W. Kazmierski

发表

A new type of synthetic peptide library for identifying ligand-binding activity

K. Lam, V. Hruby, E. Hersh, 1992, Nature.

Discovery of next generation inhibitors of HIV protease.

W. Kazmierski, V. Samano, A. Spaltenstein, 2005, Current topics in medicinal chemistry.

Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors.

Terry Kenakin, Hanbiao Yang, T. Kenakin, 2003, Bioorganic & medicinal chemistry.

Biological and Structural Characterization of Rotamers of C-C Chemokine Receptor Type 5 (CCR5) Inhibitor GSK214096.

W. Kazmierski, E. Stewart, R. Ferris, 2014, ACS medicinal chemistry letters.

Chapter 19 Small Molecule CCR5 and CXCR4-Based Viral Entry Inhibitors for Anti-HIV Therapy Currently in Development

S. Piscitelli, W. Kazmierski, K. Gudmundsson, 2007 .

CCR5 chemokine receptors: gatekeepers of HIV-1 infection.

T. Kenakin, W. Kazmierski, L. Boone, 2002, Current drug targets. Infectious disorders.

Pharmacological disruption of hepatitis C NS5A protein intra- and intermolecular conformations.

R. Hamatake, R. Striker, W. Kazmierski, 2014, Journal of General Virology.

Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors

V. Hruby, K. Gulya, H. Yamamura, 1986 .

Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.

R. Hamatake, Suoming Zhang, S. Baker, 2012, Journal of medicinal chemistry.

Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease.

Z. Ni, Suoming Zhang, S. Baker, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease.

Z. Ni, P. Rowland, S. Baker, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease.

Z. Ni, Suoming Zhang, S. Baker, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.

E. Furfine, W. Kazmierski, A. Spaltenstein, 2004, Bioorganic & medicinal chemistry letters.

Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease.

R. Hamatake, Suoming Zhang, S. Baker, 2012, Bioorganic & medicinal chemistry letters.

Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.

H. Mitsuya, K. Maeda, W. Kazmierski, 2011, Bioorganic & medicinal chemistry letters.

Conformation of two somatostatin analogues in aqueous solution. Study by NMR methods and circular dichroism.

V. Hruby, W. Kazmierski, D. Tourwé, 1989, European journal of biochemistry.

A New Experimental Method to Determine the Mutual Orientation of Helices in Coiled‐Coil Proteins: Structural Information about the Dimeric Interface of cJun, cFos, GCN4, and gp41

W. Kazmierski, A. Aulabaugh, J. Mcdermed, 1996 .

Cyclic somatostatin analogues as potent antagonists at μ-, but not δ- and κ-opioid receptors mediating presynaptic inhibition of neurotransmitter release in the brain

V. Hruby, G. Wardeh, W. Kazmierski, 1991 .

Structural characteristics of two highly selective opioid peptides

V. Hruby, R. Knapp, H. Yamamura, 1989, BioEssays : news and reviews in molecular, cellular and developmental biology.

Proton n.m.r. investigation of conformational influence of penicillamine residues on the disulfide ring system of opioid receptor selective somatostatin derivatives.

V. Hruby, W. Kazmierski, D. Tourwé, 2009, International journal of peptide and protein research.

Antagonist activity of the cyclic somatostatin analogue CTP at μ- but not δ- and κ;;-opioid receptors involved in presynaptic inhibition of neurotransmitter release

V. Hruby, G. Wardeh, W. Kazmierski, 1988 .

Effects of a novel opioid peptide antagonist on rat bladder motility in vivo

V. Hruby, F. Porreca, W. Kazmierski, 1987, Peptides.

Design and Synthesis of Conformationally Constrained Somatostatin Analogues with High Potency and Specificity for μ Opioid Receptors.

V. Hruby, K. Gulya, H. Yamamura, 1987 .

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.

Brian A. Chauder, W. Kazmierski, D. K. Jones-Hertzog, 2008, Journal of medicinal chemistry.

