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Items: 43

1.

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

Zimmer M, Bista P, Benson EL, Lee DY, Liu F, Picarella D, Vega RB, Vu CB, Yeager M, Ding M, Liang G, Horton JD, Kleemann R, Kooistra T, Morrison MC, Wielinga PY, Milne JC, Jirousek MR, Nichols AJ.

Hepatol Commun. 2017 May 12;1(4):311-325. doi: 10.1002/hep4.1042. eCollection 2017 Jun.

2.

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

Hammers DW, Sleeper MM, Forbes SC, Coker CC, Jirousek MR, Zimmer M, Walter GA, Sweeney HL.

JCI Insight. 2016 Dec 22;1(21):e90341. doi: 10.1172/jci.insight.90341.

3.

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

Vu CB, Bemis JE, Benson E, Bista P, Carney D, Fahrner R, Lee D, Liu F, Lonkar P, Milne JC, Nichols AJ, Picarella D, Shoelson A, Smith J, Ting A, Wensley A, Yeager M, Zimmer M, Jirousek MR.

J Med Chem. 2016 Feb 11;59(3):1217-31. doi: 10.1021/acs.jmedchem.5b01961. Epub 2016 Feb 1.

PMID:
26784936
4.

Crystal structures of human SIRT3 displaying substrate-induced conformational changes.

Jin L, Wei W, Jiang Y, Peng H, Cai J, Mao C, Dai H, Choy W, Bemis JE, Jirousek MR, Milne JC, Westphal CH, Perni RB.

J Biol Chem. 2009 Sep 4;284(36):24394-405. doi: 10.1074/jbc.M109.014928. Epub 2009 Jun 16.

5.

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

Bemis JE, Vu CB, Xie R, Nunes JJ, Ng PY, Disch JS, Milne JC, Carney DP, Lynch AV, Jin L, Smith JJ, Lavu S, Iffland A, Jirousek MR, Perni RB.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2350-3. doi: 10.1016/j.bmcl.2008.11.106. Epub 2008 Dec 6.

PMID:
19303289
6.

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

Smith JJ, Kenney RD, Gagne DJ, Frushour BP, Ladd W, Galonek HL, Israelian K, Song J, Razvadauskaite G, Lynch AV, Carney DP, Johnson RJ, Lavu S, Iffland A, Elliott PJ, Lambert PD, Elliston KO, Jirousek MR, Milne JC, Boss O.

BMC Syst Biol. 2009 Mar 10;3:31. doi: 10.1186/1752-0509-3-31.

7.

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

Jin L, Galonek H, Israelian K, Choy W, Morrison M, Xia Y, Wang X, Xu Y, Yang Y, Smith JJ, Hoffmann E, Carney DP, Perni RB, Jirousek MR, Bemis JE, Milne JC, Sinclair DA, Westphal CH.

Protein Sci. 2009 Mar;18(3):514-25. doi: 10.1002/pro.50.

8.

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

Vu CB, Bemis JE, Disch JS, Ng PY, Nunes JJ, Milne JC, Carney DP, Lynch AV, Smith JJ, Lavu S, Lambert PD, Gagne DJ, Jirousek MR, Schenk S, Olefsky JM, Perni RB.

J Med Chem. 2009 Mar 12;52(5):1275-83. doi: 10.1021/jm8012954.

PMID:
19199480
9.

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

Vu CB, Milne JC, Carney DP, Song J, Choy W, Lambert PD, Gagne DJ, Hirsch M, Cote A, Davis M, Lainez E, Meade N, Normington K, Jirousek MR, Perni RB.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1416-20. doi: 10.1016/j.bmcl.2009.01.044. Epub 2009 Jan 19.

PMID:
19181526
10.

SIRT1 exerts anti-inflammatory effects and improves insulin sensitivity in adipocytes.

Yoshizaki T, Milne JC, Imamura T, Schenk S, Sonoda N, Babendure JL, Lu JC, Smith JJ, Jirousek MR, Olefsky JM.

