L. Kuo

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Mutational Anatomy of an HIV-1 Protease Variant Conferring Cross-resistance to Protease Inhibitors in Clinical Trials

H. B. Schock, V. Garsky, L. Kuo, 1996, The Journal of Biological Chemistry.

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Alison R. Gregro, Amy S. Espeseth, Min Xu, 2004, Journal of medicinal chemistry.

Crystal structure at 1.9-A resolution of human immunodeficiency virus (HIV) II protease complexed with L-735,524, an orally bioavailable inhibitor of the HIV proteases.

L. Kuo, P. Darke, Z. Chen, 1996, The Journal of biological chemistry.

Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).

Min Xu, Qian Huang, D. Hazuda, 2006, Journal of medicinal chemistry.

Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution

J. Clemente, R. DesJarlais, Robyn Miller, 2011, Protein science : a publication of the Protein Society.

A combinatorial library of indinavir analogues and its in vitro and in vivo studies.

Yuan Cheng, Xin Xu, Lawrence C Kuo, 2002, Bioorganic & medicinal chemistry letters.

Rapid X-ray diffraction analysis of HIV-1 protease-inhibitor complexes: inhibitor exchange in single crystals of the bound enzyme.

L. Kuo, S. Munshi, Z. Chen, 1998, Acta crystallographica. Section D, Biological crystallography.

Ligand-induced isomerizations of Escherichia coli ornithine transcarbamoylase. An ultraviolet difference analysis.

L. Kuo, A. W. Miller, 1990, The Journal of biological chemistry.

Substrate specificity and protonation state of Escherichia coli ornithine transcarbamoylase as determined by pH studies. Binding of carbamoyl phosphate.

L. Kuo, I. Zambidis, 1990, The Journal of biological chemistry.

Zn2+ regulation of ornithine transcarbamoylase. II. Metal binding site.

L. Kuo, W. Herzberg, C. Caron, 1990, Journal of molecular biology.

Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors.

Michael Reilly, Laura Sepp-Lorenzino, Weikang Tao, 2006, Bioorganic & medicinal chemistry letters.

Sensitivity of HIV-1 reverse transcriptase and its mutants to inhibition by azidothymidine triphosphate.

L. Kuo, J. Shafer, D. Olsen, 1994, Biochemistry.

Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.

Youwei Yan, P. Coleman, L. Kuo, 2007, Bioorganic & medicinal chemistry letters.

Determination of the zero-field splitting constants of high-spin metalloproteins by a continuous-wave microwave saturation technique

L. Kuo, M. B. Yim, M. W. Makinen, 1982 .

Biochemical and structural characterization of a novel class of inhibitors of the type 1 insulin-like growth factor and insulin receptor kinases.

S. Stirdivant, L. Kuo, P. Darke, 2005, Biochemistry.

Active Human Cytomegalovirus Protease Is a Dimer (*)

L. Kuo, P. Darke, D. Hall, 1996, The Journal of Biological Chemistry.

Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.

John D. Schreier, Youwei Yan, P. Coleman, 2007, Bioorganic & medicinal chemistry letters.

Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.

Youwei Yan, P. Coleman, Christopher D. Cox, 2006, Bioorganic & medicinal chemistry letters.

Generation of allosteric enzymes from nonallosteric forms.

L. Kuo, 1991, Methods in enzymology.

Substrate specificity and protonation state of ornithine transcarbamoylase as determined by pH studies.

W. Lipscomb, L. Kuo, W. Herzberg, 1985, Biochemistry.

Inhibition of HIV-1 reverse transcriptase by pyridinone derivatives. Potency, binding characteristics, and effect of template sequence.

L. Kuo, J. Condra, D. Graham, 1993, The Journal of biological chemistry.

Purification of active herpes simplex virus-1 protease expressed in Escherichia coli.

L. Kuo, P. Darke, E. Chen, 1994, The Journal of biological chemistry.

Zn2+ regulation of ornithine transcarbamoylase. I. Mechanism of action.

L. Kuo, A. W. Miller, S. Lee, 1990, Journal of molecular biology.

Screening and Characterization of Human Monoglyceride Lipase Active Site Inhibitors Using Orthogonal Binding and Functional Assays

J. Clemente, L. Kuo, D. Maguire, 2012, Journal of biomolecular screening.

Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 A resolution.

L. Kuo, P. Darke, S. Munshi, 2003, Acta crystallographica. Section D, Biological crystallography.

Inhibition of Hepatitis C Virus NS2/3 Processing by NS4A Peptides

L. Kuo, P. Darke, L. Waxman, 1999, The Journal of Biological Chemistry.

Solution oligomerization of the rev protein of HIV-1: implications for function.

L. Kuo, J. Shafer, J. Cole, 1993, Biochemistry.

Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.

L. Kuo, W. Schleif, L. Gabryelski, 2002, Bioorganic & medicinal chemistry letters.

Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.

