J. Wityak

发表

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase in

Ping Chen, A. Doweyko, Derek J. Norris, 2006, Journal of medicinal chemistry.

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Journal of medicinal chemistry.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

J. Wityak, G. Trainor, F. Hobbs, 1998, Bioorganic & medicinal chemistry letters.

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.

Gulzar Ahmed, Arthur M Doweyko, Axel Metzger, 2005, Journal of medicinal chemistry.

Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.

J. Wityak, S. Mousa, R. Olson, 1997, Journal of medicinal chemistry.

Quantifying autophagy using novel LC3B and p62 TR-FRET assays

D. Marchionini, J. Wityak, C. Dominguez, 2018, PloS one.

Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease.

J. Wityak, A. Beresford, L. Mrzljak, 2015, Journal of medicinal chemistry.

Longitudinal microPET imaging of the zQ175 mouse model of Huntington´s disease shows in vivo changes of molecular targets in the striatum and the cerebral cortex

J. Wityak, K. Varnäs, A. Forsberg, 2016 .

Biaryl substituted alkylboronate esters as thrombin inhibitors

J. Wityak, P. Weber, C. Dominguez, 1997 .

Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.

W. DeGrado, J. Wityak, S. Mousa, 1997, Journal of medicinal chemistry.

Orally Active Isoxazoline GPIIb/IIIa Antagonists

J. Wityak, S. Mousa, 1998 .

Xv454, a Novel Nonpeptide Small-molecule Platelet Giib/iiia Antagonist with Comparable Platelet αiibβ3-binding Kinetics to c7e3

J. Wityak, S. Mousa, R. Olson, 1998 .

Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.

J. Wityak, S. Mousa, R. Olson, 2000, Bioorganic & medicinal chemistry letters.

Selective Itk inhibitors block T-cell activation and murine lung inflammation.

A. Doweyko, S. Spergel, R. Moquin, 2004, Biochemistry.

[11C]CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins.

J. Wityak, C. Halldin, K. Varnäs, 2021, Journal of medicinal chemistry.

Section Review: Cardiovascular & Renal: Glycoprotein IIb/IIIa antagonists

J. Wityak, T. Sielecki, 1996 .

Oral antiplatelet efficacy and specificity of a novel nonpeptide platelet GPIIb/IIIa receptor antagonist, DMP 802.

J. Wityak, P. Anderson, S. Mousa, 1998, Journal of cardiovascular pharmacology.

Intravenous and oral antiplatelet/antithrombotic efficacy and specificity of XR300, a novel nonpeptide platelet GPIIb/IIIa antagonist.

J. Wityak, S. Mousa, J. Bozarth, 1998, Journal of cardiovascular pharmacology.

Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.

J. Wityak, S. Mousa, R. Olson, 1997, Journal of medicinal chemistry.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

A. Doweyko, James Lin, J. Wityak, 2010, Journal of medicinal chemistry.

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

A. Doweyko, S. Spergel, R. Moquin, 2006, Bioorganic & medicinal chemistry letters.

Isoxazolines as Potent Antagonists of the Integrin αvβ3

P. Jadhav, J. Wityak, S. Mousa, 2000 .

Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.

J. Wityak, P. Anderson, S. Mousa, 1999, Journal of medicinal chemistry.

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Ping Chen, A. Doweyko, R. Moquin, 2003, Bioorganic & medicinal chemistry letters.

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

A. Doweyko, R. Moquin, James Lin, 2003, Bioorganic & medicinal chemistry letters.

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.

A. Doweyko, S. Spergel, R. Moquin, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: improvement of cell potency.

Ping Chen, Derek J. Norris, Henry H. Gu, 2002, Bioorganic & medicinal chemistry letters.

Identification of chemokine receptor CCR4 antagonist.

J. Wityak, M. Poss, Wayne Vaccaro, 2005, Bioorganic & medicinal chemistry letters.

Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.

J. Wityak, E. Saez, R. Epple, 2010, Journal of medicinal chemistry.

Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

J. Y. Roberge, Ping Chen, A. Doweyko, 2002, Bioorganic & medicinal chemistry letters.

A 1,3-dipolar cycloaddition route to the 3(R)- and 3(S)-hydroxy-2(S)-arginines

J. Wityak, S. Gould, D. Keszler, 1987 .

Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate.

