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Results: 1 to 20 of 125

1.

The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.

Grella B, Adams J, Berry JF, Delahanty G, Ferraris DV, Majer P, Ni C, Shukla K, Shuler SA, Slusher BS, Stathis M, Tsukamoto T.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7222-5. doi: 10.1016/j.bmcl.2010.10.109. Epub 2010 Oct 26.

PMID:
21074428
[PubMed - indexed for MEDLINE]
2.

Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents.

Kozikowski AP, Zhang J, Nan F, Petukhov PA, Grajkowska E, Wroblewski JT, Yamamoto T, Bzdega T, Wroblewska B, Neale JH.

J Med Chem. 2004 Mar 25;47(7):1729-38.

PMID:
15027864
[PubMed - indexed for MEDLINE]
3.

Structure-activity relationships of glutamate carboxypeptidase II (GCPII) inhibitors.

Ferraris DV, Shukla K, Tsukamoto T.

Curr Med Chem. 2012;19(9):1282-94. Review.

PMID:
22304717
[PubMed - indexed for MEDLINE]
4.

Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.

Stoermer D, Liu Q, Hall MR, Flanary JM, Thomas AG, Rojas C, Slusher BS, Tsukamoto T.

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2097-100.

PMID:
12798312
[PubMed - indexed for MEDLINE]
5.

Rationally designed sulfamides as glutamate carboxypeptidase II inhibitors.

Choy CJ, Fulton MD, Davis AL, Hopkins M, Choi JK, Anderson MO, Berkman CE.

Chem Biol Drug Des. 2013 Nov;82(5):612-9. doi: 10.1111/cbdd.12174. Epub 2013 Sep 25.

PMID:
23773397
[PubMed - indexed for MEDLINE]
6.

Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors.

Rong SB, Zhang J, Neale JH, Wroblewski JT, Wang S, Kozikowski AP.

J Med Chem. 2002 Sep 12;45(19):4140-52.

PMID:
12213057
[PubMed - indexed for MEDLINE]
7.

Tripeptidyl-peptidase II (TPP II) inhibitory activity of (S)-2,3-dihydro-2-(1H-imidazol-2-yl)-1H-indoles, a systematic SAR evaluation. Part 2.

Breslin HJ, Miskowski TA, Kukla MJ, De Winter HL, Somers MV, Roevens PW, Kavash RW.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4467-71.

PMID:
14643348
[PubMed - indexed for MEDLINE]
8.

Structural basis of interactions between human glutamate carboxypeptidase II and its substrate analogs.

Barinka C, Hlouchova K, Rovenska M, Majer P, Dauter M, Hin N, Ko YS, Tsukamoto T, Slusher BS, Konvalinka J, Lubkowski J.

J Mol Biol. 2008 Mar 7;376(5):1438-50. doi: 10.1016/j.jmb.2007.12.066. Epub 2008 Jan 5.

PMID:
18234225
[PubMed - indexed for MEDLINE]
Free PMC Article
9.
10.

MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3.

Marcq V, Mirand C, Decarme M, Emonard H, Hornebeck W.

Bioorg Med Chem Lett. 2003 Sep 1;13(17):2843-6.

PMID:
14611841
[PubMed - indexed for MEDLINE]
11.

Biochemical characterization of human glutamate carboxypeptidase III.

Hlouchová K, Barinka C, Klusák V, Sácha P, Mlcochová P, Majer P, Rulísek L, Konvalinka J.

J Neurochem. 2007 May;101(3):682-96. Epub 2007 Jan 4.

PMID:
17241121
[PubMed - indexed for MEDLINE]
12.

Design, synthesis, and pharmacological evaluation of glutamate carboxypeptidase II (GCPII) inhibitors based on thioalkylbenzoic acid scaffolds.

Stoermer D, Vitharana D, Hin N, Delahanty G, Duvall B, Ferraris DV, Grella BS, Hoover R, Rojas C, Shanholtz MK, Smith KP, Stathis M, Wu Y, Wozniak KM, Slusher BS, Tsukamoto T.

J Med Chem. 2012 Jun 28;55(12):5922-32. doi: 10.1021/jm300488m. Epub 2012 Jun 12.

PMID:
22642259
[PubMed - indexed for MEDLINE]
13.

Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity.

Plechanovová A, Byun Y, Alquicer G, Skultétyová L, Mlčochová P, Němcová A, Kim HJ, Navrátil M, Mease R, Lubkowski J, Pomper M, Konvalinka J, Rulíšek L, Bařinka C.

J Med Chem. 2011 Nov 10;54(21):7535-46. doi: 10.1021/jm200807m. Epub 2011 Oct 11.

PMID:
21923190
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

Tyrosine kinase inhibitors. 6. Structure-activity relationships among N- and 3-substituted 2,2'-diselenobis(1H-indoles) for inhibition of protein tyrosine kinases and comparative in vitro and in vivo studies against selected sulfur congeners.

Showalter HD, Sercel AD, Leja BM, Wolfangel CD, Ambroso LA, Elliott WL, Fry DW, Kraker AJ, Howard CT, Lu GH, Moore CW, Nelson JM, Roberts BJ, Vincent PW, Denny WA, Thompson AM.

J Med Chem. 1997 Feb 14;40(4):413-26.

PMID:
9046331
[PubMed - indexed for MEDLINE]
15.

Mapping of the active site of glutamate carboxypeptidase II by site-directed mutagenesis.

Mlcochová P, Plechanovová A, Barinka C, Mahadevan D, Saldanha JW, Rulísek L, Konvalinka J.

FEBS J. 2007 Sep;274(18):4731-41. Epub 2007 Aug 21.

PMID:
17714508
[PubMed - indexed for MEDLINE]
16.

Amino acids at the N- and C-termini of human glutamate carboxypeptidase II are required for enzymatic activity and proper folding.

Barinka C, Mlcochová P, Sácha P, Hilgert I, Majer P, Slusher BS, Horejsí V, Konvalinka J.

Eur J Biochem. 2004 Jul;271(13):2782-90.

PMID:
15206943
[PubMed - indexed for MEDLINE]
Free Article
17.

Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer.

Mesters JR, Barinka C, Li W, Tsukamoto T, Majer P, Slusher BS, Konvalinka J, Hilgenfeld R.

EMBO J. 2006 Mar 22;25(6):1375-84. Epub 2006 Feb 9.

PMID:
16467855
[PubMed - indexed for MEDLINE]
Free PMC Article
18.

Pyrazole-based cathepsin S inhibitors with improved cellular potency.

Wei J, Pio BA, Cai H, Meduna SP, Sun S, Gu Y, Jiang W, Thurmond RL, Karlsson L, Edwards JP.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5525-8. Epub 2007 Aug 22.

PMID:
17822900
[PubMed - indexed for MEDLINE]
19.

Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity.

Barinka C, Sácha P, Sklenár J, Man P, Bezouska K, Slusher BS, Konvalinka J.

Protein Sci. 2004 Jun;13(6):1627-35.

PMID:
15152093
[PubMed - indexed for MEDLINE]
Free PMC Article
20.

Tyrosine kinase inhibitors. 3. Structure-activity relationships for inhibition of protein tyrosine kinases by nuclear-substituted derivatives of 2,2'-dithiobis(1-methyl-N-phenyl-1H-indole-3-carboxamide).

Rewcastle GW, Palmer BD, Dobrusin EM, Fry DW, Kraker AJ, Denny WA.

J Med Chem. 1994 Jun 24;37(13):2033-42.

PMID:
8027985
[PubMed - indexed for MEDLINE]

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