L. Kuo, W. Schleif, L. Gabryelski, 2000, Bioorganic & medicinal chemistry letters.

Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.

Youwei Yan, L. Kuo, S. D. Lewis, 2003, Bioorganic & medicinal chemistry letters.

Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization.

Lawrence C Kuo, Berta Strulovici, Daniel R McMasters, 2005, Bioorganic & medicinal chemistry letters.

P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.

Youwei Yan, L. Kuo, J. Vacca, 2005, Bioorganic & medicinal chemistry letters.

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.

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

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.

Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.

Lawrence C Kuo, Daniel R McMasters, Youwei Yan, 2008, Bioorganic & medicinal chemistry letters.

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.

Small, Low Nanomolar, Noncovalent Thrombin Inhibitors Lacking a Group to Fill the “Distal Binding Pocket”.

Youwei Yan, L. Kuo, S. D. Lewis, 2003 .

HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.

Jiunn H. Lin, L. Kuo, W. Schleif, 2002, Bioorganic & medicinal chemistry letters.

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.

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

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

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.

D. Hazuda, A. Simon, G. McGaughey, 2007, Bioorganic & medicinal chemistry letters.

Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.

W. F. Hoffman, Youwei Yan, L. Kuo, 2006, Bioorganic & medicinal chemistry letters.

Catalytic role of the metal ion of carboxypeptidase A in ester hydrolysis.

L. Kuo, M. W. Makinen, S. Jaffer, 1979, The Journal of biological chemistry.

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.

Jiunn H. Lin, L. Kuo, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.

Louis-David Cantin, Lawrence C Kuo, Ralph Hirschmann, 2003, Journal of medicinal chemistry.

Inhibition of a mitotic motor protein: where, how, and conformational consequences.

Lawrence C Kuo, Youwei Yan, L. Kuo, 2004, Journal of molecular biology.

Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.

Paul J Coleman, Youwei Yan, P. Coleman, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.

Youwei Yan, S. Stirdivant, L. Kuo, 2007, Bioorganic & medicinal chemistry letters.

Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.

Lawrence C Kuo, Laura Sepp-Lorenzino, Weikang Tao, 2007, Bioorganic & medicinal chemistry letters.

Inhibition of Hepatitis C Virus RNA Replication by 2′-Modified Nucleoside Analogs*

Lawrence C Kuo, Giovanni Migliaccio, L. Kuo, 2003, The Journal of Biological Chemistry.

3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.

Lawrence C Kuo, Laura Sepp-Lorenzino, Weikang Tao, 2006, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.

L. Kuo, W. Schleif, S. Munshi, 2006, Bioorganic & medicinal chemistry letters.

The catalytic action of Zn2+-metalloenzymes requires a penta-coordinate metal-OH2 complex

L. Kuo, W. Maret, M. B. Yim, 1984 .

Catalytic conformation of carboxypeptidase A. The structure of a true reaction intermediate stabilized at subzero temperatures.

L. Kuo, M. W. Makinen, J. M. Fukuyama, 1983, Journal of molecular biology.

Dissociation and association of the HIV-1 protease dimer subunits: equilibria and rates.

L. Kuo, P. Darke, D. Hall, 1994, Biochemistry.

Synthesis of chromophoric, spin label enzyme substrates useful for cryoenzymology.

L. Kuo, M. W. Makinen, T. Koch, 1979, The Journal of biological chemistry.

Cleavage of Oligoribonucleotides by the 2′,5′-Oligoadenylate- dependent Ribonuclease L (*)

L. Kuo, E. Chen, J. Gehman, 1996, The Journal of Biological Chemistry.

Stoichiometry of 2′,5′-Oligoadenylate-induced Dimerization of Ribonuclease L

L. Kuo, J. Cole, S. Carroll, 1996, The Journal of Biological Chemistry.

Activation of RNase L by 2′,5′-Oligoadenylates

L. Kuo, J. Cole, J. Gehman, 1997, The Journal of Biological Chemistry.

Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.

E A Emini, L. Kuo, P. Darke, 2000, Journal of medicinal chemistry.

Effect of template secondary structure on the inhibition of HIV-1 reverse transcriptase by a pyridinone non-nucleoside inhibitor.

L. Kuo, J. Shafer, D. Olsen, 1994, Nucleic acids research.

X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform.

D. Hazuda, Youwei Yan, L. Kuo, 2000, Journal of molecular biology.

Crystal Structure of the Apo, Unactivated Insulin-like Growth Factor-1 Receptor Kinase

S. Stirdivant, L. Kuo, P. Darke, 2002, The Journal of Biological Chemistry.

Host cell factor requirement for hepatitis C virus enzyme maturation

L. Kuo, P. Darke, B. Pollok, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Activity and dimerization of human immunodeficiency virus protease as a function of solvent composition and enzyme concentration.

L. Kuo, P. Darke, J. Zugay, 1992, The Journal of biological chemistry.

A general procedure for the purification of human beta-secretase expressed in Escherichia coli.

