M. Jirousek

发表

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy.

Gang Liu, P. Hajduk, S. Fesik, 2003, Journal of the American Chemical Society.

Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors.

David P. Carney, D. Gagne, P. Lambert, 2009, Bioorganic & medicinal chemistry letters.

Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor.

S. Bursell, G. King, D. Koya, 1996, Science.

CAT‐2003: A novel sterol regulatory element‐binding protein inhibitor that reduces steatohepatitis, plasma lipids, and atherosclerosis in apolipoprotein E*3‐Leiden mice

Rick B. Vega, T. Kooistra, R. Kleemann, 2017, Hepatology communications.

Characterization of protein kinase C beta isoform activation on the gene expression of transforming growth factor-beta, extracellular matrix components, and prostanoids in the glomeruli of diabetic rats.

G. King, D. Koya, K. Kuboki, 1997, The Journal of clinical investigation.

Protein kinase C inhibitors as novel anticancer drugs

M. Jirousek, P. Goekjian, 2001, Expert opinion on investigational drugs.

Abnormalities of retinal metabolism in diabetes or experimental galactosemia: V. Relationship between protein kinase C and ATPases.

N. Farid, T. Kern, R. Engerman, 1998, Diabetes.

A Novel NF‐κB Inhibitor, Edasalonexent (CAT‐1004), in Development as a Disease‐Modifying Treatment for Patients With Duchenne Muscular Dystrophy: Phase 1 Safety, Pharmacokinetics, and Pharmacodynamics in Adult Subjects

E. Offman, M. Jirousek, M. Zimmer, 2017, Journal of clinical pharmacology.

Reduction of protein-tyrosine phosphatase-1B increases insulin signaling in FAO hepatoma cells.

C. Rondinone, J. Trevillyan, Harriet T. Smith, 2003, Biochemical and biophysical research communications.

Protein tyrosine phosphatase 1B reduction regulates adiposity and expression of genes involved in lipogenesis.

J. Waring, R. Ulrich, B. Monia, 2002, Diabetes.

Protein Tyrosine Phosphatase 1B Reduction Regulates Adiposity and Expression of Genes Involved in

J. Waring, R. Ulrich, B. Monia, 2002 .

PHASE 1 SINGLE AND MULTIPLE ASCENDING DOSE STUDY OF CAT-2003, A NOVEL ACTIVATOR OF LIPOPROTEIN LIPASE, DEMONSTRATES REDUCTIONS IN POSTPRANDIAL TRIGLYCERIDES

M. Curtis, M. Jirousek, R. Dunbar, 2014 .

Protein kinase C in the treatment of disease: signal transduction pathways, inhibitors, and agents in development.

M. Jirousek, P. Goekjian, 1999, Current medicinal chemistry.

Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.

M. Faul, L. M. Ballas, M. Jirousek, 2003, Bioorganic & medicinal chemistry letters.

The Identification of the SIRT1 Activator SRT2104 as a Clinical Candidate

Amy V. Lynch, David P. Carney, P. J. Elliot, 2013 .

The protein kinase C β–specific inhibitor LY379196 blocks TPA‐induced monocytic differentiation of HL60 cells the protein kinase C β–specific inhibitor LY379196 blocks TPA‐induced monocytic differentiation of HL60 cells

I. Weinstein, A. Ikui, M. Jirousek, 2000, Molecular carcinogenesis.

Prostaglandin endoperoxides 21. Covalent binding of levuglandin E2 with proteins.

R. G. Salomon, M. Jirousek, R. Sharma, 1987, Prostaglandins.

(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.

M. Faul, L. L. Winneroski, S. Hall, 1996, Journal of medicinal chemistry.

Synthesis of indole-ring fluorine-labeled analogs of LY333531, an isoform-selective inhibitor of protein kinase C

James W. White, J. T. Dixon, L. M. Ballas, 1999 .

Synthesis of bisindolylmaleimides using a palladium catalyzed cross-coupling reaction.

M. Jirousek, D. A. Neel, J. H. Mcdonald, 1998, Bioorganic & medicinal chemistry letters.

Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes

Amy V. Lynch, David P. Carney, D. Gagne, 2007, Nature.

Disease-modifying effects of orally bioavailable NF-κB inhibitors in dystrophin-deficient muscle.

David W. Hammers, H. Sweeney, S. Forbes, 2016, JCI insight.

In Vitro Enzymatic Assays of Protein Tyrosine Phosphatase 1B

J. Trevillyan, T. Lubben, M. Stashko, 2001, Current protocols in pharmacology.

Macrocyclic Bisindolylmaleimides: Synthesis by Inter- and Intramolecular Alkylation

M. Faul, K. A. Sullivan, L. L. Winneroski, 1998 .

Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.

