Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Terence K. Brunck"'
Autor:
Susanne M Anderson, Michael G Ma, Michael I. Weinhouse, Erick A. Goldman, Vernon T Bernardino, Christopher A Roberts, Cheryl R. Cohen, Kevin Masukawa, Thomas G. Nolan, Terence K. Brunck, Susan Y. Tamura, Steven A Dixon, Annette E Bradbury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:983-987
Solid- and solution-phase synthesis of peptidomimetic inhibitors of urokinase-type plasminogen activator based on the sequence dSerAlaArg-al are described. The biological activities of these unique inhibitors are reported herein. Carbonate prodrugs w
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:
K. Hakansson, Alexander Tulinsky, J. E. Semple, Raman Krishnan, O. E. Levy, E. Zhang, Terence K. Brunck, Raghuvir K. Arni, M. S. L. Lim-Wilby
Publikováno v:
Biochemistry. 37:12094-12103
The crystal structures of three highly potent and selective low-molecular weight rigid peptidyl aldehyde inhibitors complexed with thrombin have been determined and refined to R values 0.152-0. 170 at 1.8-2.1 A resolution. Since the selectivity of tw
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
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:
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:
George P. Vlasuk, Todd A. Miller, Matthew Mark Abelman, Terence K. Brunck, Alexander Tulinsky, Marguerita S. L. Lim-Wilby, Kjell Håkansson, Peter W. Bergum
Publikováno v:
Bioorganic & Medicinal Chemistry. 3:1009-1017
The low molecular weight α-keto amide inhibitor CVS-1347, benzyl-SO2-Met(O2)-Pro-Arg(CO)((CONH)CH2)-ph4enyl, is a slow, tight binding inhibitor of α-thrombin amidolytic activity having a Ki = 1.28 × 10−10 M. A complex between human α-thrombin a
Autor:
D. C. Rowley, Yu Ge, B. M. Richard, R. J. Ardecky, Erick A. Goldman, Daniel V. Siev, Timothy D. Owens, K. Haakanson, Alexander Tulinsky, Susan Yoshiko Tamura, Nathaniel K. Minami, William C. Ripka, S. H. Carpenter, Terence K. Brunck, T. G. Nolan, Ruth F. Nutt, Theresa Ha-Uong, J. E. Semple
Publikováno v:
ChemInform. 28