L. Kuo, P. Darke, S. Munshi, 2004, Protein expression and purification.

Non-active Site Changes Elicit Broad-based Cross-resistance of the HIV-1 Protease to Inhibitors*

H. B. Schock, L. Kuo, D. Olsen, 1999, The Journal of Biological Chemistry.

Elucidation of Basic Mechanistic and Kinetic Properties of Influenza Endonuclease Using Chemically Synthesized RNAs (*)

R. Dempski, L. Kuo, P. Darke, 1996, The Journal of Biological Chemistry.

Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors.

A. Gibbs, L. Kuo, Z. Sui, 2011, Bioorganic & medicinal chemistry letters.

SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.

Adam J. Simon, Georgia B. McGaughey, Philippe G. Nantermet, 2010, Bioorganic & medicinal chemistry letters.

Three-dimensional Structure of a Mutant HIV-1 Protease Displaying Cross-resistance to All Protease Inhibitors in Clinical Trials (*)

H. B. Schock, L. Kuo, E. Chen, 1995, The Journal of Biological Chemistry.

Triggering of allostery in an enzyme by a point mutation: ornithine transcarbamoylase.

L. Kuo, I. Zambidis, C. Caron, 1989, Science.

Failure of AZT: A molecular perspective

D. Hazuda, L. Kuo, 1997, Nature Medicine.

Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.

Youwei Yan, P. Coleman, Christopher D. Cox, 2008, Journal of medicinal chemistry.

Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation

K. Rhodes, J. Spurlino, L. Kuo, 2017, The Journal of Biological Chemistry.

Structural basis for elastolytic substrate specificity in rodent alpha-chymases.

J. Spurlino, X. Yao, L. Kuo, 2008, The Journal of biological chemistry.

Structural Basis for Elastolytic Substrate Specificity in Rodent α-Chymases*

J. Spurlino, X. Yao, L. Kuo, 2008, Journal of Biological Chemistry.

Allosteric cofactor-mediated enzyme cooperativity: a theoretical treatment.

L. Kuo, 1983, Proceedings of the National Academy of Sciences of the United States of America.

Zn(II)-induced cooperativity of Escherichia coli ornithine transcarbamoylase.

W. Lipscomb, L. Kuo, E. Kantrowitz, 1982, Proceedings of the National Academy of Sciences of the United States of America.

Site-directed mutagenesis of Escherichia coli ornithine transcarbamoylase: role of arginine-57 in substrate binding and catalysis.

L. Kuo, A. W. Miller, S. Lee, 1988, Biochemistry.

Polarized single-crystal absorption spectra of cobalt2+-carboxypeptidase A

W. Lipscomb, L. Kuo, M. W. Makinen, 1986 .

Utilization of conformational flexibility in enzyme action-linkage between binding, isomerization, and catalysis.

L. Kuo, J. Goldsmith, 1993, The Journal of biological chemistry.

Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.

M Katharine Holloway, Gergely M Makara, Zhongguo Chen, 2004, Journal of medicinal chemistry.

A Collaborative Screening Program for the Discovery of Inhibitors of HCV NS2/3 cis-Cleaving Protease Activity

L. Kuo, P. Darke, B. Pollok, 2002, Journal of biomolecular screening.

An alternate binding site for the P1-P3 group of a class of potent HIV-1 protease inhibitors as a result of concerted structural change in the 80s loop of the protease.

H. B. Schock, L. Kuo, S. Munshi, 2000, Acta crystallographica. Section D, Biological crystallography.

Fragment-based drug design : tools, practical approaches, and examples

L. Kuo, Lawrence C. Kuo, 2011 .

Activation of RNase L by 2′,5′-Oligoadenylates

L. Kuo, J. Cole, S. Carroll, 1997, The Journal of Biological Chemistry.

Protein expression plasmids produced rapidly: streamlining cloning protocols and robotic handling.

Lawrence C Kuo, Michael Lenard, L. Kuo, 2005, Assay and drug development technologies.

X-ray diffraction analysis on single crystals of recombinant Escherichia coli ornithine transcarbamoylase.

L. Kuo, B. Seaton, 1989, The Journal of biological chemistry.

Ground term splitting of high-spin cobalt(2+) ion as a probe of coordination structure. 1. Dependence of the splitting on coordination geometry

L. Kuo, M. B. Yim, M. W. Makinen, 1985 .

Ground term splitting of high-spin cobalt(2+) ion as a probe of coordination structure. 2. The ligand environment of the active site metal ion of carboxypeptidase A in ester hydrolysis

L. Kuo, M. W. Makinen, 1985 .

Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain.

D. Hazuda, L. Kuo, Z. Chen, 1999, Acta crystallographica. Section D, Biological crystallography.

Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation

K. Rhodes, J. Spurlino, L. Kuo, 2017, The Journal of Biological Chemistry.