Solid state conformation of constrained Somatostatin analogs with high potency and specificity for the μ-opioid receptor

J. Deschamps, C. George, J. Flippen-Anderson, 2002 .

764 IN VITRO PROFILING OF GSK2336805, A POTENT AND SELECTIVE INHIBITOR OF HCV NS5A

R. Hamatake, J. Vamathevan, W. Kazmierski, 2011 .

HCV Inhibition Mediated Through the Nonstructural Protein 5A (NS5A) Replication Complex

R. Hamatake, W. Kazmierski, A. Maynard, 2012 .

Characterization of Apo‐Form Selective Inhibition of Indoleamine 2,3‐Dioxygenase **

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2020, Chembiochem : a European journal of chemical biology.

Characterization of apo-form selective inhibition of indoleamine 2,3-dioxygenase

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2020, bioRxiv.

Characterization of novel inhibition of indoleamine 2,3-dioxygenase by targeting its apo form.

Douglas W. Thomson, Rodrigo F. Ortiz-Meoz, G. Bergamini, 2018 .

Unexpected antinociceptive potency of cyclic [D-Tca1]CTAP: potential for a novel mechanism of action.

V. Hruby, R. Knapp, H. Yamamura, 1993, European journal of pharmacology.

Antiviral Drugs: From Basic Discovery Through Clinical Trials

W. Kazmierski, 2011 .

Cholecystokinin analogues with high affinity and selectivity for brain membrane receptors.

V. Hruby, R. Knapp, H. Yamamura, 2009, International journal of peptide and protein research.

Efficient synthesis of metal binding peptides incorporating aminodiacetic acid based ligands.

W. Kazmierski, 2009, International journal of peptide and protein research.

Reduced peptide bond cyclic somatostatin based opioid octapeptides. Synthesis, conformational properties and pharmacological characterization.

V. Hruby, R. Knapp, H. Yamamura, 2009, International journal of peptide and protein research.

New Amino Acids for the Topographical Control of Peptide Conformation: Synthesis of All the Isomers of .alpha.,.beta.-Dimethylphenylalanine and .alpha.,.beta.-Dimethyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic Acid of High Optical Purity

V. Hruby, W. Kazmierski, Z. Urbańczyk-Lipkowska, 1994 .

A New Approach to Receptor Ligand Design: Synthesis and Conformation of a New Class of Potent and Highly Selective μ Opioid Antagonists Utilizing Tetrahydroisoquinoline Carboxylic Acid.

V. Hruby, W. Kazmierski, 1988 .

A new approach to receptor ligand design: synthesis and conformation of a new class of potent and highly selective μ opioid antagonists utilizing tetrahydroisoouinoline carroxylic acid

V. Hruby, W. Kazmierski, 1988 .

The Discovery of Conformationally Constrained Bicyclic Peptidomimetics as Potent Hepatitis C NS5A Inhibitors

W. Kazmierski, David K. Johnson, Nagaraju Miriyala, 2021, ACS medicinal chemistry letters.

Total synthesis and semi-synthetic approaches to analogues of antibacterial natural product althiomycin.

W. Kazmierski, P. Zarantonello, R. Ferritto, 2002, Bioorganic & medicinal chemistry letters.

Cyclic Aromatic Amino Acids with Constrained χ(1) and χ (2) Dihedral Angles.

W. Kazmierski, D. Tourwé, G. Tóth, 1999, Methods in molecular medicine.

Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.

E. Furfine, W. Kazmierski, A. Spaltenstein, 2004, Bioorganic & medicinal chemistry letters.

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.

F. Salituro, E. Furfine, W. Kazmierski, 2000, Bioorganic & medicinal chemistry letters.

Asymmetric Synthesis of Unusual Amino Acids Designed for Topographical Control of Peptide Confirmation

J. Knollenberg, E. Nicolás, W. Kazmierski, 1992 .

Emerging approaches in the molecular design of receptor-selective peptide ligands: conformational, topographical and dynamic considerations.

V. Hruby, W. Kazmierski, F. Al-Obeidi, 1990, The Biochemical journal.

Constrained phenylalanine analogues. Preferred conformation of the 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) residue.

C. Toniolo, M. Crisma, V. Hruby, 2009, International journal of peptide and protein research.

Metal chelating amino acids in the design of peptides and proteins. Synthesis of Nα-Fmoc/But protected amino acids incorporating aminodiacetic acid moiety.

W. Kazmierski, 1993 .

Recent Progress in Discovery of Small‐Molecule CCR5 Chemokine Receptor Ligands as HIV‐1 Inhibitors

T. Kenakin, W. Kazmierski, F. Deanda, 2003 .

Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties.

