Zobrazeno 1 - 10
of 89
pro vyhledávání: '"RUTH F. NUTT"'
Publikováno v:
International Journal of Peptide and Protein Research. 42:194-203
The endothelin family of polypeptides are known to exert potent physiological effects which include cardiovascular regulation. The solution conformation and dynamics of c(D-Trp-D-Cys(SO3-Na+)-Pro-D-Val-Leu), a potent endothelin-A receptor-selective a
Autor:
Paul S. Anderson, Steven M. Pitzenberger, Ruth F. Nutt, Stephen F. Brady, C. D. Colton, J. T. Sisko, M.J. Bogusky, A.M. Naylor, Daniel F. Veber
Publikováno v:
International Journal of Peptide and Protein Research. 39:63-76
The tripeptide sequence arginine-glycine-aspartic acid (RGD) has been shown to be the key recognition segment in numerous cell adhesion proteins. The solution conformation and dynamics in DMSO-d6 of the cyclic pentapeptides, Ac-Cys-Arg-Gly-Asp-Cys-OH
Publikováno v:
Tetrahedron Letters. 42:6271-6274
The Passerini reaction between suitably protected alaninal, leucine isonitrile, and ornithine components delivered adducts 10a , b in high yield. Orthogonal N -deprotection of 10a led, via a smooth O - to N -acyl migration, to 11 , which constitutes
Autor:
Cheryl R. Cohen, Susan Y. Tamura, Terence K. Brunck, John Reiner, Odile E. Levy, Ruth F. Nutt, Erick A. Goldman, Jonathan Z. Ho, J. Edward Semple, Peter W. Bergum, Theresa H. Uong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:745-749
A novel series of rigid P3-guanylpiperidine peptide mimics 3-14 was designed as potential factor Xa and prothrombinase inhibitors. Incorporation into a P2-gly-P1-argininal motif led to highly potent and selective inhibitors. The synthesis and biologi
Autor:
Matthew A. Abelman, Erick A. Goldman, J. Edward Semple, Theresa Ha-Uong, Margeurita S. Lim-Wilby, Terence K. Brunck, Susan Y. Tamura, John Reiner, Ruth F. Nutt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:895-900
A novel scaffold for P4-P2 dipeptide mimics containing a rigid pyridone spacer was designed based on a virtual library strategy. Several selected nonpeptidic 4-aralkyl or 4-alkylpyridones incorporating a P1-argininal sequence were prepared. The model
Autor:
Terence K. Brunck, Ruth F. Nutt, William C. Ripka, J. Edward Semple, Nathaniel K. Minami, Susan Y. Tamura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2421-2426
SAR and molecular modeling investigations on the potent and selective thrombin inhibitor 1b (CVS 1578) and related serine protease inhibitors led to the design of series 2a–g, featuring quaternary α-amino-α-benzyl-lactam scaffolds that serve as n
Autor:
Robert J. Ardecky, J. Edward Semple, Yu Ge, William C. Ripka, Steven H. Carpenter, Michael I. Weinhouse, Pamela Leon, Brian M. Shamblin, Susan Y. Tamura, Ruth F. Nutt
Publikováno v:
Tetrahedron Letters. 37:4109-4112
A general method for the synthesis of peptidyl argininals was developed which utilizes the novel building block Ng-nitro-L-argininal ethyl aminal·HCl. The final aldehyde structure is generated by hydrolysis of the peptidic aminal moiety and can be a
Autor:
Dong-Mei Feng, Daniel F. Veber, Thomas M. Connolly, Mei-Jy Tang, Cindra L. Condra, Ruth F. Nutt
Publikováno v:
Journal of Medicinal Chemistry. 38:4125-4130
The N-terminal thrombin receptor peptide H-Ser-Phe-Leu-Leu-Arg-Asn-Pro-Asn-Asp-Lys-Tyr-Glu-Pro-Phe-OH (1) fully activates the thrombin receptor with an EC50 of 10 microM. Structural features in the tetradecapeptide which are responsible for receptor
Autor:
K.J. Stauffer, Jules A. Shafer, Stephen F. Brady, S. D. Lewis, John T. Sisko, D. F. Veber, Howard Qiu, Assunta S. Ng, Ruth F. Nutt, Michael J. Bogusky, Christiana D. Colton
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:1063-1078
We report structure-activity investigations in a series of tripeptide amide inhibitors of thrombin, and the development of a series of highly potent active site directed α-keto carbonyl inhibitors having the side chain of lysine at P1. Compounds of
Autor:
Sidney D Lewis, Assunta S Ng, Elizabeth A Lyle, Michael J Mellott, Sandra D Appleby, Stephen F Brady, Kenneth J Stauffer, John T Sisko, Shi-Shan Mao, Daniel F Veber, Ruth F Nutt, Joseph J Lynch, Jacquelynn J Cook, Stephen J Gardll, Jules A Shafer
Publikováno v:
Thrombosis and Haemostasis. 74:1107-1112
SummarySeveral H-N-Me-D-Phe-Pro-Lysyl-α-keto carbonyl derivatives were shown to be potent thrombin inhibitors (Ki 0.2 to 27 nM). The inhibitory potencies of these compounds toward tissue plasminogen activator, plasmin and factor Xa were minimal; how