P
Paolo A. Centrella
Researcher at GlaxoSmithKline
Publications - 31
Citations - 1691
Paolo A. Centrella is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Drug discovery & Fumagillin. The author has an hindex of 19, co-authored 30 publications receiving 1351 citations.
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Journal ArticleDOI
Design, synthesis and selection of DNA-encoded small-molecule libraries
Matthew A. Clark,Raksha A. Acharya,Christopher C. Arico-Muendel,Svetlana L. Belyanskaya,Dennis Benjamin,Neil R Carlson,Paolo A. Centrella,Cynthia H. Chiu,Steffen Phillip Creaser,John W. Cuozzo,Christopher P. Davie,Yun Ding,G Joseph Franklin,Kurt D Franzen,Malcolm L. Gefter,Steven P Hale,Nils Jakob Vest Hansen,David I. Israel,Jinwei Jiang,Malcolm J. Kavarana,Michael Kelley,Christopher S. Kollmann,Fan Li,Kenneth E Lind,Sibongile Mataruse,Patricia F Medeiros,Jeffrey A. Messer,Paul Myers,Heather O’Keefe,Matthew C Oliff,Cecil E Rise,Alexander L. Satz,Steven R. Skinner,Jennifer L Svendsen,Lujia Tang,Kurt van Vloten,Richard W. Wagner,Gang Yao,Baoguang Zhao,Barry A. Morgan +39 more
TL;DR: An 800-million-member DNA-encoded library in which small molecules are covalently attached to an encoding oligonucleotide is reported, assembled by a combination of chemical and enzymatic synthesis, and interrogated by affinity selection.
Journal ArticleDOI
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Hongfeng Deng,Heather O’Keefe,Christopher P. Davie,Kenneth E Lind,Raksha A. Acharya,G Joseph Franklin,J. Larkin,Rosalie Matico,Michael Neeb,Monique M Thompson,Thomas Lohr,Jeffrey W. Gross,Paolo A. Centrella,Gary K. O’Donovan,Katie L Sargent Bedard,Kurt van Vloten,Sibongile Mataruse,Steven R. Skinner,Svetlana L. Belyanskaya,Tiffany Carpenter,Todd W Shearer,Matthew A. Clark,John W. Cuozzo,Christopher C. Arico-Muendel,Barry A. Morgan +24 more
TL;DR: This study provides the first small molecule evidence for the critical role of ADAMTS-5 in human cartilage degradation by employing encoded library technology (ELT), which enables affinity selection of small molecule binders from complex mixtures by DNA tagging.
Journal ArticleDOI
Cell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor.
Zining Wu,Todd L. Graybill,Xin Zeng,Michael Platchek,Jean Zhang,Vera Q. Bodmer,David D. Wisnoski,Jianghe Deng,Frank T. Coppo,Gang Yao,Alex M. Tamburino,Genaro S. Scavello,G Joseph Franklin,Sibongile Mataruse,Katie L Sargent Bedard,Yun Ding,Jing Chai,Jennifer Summerfield,Paolo A. Centrella,Jeffrey A. Messer,Andrew J. Pope,David I. Israel +21 more
TL;DR: This work uses a cell-based method for identifying small-molecule ligands from DNA-encoded libraries against integral membrane protein targets to identify novel, potent, and specific inhibitors of NK3, a member of the tachykinin family of G-protein coupled receptors (GPCRs).
Journal ArticleDOI
Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library
Alexander Litovchick,Christoph E. Dumelin,Sevan Habeshian,Diana Gikunju,Marie-Aude Guié,Paolo A. Centrella,Ying Zhang,Eric A. Sigel,John W. Cuozzo,Anthony D. Keefe,Matthew A. Clark +10 more
TL;DR: A chemical ligation method for construction of DNA-encoded small-molecule libraries has been developed, and inhibitors of the enzyme soluble epoxide hydrolase are identified.
Journal ArticleDOI
Encoded Library Technology as a Source of Hits for the Discovery and Lead Optimization of a Potent and Selective Class of Bactericidal Direct Inhibitors of Mycobacterium Tuberculosis Inha.
Lourdes Encinas,Heather O’Keefe,Margarete Neu,Modesto J. Remuiñán,Amish M. Patel,Ana Guardia,Christopher P. Davie,Natalia Pérez-Macías,Hongfang Yang,Máire A. Convery,Jeffrey A. Messer,Esther Pérez-Herrán,Paolo A. Centrella,Daniel Alvarez-Gomez,Matthew A. Clark,Sophie Huss,Gary K. O’Donovan,Fatima Ortega-Muro,William McDowell,Pablo Castañeda,Christopher C. Arico-Muendel,Stane Pajk,Joaquín Rullas,Iñigo Angulo-Barturen,Emilio Alvarez-Ruiz,Alfonso Mendoza-Losana,Lluís Pagès,Julia Castro-Pichel,Ghotas Evindar +28 more
TL;DR: The hit identification, the selected strategy for potency optimization, the structure-activity relationships of a hundred analogues synthesized, and the results of the in vivo efficacy studies performed with the lead compound 65 are reported.