Z. Ni, Suoming Zhang, S. Baker, 2011, Bioorganic & medicinal chemistry letters.

Conformational Constraints in the Design of Receptor Selective Peptides: Conformational Analysis and Molecular Dynamics

V. Hruby, B. Pettitt, W. Kazmierski, 1988 .

[3H]-[H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2] ([3H]CTOP), a potent and highly selective peptide for mu opioid receptors in rat brain.

V. Hruby, K. Gulya, R. Knapp, 1989, The Journal of pharmacology and experimental therapeutics.

Asymmetric synthesis of topographically constrained amino acids: synthesis of the optically pure isomers of α,β-dimethyl-phenylalanine and α,β-dimethyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid

V. Hruby, W. Kazmierski, 1991 .

Conformationally restricted analogs of oxytocin; stabilization of inhibitory conformation.

M. Lebl, V. Hruby, W. Kazmierski, 2009, International journal of peptide and protein research.

GSK2818713, a novel biphenylene scaffold-based Hepatitis C NS5A replication complex inhibitor with broad genotype coverage.

R. Hamatake, W. Kazmierski, R. Crosby, 2020, Journal of medicinal chemistry.

Preclinical Characterization of GSK2336805, a Novel Inhibitor of Hepatitis C Virus Replication That Selects for Resistance in NS5A

R. Hamatake, J. Vamathevan, W. Kazmierski, 2013, Antimicrobial Agents and Chemotherapy.

Running title: Preclinical characterization of GSK2336805

R. Hamatake, J. Vamathevan, W. Kazmierski, 2013 .

Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors.

V. Hruby, T. Burks, R. Knapp, 1988, Journal of medicinal chemistry.

Peptide, Peptidomimetic and Small‐molecule Drug Discovery Targeting HIV‐1 Host‐cell Attachment and Entry through gp120, gp41, CCR5 and CXCR4 †

T. Kenakin, W. Kazmierski, K. Gudmundsson, 2006, Chemical biology & drug design.

A Convenient Synthesis of the Orthogonally-Protected Benzodiazepine-2,5-Dione Scaffold

W. Kazmierski, J. Mcdermed, 2000 .

New, potent P1/P2-morpholinone-based HIV-protease inhibitors.

E. Furfine, W. Kazmierski, A. Spaltenstein, 2006, Bioorganic & medicinal chemistry letters.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.

Brian A. Chauder, W. Kazmierski, B. Chauder, 2011, Journal of medicinal chemistry.

Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo.

V. Hruby, T. Burks, W. Kazmierski, 1989, The Journal of pharmacology and experimental therapeutics.

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.

J. Lehmann, P. Charifson, L. Leesnitzer, 1998, Journal of medicinal chemistry.

Recent advances in the design and synthesis of small-molecule mimetic drugs.

W. Kazmierski, 1994, Trends in biotechnology.

A solid-phase approach to analogues of the antibiotic mureidomycin.

W. Kazmierski, A. Bozzoli, G. Kennedy, 2000, Bioorganic & medicinal chemistry letters.

The Relative Activity of “Function Sparing” HIV-1 Entry Inhibitors on Viral Entry and CCR5 Internalization: Is Allosteric Functional Selectivity a Valuable Therapeutic Property?

T. Kenakin, R. Hollingsworth, K. Chiswell, 2009, Molecular Pharmacology.

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.

T. Kenakin, W. Kazmierski, R. Ferris, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1.

W. Kazmierski, G. A. Freeman, R. Ferris, 2011, Bioorganic & medicinal chemistry letters.

The CCR5 Receptor-Based Mechanism of Action of 873140, a Potent Allosteric Noncompetitive HIV Entry Inhibitor

T. Kenakin, W. Kazmierski, S. Jenkinson, 2005, Molecular Pharmacology.

Total Synthesis and Semi‐Synthetic Approaches to Analogues of Antibacterial Natural Product Althiomycin.

W. Kazmierski, P. Zarantonello, R. Ferritto, 2002 .

Alkali Carbonate Effects on N‐(2‐Hydroxyethyl)urea Cyclization: Application to a 2‐Imidazolidinone Scale‐Up

W. Kazmierski, T. Spitzer, I. Kaldor, 2013 .

Discovery of a novel series of cyclic urea as potent CCR5 antagonists.