Amy V. Lynch, David P. Carney, D. Gagne, 2009, Journal of medicinal chemistry.

A practical and efficient intramolecular Michael addition of ureas to α,β-unsaturated esters

Z. Pei, Zhili Xin, M. Jirousek, 2000 .

A synthesis or indolizidines related to castanospermine and swainsonine.

M. Wick, R. Babine, S. Schow, 1993 .

Structure activity studies on pseudo-symmetrical HIV-1 protease inhibitors

M. Wick, R. Babine, S. Kerwar, 1993 .

PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice

J. Waring, R. Ulrich, S. Crosby, 2002, Proceedings of the National Academy of Sciences of the United States of America.

Protein tyrosine phosphatase 1B inhibitors for diabetes

J. Ermolieff, M. Jirousek, T. O. Johnson, 2002, Nature Reviews Drug Discovery.

The Effect of Carbonyl Containing Terminal Chains on Mesomorphic Properties in 4,4′- Disubstituted Phenylbenzoates and Phenylthiobenzoates. 4. Phenylbenzoates Containing A (CH2)nCO2R'Group (n = 0–2) on the Phenolic End

M. Neubert, M. Jirousek, R. Sharma, 1991 .

Amelioration of Vascular Dysfunctions in Diabetic Rats by an Oral PKC β Inhibitor

S. Bursell, G. King, D. Koya, 1996, Science.

The Effect of Two Terminal Alkoxy Groups on the Mesomorphic Properties of 4, 4′-Disubstituted Phenylthiobenzoates

M. Neubert, M. Jirousek, S. J. Laskos, 1988 .

Mesomorphic Properties of Some 4, 4′- Alkyl and Alkoxy Disubstituted Phenylbenzoates

M. Neubert, M. Jirousek, C. Hanlon, 1986 .

The effect of 2- and 3-lateral substituents on the acid side of 4,4'-disubstituted phenylbenzoates and phenylthiobenzoates on mesomorphic properties

M. Jirousek, S. S. Keast, M. Neubert, 1994 .

The Effect of Carbonyl Containing Substituents in the Terminal Chains on Mesomorphic Properties in Some Aromatic Esters and Thioesters. 3. Acyloxy Groups on the Acid End

M. Neubert, M. Jirousek, M. Ezenyilimba, 1988 .

Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands.

Gang Liu, Cristina M Rondinone, P. Hajduk, 2003, Journal of medicinal chemistry.

Potent, selective inhibitors of protein tyrosine phosphatase 1B.

Gang Liu, P. Hajduk, C. Abad-Zapatero, 2003, Bioorganic & medicinal chemistry letters.

Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid.

David P. Carney, P. Bista, F. Liu, 2016, Journal of medicinal chemistry.

Sirtuins: novel targets for metabolic disease.

P. Elliott, M. Jirousek, 2008, Current opinion in investigational drugs.

Antisense protein tyrosine phosphatase 1B reverses activation of p38 mitogen-activated protein kinase in liver of ob/ob mice.

J. Waring, R. Ulrich, C. Rondinone, 2003, Molecular endocrinology.

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.

Gang Liu, P. Hajduk, S. Fesik, 2003, Journal of medicinal chemistry.

PTP1B antisense-treated mice show regulation of genes involved in lipogenesis in liver and fat

J. Waring, R. Ulrich, C. Rondinone, 2003, Molecular and Cellular Endocrinology.

Characterization of vascular endothelial growth factor's effect on the activation of protein kinase C, its isoforms, and endothelial cell growth.

L. Aiello, G. King, Z. Jiang, 1996, The Journal of clinical investigation.

Inhibition of intraocular neovascularization caused by retinal ischemia in pigs by PKCbeta inhibition with LY333531.

R. Danis, M. Jirousek, Y. Yang, 1998, Investigative ophthalmology & visual science.

Vascular Endothelial Growth Factor–Induced Retinal Permeability Is Mediated by Protein Kinase C In Vivo and Suppressed by an Orally Effective β-Isoform–Selective Inhibitor

Hidehiro Ishii, Lloyd Paul Aiello, Lois E. H. Smith, 1997, Diabetes.

SIRT1 Exerts Anti-Inflammatory Effects and Improves Insulin Sensitivity in Adipocytes

J. Olefsky, T. Imamura, S. Schenk, 2008, Molecular and Cellular Biology.

Protein tyrosine phosphatase 1B negatively regulates leptin signaling in a hypothalamic cell line

D. White, D. Haasch, P. Kroeger, 2002, Molecular and Cellular Endocrinology.

Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor.

Gang Liu, Hongyu Zhao, Cristina M Rondinone, 2003, Journal of medicinal chemistry.

Synthesis of Fluorinated Macrocyclic Bis(indolyl)maleimides as Potential 19F NMR Probes for Protein Kinase C.

