T. Tomaszek

发表

A symmetric inhibitor binds HIV-1 protease asymmetrically.

A M Hassell, R. DesJarlais, J. Boehm, 1993, Biochemistry.

Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere.

R. DesJarlais, K. Murthy, E. Winborne, 1994, Journal of medicinal chemistry.

A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys.

D. Veber, S. Kumar, D. Yamashita, 2007, Bone.

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

R. DesJarlais, Y. Ru, M. Head, 1998, Journal of medicinal chemistry.

Interaction of azide with beef heart mitochondrial ATPase.

S. Schuster, T. Tomaszek, S. G. Daggett, 1985, Archives of biochemistry and biophysics.

Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.

Neysa Nevins, D. Yamashita, T. Tomaszek, 2011, Bioorganic & medicinal chemistry letters.

Development and Characterization of a Human In Vitro Resorption Assay: Demonstration of Utility Using Novel Antiresorptive Agents

M. Lark, I. James, T. Tomaszek, 1999, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

Potent and Selective Cathepsin L Inhibitors Do Not Inhibit Human Osteoclast Resorption in Vitro *

Y. Ru, D. Veber, D. Yamashita, 2001, The Journal of Biological Chemistry.

Peptide Aldehyde Inhibitors of Cathepsin K Inhibit Bone Resorption Both In Vitro and In Vivo

D. Veber, A. Badger, I. James, 1997, Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.

Structure and Design of Potent and Selective Cathepsin K Inhibitors

S. Carr, R. DesJarlais, Baoguang Zhao, 1997 .

Proteolytic Activity of Human Osteoclast Cathepsin K

D. Mcnulty, B. Amegadzie, T. Tomaszek, 1996, The Journal of Biological Chemistry.

Benzodioxocin-3-ones and N-acyl-3-amino-3-buten-2-ones: novel classes of cathepsin K cysteine protease inhibitors.

D. Veber, M. Hemling, D. Yamashita, 2004, The journal of peptide research : official journal of the American Peptide Society.

Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.

R. DesJarlais, D. Veber, K. Duffy, 1999, Bioorganic & medicinal chemistry letters.

Structure-based design of non-peptide, carbohydrazide-based cathepsin K inhibitors.

R. DesJarlais, D. Veber, D. Tew, 1999, Bioorganic & medicinal chemistry.

Steroidal acetylenes: Mechanism-based inactivators of lanosterol 14α-demethylase

J. Adams, T. Gallagher, T. Tomaszek, 1991 .

A novel, convenient assay of lanosterol 14α-demethylase

J. Adams, T. Tomaszek, B. Metcalf, 1989 .

Identification of a loop outside the active site cavity of the human immunodeficiency virus proteases which confers inhibitor specificity.

C. Debouck, T. Tomaszek, S. Thompson, 1997, Biochemistry.

Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.

D. Holt, S. Semus, Baochau Le, 2017, Bioorganic & medicinal chemistry letters.

Hydroxyethylene isostere inhibitors of human immunodeficiency virus-1 protease: structure-activity analysis using enzyme kinetics, X-ray crystallography, and infected T-cell assays.

A M Hassell, M. Minnich, D. Lambert, 1992, Biochemistry.

Synthesis and activity of an HIV-1 Protease inhibitor containing a contiguous (E)-olefin-hydroxyethylene peptide mimetic

R. Keenan, T. Tomaszek, D. F. Eppley, 1995 .

Inhibition of human immunodeficiency virus-1 protease by a C2-symmetric phosphinate. Synthesis and crystallographic analysis.

R. DesJarlais, K. Murthy, E. Winborne, 1993, Biochemistry.

Inhibition of HIV-1 protease in infected T-lymphocytes by synthetic peptide analogues

Brian W. Metcalf, Michael L. Moore, C. Debouck, 1990, Nature.

Inactivation of HIV-1 protease by a tripeptidyl epoxide

T. Meek, T. Tomaszek, S. Grant, 1992 .

4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.

