S. Lewis

发表

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.

M. Bock, R. Freidinger, J. Vacca, 1997, Journal of medicinal chemistry.

Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position.

J. Vacca, S. Gardell, T. Tucker, 1997, Journal of medicinal chemistry.

L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor

J. Vacca, S. Gardell, A. Mulichak, 1997 .

Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.

R. Freidinger, L. Kuo, Z. Chen, 1997, Journal of medicinal chemistry.

Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability.

Youwei Yan, J. Vacca, B. Wong, 2006, Bioorganic & medicinal chemistry.

A Kinetic Method for Characterization of Heterogenous Fibrinogen and Its Application to Fibrinogen Grand Rapids, a Congenital Dysfibrinogenemia

J. Shafer, J. Penner, D. Higgins, 1982, Thrombosis and Haemostasis.

Characterization of the kinetic pathway for liberation of fibrinopeptides during assembly of fibrin.

Paul, J. Shafer, Lewis, 1985, The Journal of biological chemistry.

Steady state kinetic parameters for the thrombin-catalyzed conversion of human fibrinogen to fibrin.

J. Shafer, D. Higgins, S. Lewis, 1983, The Journal of biological chemistry.

Reactivity of small thiolate anions and cysteine-25 in papain toward methyl methanethiosulfonate.

J. Shafer, S. Olson, D. Roberts, 1986, Biochemistry.

Identification of basic amino acid residues in thrombin essential for heparin-catalyzed inactivation by antithrombin III.

Y. Li, J. Shafer, Z. Chen, 1994, The Journal of biological chemistry.

Reconstitution of catalytically competent human zeta-thrombin by combination of zeta-thrombin residues A1-36 and B1-148 and an Escherichia coli expressed polypeptide corresponding to zeta-thrombin residues B149-259.

J. Shafer, J. R. Stone, Z. Gan, 1991, Biochemistry.

Inhibition of Thrombin by Peptides Containing Lysyl-α-Keto Carbonyl Derivatives

D. Veber, R. Nutt, S. Brady, 1995, Thrombosis and Haemostasis.

Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

M. Bock, R. Freidinger, R. Chang, 2006, Journal of medicinal chemistry.

The glycine-rich region of Escherichia coli D-serine dehydratase. Altered interactions with pyridoxal 5'-phosphate produced by substitution of aspartic acid for glycine.

J. Shafer, S. D. Lewis, M. Marceau, 1988, The Journal of biological chemistry.

D-serine dehydratase from Escherichia coli. DNA sequence and identification of catalytically inactive glycine to aspartic acid variants.

J. Shafer, E. McFall, M. Marceau, 1988, The Journal of biological chemistry.

Catalytically competent human and bovine ζ‐thrombin and chimeras generated from unfolded polypeptide chains

J. Shafer, J. Fenton, D. V. Brezniak, 1992, Protein science : a publication of the Protein Society.

Growth hormone promoted tyrosyl phosphorylation of growth hormone receptors in murine 3T3-F442A fibroblasts and adipocytes.

J. Shafer, J. Schwartz, C. Carter-Su, 1988, Biochemistry.

Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis.

S. Brady, J. Vacca, T. Tucker, 1998, Journal of medicinal chemistry.

Identification and SAR for a selective, nonpeptidyl thrombin inhibitor.

B. T. Phillips, W. M. Sanders, J. Vacca, 1998, Bioorganic & medicinal chemistry letters.

Quantifying thrombin-catalyzed release of fibrinopeptides from fibrinogen using high-performance liquid chromatography.

J. Shafer, A. S. Ng, S. Lewis, 1993, Methods in enzymology.

Potentiometric determination of ionizations at the active site of papain.

J. Shafer, S. D. Lewis, F. A. Johnson, 1976, Biochemistry.

Perturbations in the free energy and enthalpy of ionization of histidine-159 at the active site of papain as determined by fluorescence spectroscopy.

J. Shafer, F. A. Johnson, S. Lewis, 1981, Biochemistry.

Determination of a low pK for histidine-159 in the S-methylthio derivative of papain by proton nuclear magnetic resonance spectroscopy.

J. Shafer, F. A. Johnson, S. Lewis, 1981, Biochemistry.

Effect of cysteine-25 on the ionization of histidine-159 in papain as determined by proton nuclear magnetic resonance spectroscopy. Evidence for a his-159--Cys-25 ion pair and its possible role in catalysis.

J. Shafer, S. D. Lewis, F. A. Johnson, 1981, Biochemistry.

A two-step procedure for purification of papain from extract of papaya latex.

J. Shafer, D. E. Burke, S. Lewis, 1974, Archives of biochemistry and biophysics.

A thrombin assay based upon the release of fibrinopeptide A from fibrinogen: definition of a new thrombin unit.