J. T. Dixon, L. M. Ballas, M. Jirousek, 1999 .

Purification Of A Water-Sensitive Natural Product With An Aprotic Cpc Solvent System

R. G. Salomon, M. Jirousek, 1988 .

Synthesis and biological evaluation of a series of HIV-1 protease inhibitors

M. Wick, R. Babine, S. Kerwar, 1993 .

Vitamin E prevents diabetes-induced abnormal retinal blood flow via the diacylglycerol-protein kinase C pathway.

S. Bursell, G. King, A. Clermont, 1995, The American journal of physiology.

Crystal Structures of Human SIRT3 Displaying Substrate-induced Conformational Changes

Wentao Wei, Lei Jin, C. Mao, 2009, The Journal of Biological Chemistry.

Targeted overexpression of protein kinase C beta2 isoform in myocardium causes cardiomyopathy.

G. King, F. Schoen, R. Walsh, 1997, Proceedings of the National Academy of Sciences of the United States of America.

Effects of protein kinase C inhibitors on thromboxane production by thrombin-stimulated platelets.

D. K. Ways, G. Samokhin, R. Henriksen, 1999, European journal of pharmacology.

Vascular endothelial growth factor-induced retinal permeability is mediated by protein kinase C in vivo and suppressed by an orally effective beta-isoform-selective inhibitor.

L. Aiello, S. Bursell, E. Duh, 1998, Diabetes.

Reduction of protein tyrosine phosphatase 1B increases insulin-dependent signaling in ob/ob mice.

R. Ulrich, C. Rondinone, R. Gum, 2003, Diabetes.

Small molecule activators of SIRT1 replicate signaling pathways triggered by calorie restriction in vivo

David J. Gagne, Brian P. Frushour, Peter J. Elliott, 2009, BMC Syst. Biol..

Acid-Base Equilibria of (2,2'-Bipyridyl-4,4'-dicarboxylic acid)ruthenium(II) Complexes and the Effect of Protonation on Charge-Transfer Sensitization of Nanocrystalline Titania.

P. Liska, P. Liska, S. Zakeeruddin, 1999, Inorganic chemistry.

Biochemical characterization, localization, and tissue distribution of the longer form of mouse SIRT3

David P. Carney, Lei Jin, J. Milne, 2009, Protein science : a publication of the Protein Society.

Proteomic analysis of liver in rats chronically exposed to fluoride and AIN-93 M-hypercaloric diet

J. Shaw, L. Almasy, J. Blangero, 2013 .

Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.

P. Hajduk, C. Abad-Zapatero, C. Rondinone, 2004, Bioorganic & medicinal chemistry letters.

Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B.

P. Hajduk, C. Abad-Zapatero, Xiaofen Li, 2003, Bioorganic & Medicinal Chemistry Letters.

Discovery and SAR of novel, potent and selective protein tyrosine phosphatase 1B inhibitors.

Gang Liu, C. Abad-Zapatero, Xiaofen Li, 2003, Bioorganic & medicinal chemistry letters.

Acyclic N-(Azacycloalkyl)bisindolylmaleimides: Isozyme Selective Inhibitors of PKCβ.

M. Faul, L. M. Ballas, M. Jirousek, 2003 .

Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid.

David P. Carney, P. Bista, J. Milne, 2016, Journal of medicinal chemistry.

Abstract 6: CAT-2003 is a Novel Small Molecule That Inhibits Proprotein Convertase Subtilisin/Kexin Type 9 Production and Lowers Non--High-Density Lipoprotein Cholesterol

P. Bista, M. Jirousek, M. Zimmer, 2014, Arteriosclerosis, Thrombosis, and Vascular Biology.

Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators.

Amy V. Lynch, David P. Carney, Siva Lavu, 2009, Bioorganic & medicinal chemistry letters.

Reduction of PTP1B induces differential expression of PI3-kinase (p85α) isoforms

C. Rondinone, R. Gum, J. Trevillyan, 2004 .

Small molecule activators of SIRT1 replicate signaling pathways triggered by calorie restriction in vivo

Amy V. Lynch, David P. Carney, Robin J. Johnson, 2009, BMC Systems Biology.

Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.

Amy V. Lynch, David P. Carney, D. Gagne, 2009, Journal of medicinal chemistry.

Protein tyrosine phosphatase 1B inhibitors for diabetes

J. Ermolieff, M. Jirousek, T. O. Johnson, 2002, Nature Reviews Drug Discovery.

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.

P. Hajduk, S. Fesik, C. Abad-Zapatero, 2003, Journal of medicinal chemistry.

Treatment of zucker diabetic fatty rats with antisense oligonucleotide to phosphotyrosine phosphatase-1B for 5 weeks halts development of diabetes

E. Bush, J. Trevillyan, P. Jacobson, 2001 .