W. Kazmierski, R. Ferris, J. Jun, 2011, Bioorganic & medicinal chemistry letters.

H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2: a potent and selective antagonist opioid receptors.

V. Hruby, K. Gulya, H. Yamamura, 1986, NIDA research monograph.

Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for mu opioid receptors.

V. Hruby, K. Gulya, H. Yamamura, 1986, Journal of medicinal chemistry.

Synthesis of 4‐Substituted Piperidines via a Mild and Scalable Two‐Step Cu2O‐Mediated Decarboxylation of Cyanoesters

W. Kazmierski, B. Chauder, C. Koble, 2006 .

Synthesis of 4-Substituted Piperidines via a Mild and Scalable Two-Step Cu2O-Mediated Decarboxylation of Cyanoesters.

W. Kazmierski, B. Chauder, C. Koble, 2006 .

A cyclic somatostatin analog that precipitates withdrawal in morphine-dependent mice.

V. Hruby, T. Burks, W. Kazmierski, 1987, NIDA research monograph.

DNA Encoded Library Technology-based discovery, lead optimization and prodrug strategy toward structurally-unique indoleamine 2,3-dioxygenase (IDO1) inhibitors.

Zhengrong Zhu, John Miller, N. Prabhu, 2020, Journal of medicinal chemistry.

4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents.

W. Kazmierski, R. Ferris, Maosheng Duan, 2009, Bioorganic & medicinal chemistry letters.

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats.

W. Kazmierski, R. Ferris, F. Deanda, 2011, Bioorganic & medicinal chemistry letters.

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.

W. Kazmierski, R. Ferris, A. Spaltenstein, 2010, Bioorganic & medicinal chemistry letters.

Recent Progress in the Discovery of New CCR5 and CXCR4 Chemokine Receptor Antagonists as Inhibitors of HIV-1 Entry. Part 2*

Stephen Jenkinson, S. Piscitelli, W. Kazmierski, 2005 .

Corrigendum to “Recent Progress in Discovery of Small–Molecule CCR5 Chemokine Receptor Ligands as HIV-1 Inhibitors” [Bioorg. Med. Chem. 2003, 11, 2663–2676]

T. Kenakin, W. Kazmierski, F. Deanda, 2003 .

Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease.

E. Furfine, W. Kazmierski, A. Spaltenstein, 2002, Bioorganic & medicinal chemistry letters.

Opioid receptor selectivity of beta-endorphin in vitro and in vivo: mu, delta and epsilon receptors.

V. Hruby, T. Burks, W. Kazmierski, 1988, The Journal of pharmacology and experimental therapeutics.

TARGETING THE NS5A PROTEIN OF HCV: AN EMERGING OPTION.

C. Cameron, W. Kazmierski, D. Cordek, 2011, Drugs of the future.

Topographic design of peptide neurotransmitters and hormones on stable backbone templates: relation of conformation and dynamics to bioactivity

V. Hruby, H. Yamamura, W. Kazmierski, 1991 .

Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates.

William McDowell, Yang Liu, Dazhong Fan, 2010, Bioorganic & medicinal chemistry letters.

The chemical synthesis of large random peptide libraries and their use for the discovery of ligands for macromolecular acceptors

K. Lam, M. Lebl, V. Hruby, 1993 .

Precipitation of spinally mediated withdrawal signs by intrathecal administration of naloxone and the mu-receptor antagonist CTP in morphine-dependent mice.

V. Hruby, T. Burks, W. Kazmierski, 1988, NIDA research monograph.

Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: from lead to clinical compound.

R. Hamatake, W. Kazmierski, R. Crosby, 2014, Journal of medicinal chemistry.

Conformationally restricted analogs of oxytocin; stabilization of inhibitory conformation.

W. Kazmierski, J. Slaninová, Victor J. Hruby, 2009 .

Inhibitors of human immunodeficiency virus type 1 derived from gp41 transmembrane protein: structure--activity studies.

W. Kazmierski, A. Aulabaugh, R. Hazen, 1996, Journal of medicinal chemistry.

Iron chelates bind nitric oxide and decrease mortality in an experimental model of septic shock.

D. S. Williams, W. Kazmierski, H. Thorp, 1996, Proceedings of the National Academy of Sciences of the United States of America.