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Items: 27

1.

Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 Inhibitors.

Farrell PJ, Zopf CJ, Huang HJ, Balakrishna D, Holub C, Bilakovics J, Fanjul A, Matuszkiewicz J, Plonowski A, Rolzin P, Banerjee U, Ermolieff J, Cheruvallath ZS, McBride C, Bartkowski D, Mazur C, Pachori A, Larson CJ.

J Pharmacol Exp Ther. 2019 Nov;371(2):299-308. doi: 10.1124/jpet.119.259028. Epub 2019 Sep 19.

PMID:
31537613
2.

Correction to "Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure".

Lanier M, Pickens J, Bigi SV, Bradshaw-Pierce EL, Chambers A, Cheruvallath ZS, Cole D, Dougan DR, Ermolieff J, Gibson T, Halkowycz P, Hirokawa A, Ivetac A, McBride C, Miura J, Nunez E, Sabat M, Tyhonas J, Wang H, Wang X, Swann S.

ACS Med Chem Lett. 2017 Nov 8;8(12):1341. doi: 10.1021/acsmedchemlett.7b00457. eCollection 2017 Dec 14.

3.

Time-dependent inhibition of PHD2.

Tcholakov I, Grimshaw CE, Shi L, Kiryanov A, Murphy ST, Larson CJ, Plonowski A, Ermolieff J.

Biosci Rep. 2017 Jun 30;37(3). pii: BSR20170275. doi: 10.1042/BSR20170275. Print 2017 Jun 30.

4.

Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.

Lanier M, Pickens J, Bigi SV, Bradshaw-Pierce EL, Chambers A, Cheruvallath ZS, Cole D, Dougan DR, Ermolieff J, Gibson T, Halkowycz P, Hirokawa A, Ivetac A, Miura J, Nunez E, Sabat M, Tyhonas J, Wang H, Wang X, Swann S.

ACS Med Chem Lett. 2017 Feb 8;8(3):316-320. doi: 10.1021/acsmedchemlett.6b00481. eCollection 2017 Mar 9. Erratum in: ACS Med Chem Lett. 2017 Nov 08;8(12 ):1341.

5.

Residence time and kinetic efficiency analysis of extracellular signal-regulated kinase 2 inhibitors.

Vanderpool D, Grimshaw CE, Lawson JD, Ermolieff J.

Anal Biochem. 2015 Mar 15;473:46-52. doi: 10.1016/j.ab.2014.12.008. Epub 2014 Dec 20.

PMID:
25535956
6.

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.

Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24.

PMID:
23489629
7.

Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).

Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH.

J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23.

PMID:
22040023
8.

Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery.

Johnson MC, Hu Q, Lingardo L, Ferre RA, Greasley S, Yan J, Kath J, Chen P, Ermolieff J, Alton G.

J Comput Aided Mol Des. 2011 Jul;25(7):689-98. doi: 10.1007/s10822-011-9456-7. Epub 2011 Jul 22.

PMID:
21779981
9.

Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays.

Hofler A, Nichols T, Grant S, Lingardo L, Esposito EA, Gridley S, Murphy ST, Kath JC, Cronin CN, Kraus M, Alton G, Xie Z, Sutton S, Gehring M, Ermolieff J.

Anal Biochem. 2011 Jul 15;414(2):179-86. doi: 10.1016/j.ab.2011.03.013. Epub 2011 Mar 12.

PMID:
21402045
10.

The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.

Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P.

Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10.

PMID:
20363126
11.

Characterization of the CHK1 allosteric inhibitor binding site.

Vanderpool D, Johnson TO, Ping C, Bergqvist S, Alton G, Phonephaly S, Rui E, Luo C, Deng YL, Grant S, Quenzer T, Margosiak S, Register J, Brown E, Ermolieff J.

Biochemistry. 2009 Oct 20;48(41):9823-30. doi: 10.1021/bi900258v.

PMID:
19743875
12.

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.