Mol Cell Biol. 2009 Mar;29(5):1363-74. doi: 10.1128/MCB.00705-08. Epub 2008 Dec 22.

11.

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

Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH.

Nature. 2007 Nov 29;450(7170):712-6.

12.

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

Zhao H, Liu G, Xin Z, Serby MD, Pei Z, Szczepankiewicz BG, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5543-6.

PMID:
15482920
13.

Reduction of PTP1B induces differential expression of PI3-kinase (p85alpha) isoforms.

Rondinone CM, Clampit J, Gum RJ, Zinker BA, Jirousek MR, Trevillyan JM.

Biochem Biophys Res Commun. 2004 Oct 15;323(2):652-9.

PMID:
15369800
14.

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

Xin Z, Liu G, Abad-Zapatero C, Pei Z, Szczepankiewicz BG, Li X, Zhang T, Hutchins CW, Hajduk PJ, Ballaron SJ, Stashko MA, Lubben TH, Trevillyan JM, Jirousek MR.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3947-50.

PMID:
14592481
15.

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

Liu G, Xin Z, Pei Z, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Zhao H, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 Sep 25;46(20):4232-5.

PMID:
13678400
16.

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

Pei Z, Li X, Liu G, Abad-Zapatero C, Lubben T, Zhang T, Ballaron SJ, Hutchins CW, Trevillyan JM, Jirousek MR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3129-32.

PMID:
12951078
17.

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

Liu G, Xin Z, Liang H, Abad-Zapatero C, Hajduk PJ, Janowick DA, Szczepankiewicz BG, Pei Z, Hutchins CW, Ballaron SJ, Stashko MA, Lubben TH, Berg CE, Rondinone CM, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 Jul 31;46(16):3437-40.

PMID:
12877578
18.

Potent, selective inhibitors of protein tyrosine phosphatase 1B.

Xin Z, Oost TK, Abad-Zapatero C, Hajduk PJ, Pei Z, Szczepankiewicz BG, Hutchins CW, Ballaron SJ, Stashko MA, Lubben T, Trevillyan JM, Jirousek MR, Liu G.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1887-90.

PMID:
12749891
19.

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

Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.

PMID:
12749884
20.

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

Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 May 22;46(11):2093-103.

PMID:
12747781
21.

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

Szczepankiewicz BG, Liu G, Hajduk PJ, Abad-Zapatero C, Pei Z, Xin Z, Lubben TH, Trevillyan JM, Stashko MA, Ballaron SJ, Liang H, Huang F, Hutchins CW, Fesik SW, Jirousek MR.

J Am Chem Soc. 2003 Apr 9;125(14):4087-96.

PMID:
12670229
22.

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

Gum RJ, Gaede LL, Heindel MA, Waring JF, Trevillyan JM, Zinker BA, Stark ME, Wilcox D, Jirousek MR, Rondinone CM, Ulrich RG.

Mol Endocrinol. 2003 Jun;17(6):1131-43. Epub 2003 Mar 20.

PMID:
12649327
23.

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

Clampit JE, Meuth JL, Smith HT, Reilly RM, Jirousek MR, Trevillyan JM, Rondinone CM.

Biochem Biophys Res Commun. 2003 Jan 10;300(2):261-7.

PMID:
12504077
24.

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

Gum RJ, Gaede LL, Koterski SL, Heindel M, Clampit JE, Zinker BA, Trevillyan JM, Ulrich RG, Jirousek MR, Rondinone CM.

Diabetes. 2003 Jan;52(1):21-8.

25.

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

Kaszubska W, Falls HD, Schaefer VG, Haasch D, Frost L, Hessler P, Kroeger PE, White DW, Jirousek MR, Trevillyan JM.

Mol Cell Endocrinol. 2002 Sep 30;195(1-2):109-18.

PMID:
12354677
26.