Guang Yang, Keith W Ward, D. Veber, 2005, Journal of medicinal chemistry.

Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1′-P2′ amide bond isostere

R. Lum, M. Darcy, D. Lambert, 1994 .

Inhibition of human immunodeficiency virus 1 protease in vitro: rational design of substrate analogue inhibitors.

C. Debouck, J. Strickler, T. Meek, 1989, Proceedings of the National Academy of Sciences of the United States of America.

A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate.

T. Tomaszek, J. Callahan, W. Huffman, 1993, Journal of medicinal chemistry.

Dependence of the activity of beef heart mitochondrial adenosinetriphosphatase on the properties of the catalytic metal ion.

S. Schuster, T. Tomaszek, J. Urbauer, 1987, Biochemistry.

Chromophoric peptide substrates for the spectrophotometric assay of HIV-1 protease.

T. Meek, T. Tomaszek, M. Moore, 1990, Biochemical and biophysical research communications.

Azepanone-based inhibitors of human and rat cathepsin K.

Y. Ru, D. Veber, K. Ward, 2001, Journal of medicinal chemistry.

Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.

Baoguang Zhao, M. Head, D. Veber, 2006, Journal of medicinal chemistry.

Cyclic ketone inhibitors of the cysteine protease cathepsin K.

Y. Ru, D. Veber, M. Hemling, 2001, Journal of medicinal chemistry.

Human immunodeficiency virus-1 protease. 2. Use of pH rate studies and solvent kinetic isotope effects to elucidate details of chemical mechanism.

T. Meek, T. Tomaszek, T D Meek, 1991, Biochemistry.

Use of X-Ray Co-Crystal Structures and Molecular Modeling to Design Potent and Selective Non-Peptide Inhibitors of Cathepsin K

Renee L. DesJarlais, Cheryl A. Janson, R. DesJarlais, 1998 .

Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.

D. Veber, D. Tew, D. Yamashita, 1999, Journal of combinatorial chemistry.

Design of potent and selective human cathepsin K inhibitors that span the active site.

J G Gleason, S. Carr, R. DesJarlais, 1997, Proceedings of the National Academy of Sciences of the United States of America.

Purification and biochemical characterization of recombinant simian immunodeficiency virus protease and comparison to human immunodeficiency virus type 1 protease.

M. Minnich, J. Culp, C. Debouck, 1991, Biochemistry.

Human immunodeficiency virus-1 protease. 1. Initial velocity studies and kinetic characterization of reaction intermediates by 18O isotope exchange.

S. Carr, M. Minnich, J. Culp, 1991, Biochemistry.

Proteolysis of an active site peptide of lactate dehydrogenase by human immunodeficiency virus type 1 protease.

C. Debouck, I. Brooks, J. Strickler, 1992, Biochemistry.

2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.

T. Tomaszek, K. Wells-Knecht, J. Lenhard, 2005, Bioorganic & medicinal chemistry letters.

Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.

R. DesJarlais, D. Veber, S. Abdel-Meguid, 1999, Journal of medicinal chemistry.

Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.

R. DesJarlais, D. Veber, S. Abdel-Meguid, 1998, Journal of medicinal chemistry.

Potent and Selective Nonpeptide Inhibitors of Caspases 3 and 7 Inhibit Apoptosis and Maintain Cell Functionality*

J. Adams, C. Debouck, M. Head, 2000, The Journal of Biological Chemistry.

An orally bioavailable HIV-1 protease inhibitor containing an imidazole-derived peptide bond replacement: crystallographic and pharmacokinetic analysis.

R. DesJarlais, Baoguang Zhao, K. Murthy, 1994, Biochemistry.

Peptidyl Epoxides as Potent, Active Site-Directed Irreversible Inhibitors of HIV-1 Protease,

T. Tomaszek, S. Fakhoury, M. Moore, 1992 .

Azepanone-based inhibitors of human cathepsin L.

Y. Ru, M. Head, D. Veber, 2005, Journal of medicinal chemistry.