Zobrazeno 1 - 10
of 34
pro vyhledávání: '"William C. Ripka"'
Publikováno v:
International Journal of Peptide and Protein Research. 38:314-323
The solution structure of a gramicidin S (GS) analog containing a beta-turn mimic [BTD4-5, Lys2.2']GS has been compared to that of native GS. The linear [BTD4-5, Lys2.2']GS was synthesized by solid phase methodology and the cyclized peptide was analy
Publikováno v:
Drug Discovery Today. 6:471-477
Synthesis of combinatorial libraries by parallel synthesis, followed by high- throughput biological screening, is the new paradigm for drug discovery. Purity of these libraries is an important consideration to obtain high-quality assay data. Liquid
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:
William C Ripka
Publikováno v:
Current Opinion in Chemical Biology. 1:242-253
Thrombin is a multifunctional serine protease that plays a primary role in the pathogenic pathway of thrombosis as a consequence of its actions on the two principal components of blood clots, fibrin and activated platelets. Deficiencies in available
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:315-320
Molecular modeling and topographic considerations of the thrombin-specific sequences Boc-Asp-Pro-Arg-TS or Ac-d-Phe-Pro-Arg-TS (TS = transition state analog electrophilic center) and related scaffolds led to the design of novel P2–P4-azapeptidomime
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:331-336
Based on molecular modeling and judicious combination of the salient topographic features of the recently discovered P3-lactam derivative 1 with the P2-prolyl derivatives 2a, b, the novel thrombin inhibitor 3a was designed. Inhibitor 3a incorporates
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:
George P. Vlasuk, Raman Krishnan, Peter W. Bergum, Daniel Andrew Pearson, William C. Ripka, Terence K. Brunck, Alexander Tulinsky, Pureza Vallar
Publikováno v:
Protein Science. 5:422-433
A new class of divalent thrombin inhibitors is described that contains an alpha-keto-amide transition-state mimetic linking an active site binding group and a group that binds to the fibrinogen-binding exosite. The X-ray crystallographic structure of
Autor:
Åke Nyström, William C Ripka, Jean Marie Stassen, G Matthyssens, Jan J. Sixma, Jos Vermylen, Anne-Marie Lambeir
Publikováno v:
Thrombosis and Haemostasis. 74:646-654
SummaryPrevious investigations have indicated that interference with the initial level of the blood coagulation may lead to effective antithrombotic therapy. Recently a series of potential coagulation inhibitors derived from bovine pancreatic trypsin