Siu M, Johnson TO, Wang Y, Nair SK, Taylor WD, Cripps SJ, Matthews JJ, Edwards MP, Pauly TA, Ermolieff J, Castro A, Hosea NA, LaPaglia A, Fanjul AN, Vogel JE.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7. doi: 10.1016/j.bmcl.2009.05.011. Epub 2009 May 7.

PMID:
19473839
13.

A novel selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitor prevents human adipogenesis.

Bujalska IJ, Gathercole LL, Tomlinson JW, Darimont C, Ermolieff J, Fanjul AN, Rejto PA, Stewart PM.

J Endocrinol. 2008 May;197(2):297-307. doi: 10.1677/JOE-08-0050.

14.

Assay optimization and kinetic profile of the human and the rabbit isoforms of 11beta-HSD1.

Castro A, Zhu JX, Alton GR, Rejto P, Ermolieff J.

Biochem Biophys Res Commun. 2007 Jun 1;357(2):561-6. Epub 2007 Apr 9.

PMID:
17434447
15.

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
16.

Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).

Ghosh AK, Bilcer G, Harwood C, Kawahama R, Shin D, Hussain KA, Hong L, Loy JA, Nguyen C, Koelsch G, Ermolieff J, Tang J.

J Med Chem. 2001 Aug 30;44(18):2865-8.

PMID:
11520194
17.

Subsite specificity of memapsin 2 (beta-secretase): implications for inhibitor design.

Turner RT 3rd, Koelsch G, Hong L, Castanheira P, Ermolieff J, Ghosh AK, Tang J.

Biochemistry. 2001 Aug 28;40(34):10001-6. Erratum in: Biochemistry 2001 Oct 9;40(40):12230. Castenheira, P [corrected to Castanheira, P]; Ghosh, A [corrected to Ghosh, AK].

PMID:
11513577
18.

Polyoxometalate HIV-1 protease inhibitors. A new mode of protease inhibition.

Judd DA, Nettles JH, Nevins N, Snyder JP, Liotta DC, Tang J, Ermolieff J, Schinazi RF, Hill CL.

J Am Chem Soc. 2001 Feb 7;123(5):886-97.

PMID:
11456622
19.

Proteolytic activation of recombinant pro-memapsin 2 (Pro-beta-secretase) studied with new fluorogenic substrates

Ermolieff J, Loy JA, Koelsch G, Tang J.

Biochemistry. 2000 Dec 26;39(51):16263. No abstract available.

PMID:
11123957
20.

Proteolytic activation of recombinant pro-memapsin 2 (pro-beta-secretase) studied with new fluorogenic substrates.

Ermolieff J, Loy JA, Koelsch G, Tang J.

Biochemistry. 2000 Oct 10;39(40):12450-6. Erratum in: Biochemistry 2000 Dec 26;39(51):16263.

PMID:
11015226
21.

Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase).

Ghosh AK, Shin D, Downs D, Koelsch G, Lin X, Ermolieff J, Tang J.

J Am Chem Soc. 2000 Apr 12;122(14):3522-3523. doi: 10.1021/ja000300g. Epub 2000 Mar 23. No abstract available.

22.

Heparin accelerates the inhibition of cathepsin G by mucus proteinase inhibitor: potent effect of O-butyrylated heparin.

Ermolieff J, Duranton J, Petitou M, Bieth JG.

Biochem J. 1998 Mar 15;330 ( Pt 3):1369-74.

23.

The effect of substrates on the kinetics and the in vivo threshold activity of mutant HIV-1 proteases.

Ermolieff J, Lin X, Tang J.

Adv Exp Med Biol. 1998;436:47-51. No abstract available.

PMID:
9561198
24.
26.

Mapping the heparin-binding site of mucus proteinase inhibitor.

Mellet P, Ermolieff J, Bieth JG.

Biochemistry. 1995 Feb 28;34(8):2645-52.

PMID:
7873546
27.

Heparin protects cathepsin G against inhibition by protein proteinase inhibitors.

Ermolieff J, Boudier C, Laine A, Meyer B, Bieth JG.

J Biol Chem. 1994 Nov 25;269(47):29502-8.

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