent Sci] 2024 Feb 12; Vol. 10 (2), pp. 477-486. Date of Electronic Publication: 2024 Feb 12 (Print Publication: 2024).

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.

Autor: Caldwell RD; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Qiu H; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Askew BC; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Bender AT; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Brugger N; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Camps M; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Dhanabal M; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Dutt V; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Eichhorn T; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Gardberg AS; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Goutopoulos A; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Grenningloh R; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Head J; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Healey B; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Hodous BL; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Huck BR; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Johnson TL; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Jones C; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Jones RC; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Mochalkin I; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Morandi F; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Nguyen N; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Meyring M; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Potnick JR; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Santos DC; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Schmidt R; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Sherer B; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Shutes A; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Urbahns K; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Follis AV; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Wegener AA; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Zimmerli SC; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States., Liu-Bujalski L; EMD Serono Research & Development Institute, Inc. (a Business of Merck KGaA, Darmstadt, Germany) , 45 A Middlesex Turnpike , Billerica , Massachusetts 01821 , United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2019 Sep 12; Vol. 62 (17), pp. 7643-7655. Date of Electronic Publication: 2019 Aug 15.

Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.

Autor: Qiu H; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA. Electronic address: hui.qiu@emdserono.com., Liu-Bujalski L; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Caldwell RD; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Follis AV; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Gardberg A; Constellation Pharmaceuticals, 215 First Street, Suite 200, Cambridge, MA 02142, USA., Goutopoulos A; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Grenningloh R; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Head J; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Johnson T; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Jones R; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Mochalkin I; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Morandi F; F. Hoffmann-La Roche AG, Konzern-Hauptsitz, Grenzacherstrasse 124, CH-4070 Basel, Switzerland., Neagu C; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA., Sherer B; EMD Serono Research & Development Institute, Inc., 45A Middlesex Turnpike, Billerica 01821, MA, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Sep 15; Vol. 28 (17), pp. 2939-2944. Date of Electronic Publication: 2018 Jul 05.

Dynamic Protein Interaction Networks and New Structural Paradigms in Signaling.

Autor: Csizmok V; Molecular Structure & Function, The Hospital for Sick Children , Toronto, ON M5G 0A4, Canada., Follis AV; Department of Structural Biology, St. Jude Children's Research Hospital , Memphis, Tennessee 38105, United States., Kriwacki RW; Department of Structural Biology, St. Jude Children's Research Hospital , Memphis, Tennessee 38105, United States.; Department of Microbiology, Immunology and Biochemistry, University of Tennessee Health Sciences Center , Memphis, Tennessee 38163, United States., Forman-Kay JD; Molecular Structure & Function, The Hospital for Sick Children , Toronto, ON M5G 0A4, Canada.; Department of Biochemistry, University of Toronto , Toronto, ON M5S 1A8, Canada.

Publikováno v: Chemical reviews [Chem Rev] 2016 Jun 08; Vol. 116 (11), pp. 6424-62. Date of Electronic Publication: 2016 Feb 29.

The DNA-binding domain mediates both nuclear and cytosolic functions of p53.

Autor: Follis AV; Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA., Llambi F; Department of Immunology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA., Ou L; Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA., Baran K; Department of Immunology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA., Green DR; Department of Immunology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA., Kriwacki RW; 1] Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, Tennessee, USA. [2] Department of Microbiology, Immunology and Biochemistry, University of Tennessee Health Sciences Center, Memphis, Tennessee, USA.

Publikováno v: Nature structural & molecular biology [Nat Struct Mol Biol] 2014 Jun; Vol. 21 (6), pp. 535-43. Date of Electronic Publication: 2014 May 11.