Thomas P. O’Brien
Eli Lilly and Company
9 Papers
61 Citations
Thomas P. O’Brien is an academic researcher from Eli Lilly and Company. The author has contributed to research in topics: Melanocortin & Substituent. The author has an hindex of 6, co-authored 9 publications. Previous affiliations of Thomas P. O’Brien include Albany Molecular Research, Inc..
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Papers
Discovery of a β-MSH-derived MC-4R selective agonist
John P. Mayer,Hansen M. Hsiung,David B. Flora,Patrick Edwards,Dennis P. Smith,Xing-Yue Zhang,Robert Alan Gadski,Mark L. Heiman,Jeanne L. Hertel,Paul J. Emmerson,Saba Husain,Thomas P. O’Brien,Steven D. Kahl,David L. Smiley,Lianshan Zhang,Richard D. DiMarchi,Liang Zeng Yan +16 more
TL;DR: A series of novel, disulfide-constrained human beta-melanocyte stimulating hormone (beta-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor (MC-4R) binding affinity, agonist efficacy, and selectivity.
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Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.
Qing Shi,Paul L. Ornstein,Karin Briner,Timothy Ivo Richardson,Macklin Brian Arnold,Ryan Thomas Backer,Jennifer L. Buckmaster,Emily Jane Canada,Christopher W. Doecke,Larry Wayne Hertel,Nick Honigschmidt,Hansen M. Hsiung,Saba Husain,Steve L. Kuklish,Michael J. Martinelli,Jeffrey T. Mullaney,Thomas P. O’Brien,Matt R. Reinhard,Roger Ryan Rothhaar,Jikesh Arvind Shah,Zhipei Wu,Chaoyu Xie,John M. Zgombick,Matthew J. Fisher +23 more
TL;DR: Several novel di peptides and reduced dipeptides with high MC4R binding affinities and selectivity emerged from the structure-activity relationship (SAR) studies on the N-terminal residue of the 'address element'.
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Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives.
Karin Briner,Ivan Collado,Matthew J. Fisher,Cristina Garcia-Paredes,Saba Husain,Kuklish Steven Lee,Ana I. Mateo,Thomas P. O’Brien,Paul L. Ornstein,John M. Zgombick,Oscar de Frutos +10 more
TL;DR: Aliphatic carbocyclic replacement of the benzyl group of compound 1 yielded compounds with high affinity for the melanocortin-4 receptor (MC4R) as mentioned in this paper.
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Potent and selective MC-4 receptor agonists based on a novel disulfide scaffold
Liang Z. Yan,David B. Flora,Patrick Edwards,David L. Smiley,Paul J. Emmerson,Hansen M. Hsiung,Robert Alan Gadski,Jeanne L. Hertel,Mark L. Heiman,Saba Husain,Thomas P. O’Brien,Steven D. Kahl,Lianshan Zhang,Richard D. DiMarchi,John P. Mayer +14 more
TL;DR: These cyclic peptide analogs provide novel and enhanced reagents for use in the elucidation of melanocortin-4 receptor-related physiology, and may additionally find application in the treatment of obesity and related metabolic disorders.
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Privileged structure based ligands for melanocortin receptors—4,4-Disubstituted piperidine derivatives
Kuklish Steven Lee,Ryan Thomas Backer,Karin Briner,Christopher W. Doecke,Saba Husain,Jeffrey T. Mullaney,Paul L. Ornstein,John M. Zgombick,Thomas P. O’Brien,Matthew J. Fisher +9 more
TL;DR: Homologation and cyclization back to the chiral methine of compound 3 yields achiral 4,4-disubstituted piperidine privileged structures useful in the construction of melanocortin 4 receptor (MC4R) ligands.
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