J. Shafer, S. Lewis, 1984, Thrombosis research.

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Daniel R McMasters, James C Barrow, W. M. Sanders, 2003, Journal of medicinal chemistry.

9-hydroxyazafluorenes and their use in thrombin inhibitors.

Youwei Yan, B. Wong, P. Nantermet, 2005, Journal of medicinal chemistry.

Contribution of a conserved arginine near the active site of Escherichia coli D-serine dehydratase to cofactor affinity and catalytic activity.

J. Shafer, S. D. Lewis, M. Marceau, 1989, Journal of Biological Chemistry.

Regulation of formation of factor XIIIa by its fibrin substrates.

L. Lorand, J. Shafer, S. D. Lewis, 1985, Biochemistry.

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

Lawrence C Kuo, Daniel R McMasters, James C Barrow, 2003, Bioorganic & medicinal chemistry letters.

Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.

J. Vacca, J. Shafer, Z. Chen, 1998, Journal of medicinal chemistry.

C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.

J. Vacca, S. Gardell, S. D. Lewis, 1998, Bioorganic & Medicinal Chemistry Letters.

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

J. Vacca, J. Shafer, Z. Chen, 1998, Bioorganic & medicinal chemistry letters.

Kinetic parameters for the binding of p-nitrophenyl α-d-mannopyranoside to concanavalin A

I. Goldstein, J. Shafer, S. D. Lewis, 1976 .

Reaction pathway for inhibition of blood coagulation factor Xa by tick anticoagulant peptide.

J. Shafer, S. D. Lewis, S. Mao, 1992, Biochemistry.

Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.

Lawrence C Kuo, Daniel R McMasters, James C Barrow, 2004, Journal of medicinal chemistry.

Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.

Youwei Yan, L. Kuo, J. Vacca, 2003, Bioorganic & medicinal chemistry letters.

Promotion of thrombin-catalyzed activation of factor XIII by fibrinogen.

L. Lorand, J. Shafer, T. Janus, 1983, Biochemistry.

Crystal structure of human alpha-thrombin complexed with hirugen and p-amidinophenylpyruvate at 1.6 A resolution.

Y Li, Z. Chen, Y. Li, 1995, Archives of biochemistry and biophysics.

Determination of interactive thiol ionizations in bovine serum albumin, glutathione, and other thiols by potentiometric difference titration.

J. Shafer, S. D. Lewis, D. Misra, 1980, Biochemistry.

Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.

S. Brady, J. Vacca, S. Gardell, 1998, Journal of medicinal chemistry.

Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor.

W. M. Sanders, R. Freidinger, S. Gardell, 1997 .

Selective Inhibition of Factor Xa in the Prothrombinase Complex by the Carboxyl-terminal Domain of Antistasin*

V. Garsky, J. Shafer, J. Joyce, 1998, The Journal of Biological Chemistry.

Inhibition of thrombin and other trypsin-like serine proteinases by cyclotheonamide A.

J. Shafer, J. Baldwin, N. Fusetani, 1993, Thrombosis research.

3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors.

Youwei Yan, S. D. Lewis, E. A. Lyle, 2003, Bioorganic & medicinal chemistry letters.

Dependence of the catalytic activity of papain on the ionization of two acidic groups.

J. Shafer, F. A. Johnson, A. K. Ohno, 1978, The Journal of biological chemistry.

Assessment of Thrombin Inhibitor Efficacy in a Novel Rabbit Model of Simultaneous Arterial and Venous Thrombosis

S. Gardell, S. D. Lewis, J. Lynch, 1998, Thrombosis and Haemostasis.

Conversion of exposed aspartyl and glutamyl residues in proteins to asparaginyl and glutaminyl residues.

J. Shafer, S. Lewis, 1973, Biochimica et biophysica acta.

Effects of proflavine on papain's catalytic activity. A proflavine-mediated decrease in K M .

J. Shafer, S. D. Lewis, E. Maggio, 1973, Biochemistry.

Ionization of a nitrophenol-containing reporter group at the active site of papain.

J. Shafer, S. D. Lewis, S. Lewis, 1974, Biochemistry.

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.

Youwei Yan, J. Barrow, L. Kuo, 2003, Bioorganic & medicinal chemistry letters.

Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy.

J. Vacca, S. Gardell, T. Tucker, 1997, Journal of medicinal chemistry.

Design, syntheses, and activity of new 3-[(sulfonylaryl)-amino]-1,4-benzodiazepin-2-one derivatives as α-thrombin inhibitors

M. Murcko, J. Baldwin, S. D. Lewis, 1998 .

Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors.

C. Coburn, J. Vacca, S. D. Lewis, 2000, Bioorganic & medicinal chemistry letters.

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.

S. Brady, J. Vacca, S. Gardell, 1998, Journal of medicinal chemistry.