Zobrazeno 1 - 10
of 24
pro vyhledávání: '"John X. He"'
Autor:
J. Ronald Rubin, Darin R. Kent, Debra R. Holland, John DiMaio, Yves St-Denis, Annette Marian Doherty, Sophie Levesque, Cuiman Cai, Peter D. Winocour, Jeremy J. Edmunds, M. Arshad Siddiqui, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Janet S. Plummer, John X. He, Alan J. Susser, Kent A. Berryman, Wayne L. Cody
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3409-3414
The synthesis and antithrombotic activity of a series of nonpeptide bicyclic thrombin inhibitors is described. We have explored the SAR with modifications to the P1 site. The introduction of arginine mimetics at the P1 site led to potent and selectiv
Autor:
John X. He, Micheline Tarazi, Patrice Preville, Annette Marian Doherty, Wayne L. Cody, M. Arshad Siddiqui
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1563-1566
Inogatran is an effective and selective pseudopeptide inhibitor of thrombin that has been shown to be efficacious in a series of in vitro and in vivo models of thrombosis. Herein, we report an efficient and convergent chemical synthesis of Inogatran
Autor:
Wayne L. Cody, John X. He, Elizabeth A. Lunney, Christine C. Humblet, Gina H. Lu, Robert L. Panek, David T. Dudley
Publikováno v:
Protein & Peptide Letters. 3:107-112
Abstract: Angiotensin II is a potent pressor agent acting through two distinct G-protein coupled receptors. The Type I (AT1) receptor is responsible for the pressor activity while the function of the Type II(AT2) receptor remains unclear. Specific mo
Autor:
Annette Marian Doherty, Barbra H. Stewart, Werness S, Wayne L. Cody, E. Tse, John X. He, Hayes Rn, E. L. Reyner
Publikováno v:
Life Sciences. 58:971-982
Endothelin (ET-1) is a 21-amino acid, vasoconstrictive peptide originally isolated from endothelial cells. It is one member of a class of potent, purportedly paracrine substances that act at receptors in multiple target organs. Antagonists to the rec
Publikováno v:
The Journal of Organic Chemistry. 60:8262-8266
Autor:
Annette Marian Doherty, E. E. Reynolds, Kathleen M. Welch, M. A. Flynn, John X. He, Wayne L. Cody
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:621-626
RES-701-1 is a cyclic peptide isolated from Streptomyces sp. RES-701 that has been reported to selectively inhibit the ETB receptor subtype with an IC50 of 10 nM. Independently, we have prepared RES-701-1 and found that it only possesses micromolar a
Autor:
Katherine E. Holub, Diana O. Omecinsky, Venkataraman Thanabal, Tomi K. Sawyer, John X. He, Michael D. Reily, Wayne L. Cody, Hyacinth Akunne, Andrea M. Sefler
Publikováno v:
Journal of Medicinal Chemistry. 38:249-257
Neurotensin (NT) is a linear tridecapeptide with a broad range of central and peripheral pharmacological effects. The C-terminal hexapeptide of NT (NT8-13) has been shown to possess similar properties to NT itself, and in fact, an analogue of NT8-13
Publikováno v:
Letters in Peptide Science. 1:25-30
An efficient and generally applicable method for the synthesis of head-to-tail cyclic peptides with HBTU (2-(1H-benzotriazol-1-yl)-1,1,3, 3-tetramethyluronium hexafluorophosphate) has been developed. The utility of this approach was exemplified with
Autor:
Gary P. Hingorani, Wayne L. Cody, John X. He, David T. Dudley, P. L. DePue, E. E. Reynolds, Annette Marian Doherty, Stephen T. Rapundalo, Kristen E. Hill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:567-572
Monocyclic fragment analogues of endothelin-1 (ET-1) were prepared to explore the importance of the bicyclic structure of ET-1 to its binding affinity and functional activity. Most of the monocyclic analogues prepared showed low micro to high nanomol
Autor:
T. Kataoka, K. Plucinska, Gina Lu, Wayne L. Cody, Christine Humblet, Yodo M, Elizabeth A. Lunney, John X. He, T C Major, Panek Rl
Publikováno v:
Journal of Medicinal Chemistry. 36:1902-1913
Angiotensin II, Asp-Arg-Val-Tyr-His-Pro-Phe, binds its receptor with a postulated turn centered at residue four. Analogs of angiotensin II which contain a disulfide bridge between the side chains of residues 3 and 5 retain significant activity consis