Protein tyrosine phosphatase 1B inhibitors for diabetes.

Johnson TO, Ermolieff J, Jirousek MR.

Nat Rev Drug Discov. 2002 Sep;1(9):696-709. Review.

PMID:
12209150
27.

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

Zinker BA, Rondinone CM, Trevillyan JM, Gum RJ, Clampit JE, Waring JF, Xie N, Wilcox D, Jacobson P, Frost L, Kroeger PE, Reilly RM, Koterski S, Opgenorth TJ, Ulrich RG, Crosby S, Butler M, Murray SF, McKay RA, Bhanot S, Monia BP, Jirousek MR.

Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11357-62. Epub 2002 Aug 8.

28.

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

Rondinone CM, Trevillyan JM, Clampit J, Gum RJ, Berg C, Kroeger P, Frost L, Zinker BA, Reilly R, Ulrich R, Butler M, Monia BP, Jirousek MR, Waring JF.

Diabetes. 2002 Aug;51(8):2405-11.

29.

Protein kinase C inhibitors as novel anticancer drugs.

Goekjian PG, Jirousek MR.

Expert Opin Investig Drugs. 2001 Dec;10(12):2117-40. Review.

PMID:
11772309
30.

In vitro enzymatic assays of protein tyrosine phosphatase 1B.

Lubben T, Clampit J, Stashko M, Trevillyan J, Jirousek MR.

Curr Protoc Pharmacol. 2001 Aug;Chapter 3:Unit3.8. doi: 10.1002/0471141755.ph0308s13.

PMID:
21959757
32.

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

Samokhin GP, Jirousek MR, Ways DK, Henriksen RA.

Eur J Pharmacol. 1999 Dec 15;386(2-3):297-303.

PMID:
10618482
33.
34.

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

Neel DA, Jirousek MR, McDonald JH 3rd.

Bioorg Med Chem Lett. 1998 Jan 6;8(1):47-50.

PMID:
9871626
35.

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

Kowluru RA, Jirousek MR, Stramm L, Farid N, Engerman RL, Kern TS.

Diabetes. 1998 Mar;47(3):464-9.

PMID:
9519755
36.

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

Wakasaki H, Koya D, Schoen FJ, Jirousek MR, Ways DK, Hoit BD, Walsh RA, King GL.

Proc Natl Acad Sci U S A. 1997 Aug 19;94(17):9320-5.

38.

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

Xia P, Aiello LP, Ishii H, Jiang ZY, Park DJ, Robinson GS, Takagi H, Newsome WP, Jirousek MR, King GL.

J Clin Invest. 1996 Nov 1;98(9):2018-26.

39.

(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.

Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH 3rd, Neel DA, Rito CJ, Singh U, Stramm LE, Melikian-Badalian A, Baevsky M, Ballas LM, Hall SE, Winneroski LL, Faul MM.

J Med Chem. 1996 Jul 5;39(14):2664-71.

PMID:
8709095
40.

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

Ishii H, Jirousek MR, Koya D, Takagi C, Xia P, Clermont A, Bursell SE, Kern TS, Ballas LM, Heath WF, Stramm LE, Feener EP, King GL.

Science. 1996 May 3;272(5262):728-31.

PMID:
8614835
41.

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

Kunisaki M, Bursell SE, Clermont AC, Ishii H, Ballas LM, Jirousek MR, Umeda F, Nawata H, King GL.

Am J Physiol. 1995 Aug;269(2 Pt 1):E239-46.

PMID:
7653541
42.

Electrophilic levuglandin E2-protein adducts bind glycine: a model for protein crosslinking.

Jirousek MR, Murthi KK, Salomon RG.

Prostaglandins. 1990 Aug;40(2):187-203.

PMID:
2217833
43.

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

Salomon RG, Jirousek MR, Ghosh S, Sharma RB.

Prostaglandins. 1987 Nov;34(5):643-56.

PMID:
3481092

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