J. Wityak, S. Mousa, R. Olson, 1999, Bioorganic & medicinal chemistry letters.

A versatile synthesis of C‐5 labeled ornithines

J. Wityak, S. Gould, V. Palaniswamy, 1985 .

Biosynthesis of streptothricin F

J. Wityak, S. Gould, Junning Lee, 1991 .

A Monoclonal Antibody TrkB Receptor Agonist as a Potential Therapeutic for Huntington’s Disease

S. Dowler, J. Wityak, G. Mcallister, 2014, PloS one.

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Ping Chen, A. Doweyko, Derek J. Norris, 2004, Bioorganic & medicinal chemistry letters.

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Wei Li, Gulzar Ahmed, John Dodd, 2004, Journal of medicinal chemistry.

Synthesis of 1,3-Diynes Using Palladium-Copper Catalysis

J. Wityak, J. Chan, 1991 .

Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.

J. Wityak, G. Trainor, R. Copeland, 2004, Bioorganic & medicinal chemistry letters.

Pharmacodynamic Biomarkers for HTT-Lowering Therapies

B. Borowsky, J. Wityak, L. Mrzljak, 2015 .

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

A. Doweyko, S. Spergel, R. Moquin, 2006, Bioorganic & medicinal chemistry letters.

Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

J. Wityak, H. Lashuel, C. Scheich, 2021, Scientific Reports.

Improved synthesis of [18F] fallypride and characterization of a Huntington’s disease mouse model, zQ175DN KI, using longitudinal PET imaging of D2/D3 receptors

J. Wityak, A. Airaksinen, L. Park, 2019, EJNMMI Radiopharmacy and Chemistry.

A Profiling Platform for the Characterization of Transglutaminase 2 (TG2) Inhibitors

J. Wityak, C. Dominguez, R. Pacifici, 2010, Journal of biomolecular screening.

Lead optimization toward proof-of-concept tools for Huntington's disease within a 4-(1H-pyrazol-4-yl)pyrimidine class of pan-JNK inhibitors.

David D. Manning, J. Wityak, D. Kitchen, 2015, Journal of medicinal chemistry.

Longitudinal Characterization of mGluR5 Using 11C-ABP688 PET Imaging in the Q175 Mouse Model of Huntington Disease

J. Wityak, L. Mrzljak, C. Dominguez, 2018, The Journal of Nuclear Medicine.

MR-based spatial normalization improves [18F]MNI-659 PET regional quantification and detectability of disease effect in the Q175 mouse model of Huntington’s disease

A. Van der Linden, J. Wityak, L. Mrzljak, 2018, PloS one.

Noninvasive Relative Quantification of [11C]ABP688 PET Imaging in Mice Versus an Input Function Measured Over an Arteriovenous Shunt

M. Verhoye, A. Van der Linden, J. Wityak, 2018, Front. Neurol..

Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.

Andreas Ebneth, Sabine Schaertl, Andreas Scheel, 2012, Journal of medicinal chemistry.

3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.

J. Wityak, A. Kreusch, E. Saez, 2006, Bioorganic & medicinal chemistry letters.

Isoxazolines as Potent Antagonists of the Integrin αvβ3.

J. Wityak, 2000 .

SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.

J. Wityak, C. Dominguez, M. Beconi, 2012, ACS medicinal chemistry letters.

Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease.

J. Wityak, C. Dominguez, O. Ichihara, 2012, ACS medicinal chemistry letters.

N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.

Peter Tontonoz, Tove Tuntland, Ansgar Brock, 2007, Journal of medicinal chemistry.

Imaging Mutant Huntingtin Aggregates: Development of a Potential PET ligand.

J. Wityak, C. Halldin, L. Mrzljak, 2020, Journal of medicinal chemistry.

Longitudinal Small-Animal PET Imaging of the zQ175 Mouse Model of Huntington Disease Shows In Vivo Changes of Molecular Targets in the Striatum and Cerebral Cortex

J. Wityak, C. Halldin, K. Varnäs, 2017, The Journal of Nuclear Medicine.

Synthesis and antiplatelet activity of DMP 757 analogs

W. DeGrado, J. Wityak, S. Mousa, 1995 .

Novel nonpeptide antiplatelet glycoprotein llb/llla receptor antagonist, DMP754: receptor binding affinity and specificity

M. Hussain, W. DeGrado, J. Wityak, 1996, Coronary artery disease.