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Items: 18

1.
2.

Neutral sphingomyelinase 2 inhibitors based on the 4-(1H-imidazol-2-yl)-2,6-dialkoxyphenol scaffold.

Stepanek O, Hin N, Thomas AG, Dash RP, Alt J, Rais R, Rojas C, Slusher BS, Tsukamoto T.

Eur J Med Chem. 2019 May 15;170:276-289. doi: 10.1016/j.ejmech.2019.03.015. Epub 2019 Mar 9.

PMID:
30921693
3.

Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.

Barinka C, Novakova Z, Hin N, Bím D, Ferraris DV, Duvall B, Kabarriti G, Tsukamoto R, Budesinsky M, Motlova L, Rojas C, Slusher BS, Rokob TA, Rulíšek L, Tsukamoto T.

Bioorg Med Chem. 2019 Jan 15;27(2):255-264. doi: 10.1016/j.bmc.2018.11.022. Epub 2018 Nov 14.

PMID:
30552009
4.

DPTIP, a newly identified potent brain penetrant neutral sphingomyelinase 2 inhibitor, regulates astrocyte-peripheral immune communication following brain inflammation.

Rojas C, Barnaeva E, Thomas AG, Hu X, Southall N, Marugan J, Chaudhuri AD, Yoo SW, Hin N, Stepanek O, Wu Y, Zimmermann SC, Gadiano AG, Tsukamoto T, Rais R, Haughey N, Ferrer M, Slusher BS.

Sci Rep. 2018 Dec 7;8(1):17715. doi: 10.1038/s41598-018-36144-2.

5.

Structural basis for potent inhibition of d-amino acid oxidase by thiophene carboxylic acids.

Kato Y, Hin N, Maita N, Thomas AG, Kurosawa S, Rojas C, Yorita K, Slusher BS, Fukui K, Tsukamoto T.

Eur J Med Chem. 2018 Nov 5;159:23-34. doi: 10.1016/j.ejmech.2018.09.040. Epub 2018 Sep 18.

PMID:
30265959
6.

Oral administration of D-alanine in monkeys robustly increases plasma and cerebrospinal fluid levels but experimental D-amino acid oxidase inhibitors had minimal effect.

Rojas C, Alt J, Ator NA, Wilmoth H, Rais R, Hin N, DeVivo M, Popiolek M, Tsukamoto T, Slusher BS.

J Psychopharmacol. 2016 Sep;30(9):887-95. doi: 10.1177/0269881116652586. Epub 2016 Jun 10.

PMID:
27287825
7.

Unprecedented Binding Mode of Hydroxamate-Based Inhibitors of Glutamate Carboxypeptidase II: Structural Characterization and Biological Activity.

Novakova Z, Wozniak K, Jancarik A, Rais R, Wu Y, Pavlicek J, Ferraris D, Havlinova B, Ptacek J, Vavra J, Hin N, Rojas C, Majer P, Slusher BS, Tsukamoto T, Barinka C.

J Med Chem. 2016 May 26;59(10):4539-50. doi: 10.1021/acs.jmedchem.5b01806. Epub 2016 Apr 25.

PMID:
27074627
8.

D-Amino acid oxidase inhibitors based on the 5-hydroxy-1,2,4-triazin-6(1H)-one scaffold.

Hin N, Duvall B, Berry JF, Ferraris DV, Rais R, Alt J, Rojas C, Slusher BS, Tsukamoto T.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2088-91. doi: 10.1016/j.bmcl.2016.02.068. Epub 2016 Feb 23.

9.

D-Amino-Acid Oxidase Inhibition Increases D-Serine Plasma Levels in Mouse But not in Monkey or Dog.

Rojas C, Alt J, Ator NA, Thomas AG, Wu Y, Hin N, Wozniak K, Ferraris D, Rais R, Tsukamoto T, Slusher BS.

Neuropsychopharmacology. 2016 May;41(6):1610-9. doi: 10.1038/npp.2015.319. Epub 2015 Oct 16.

10.

6-Hydroxy-1,2,4-triazine-3,5(2H,4H)-dione Derivatives as Novel D-Amino Acid Oxidase Inhibitors.

Hin N, Duvall B, Ferraris D, Alt J, Thomas AG, Rais R, Rojas C, Wu Y, Wozniak KM, Slusher BS, Tsukamoto T.

J Med Chem. 2015 Sep 24;58(18):7258-72. doi: 10.1021/acs.jmedchem.5b00482. Epub 2015 Sep 3.

11.

Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.

Hin N, Alt J, Zimmermann SC, Delahanty G, Ferraris DV, Rojas C, Li F, Liu Q, Dong X, Slusher BS, Tsukamoto T.

Bioorg Med Chem. 2014 Nov 1;22(21):5831-7. doi: 10.1016/j.bmc.2014.09.025. Epub 2014 Sep 19.

12.

Activation of MrgC receptor inhibits N-type calcium channels in small-diameter primary sensory neurons in mice.

Li Z, He SQ, Xu Q, Yang F, Tiwari V, Liu Q, Tang Z, Han L, Chu YX, Wang Y, Hin N, Tsukamoto T, Slusher B, Guan X, Wei F, Raja SN, Dong X, Guan Y.

Pain. 2014 Aug;155(8):1613-21. doi: 10.1016/j.pain.2014.05.008. Epub 2014 May 9.

13.

MrgC agonism at central terminals of primary sensory neurons inhibits neuropathic pain.

He SQ, Li Z, Chu YX, Han L, Xu Q, Li M, Yang F, Liu Q, Tang Z, Wang Y, Hin N, Tsukamoto T, Slusher B, Tiwari V, Shechter R, Wei F, Raja SN, Dong X, Guan Y.

Pain. 2014 Mar;155(3):534-44. doi: 10.1016/j.pain.2013.12.008. Epub 2013 Dec 11.

14.

Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase.

Raje M, Hin N, Duvall B, Ferraris DV, Berry JF, Thomas AG, Alt J, Rojas C, Slusher BS, Tsukamoto T.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3910-3. doi: 10.1016/j.bmcl.2013.04.062. Epub 2013 May 1.

15.

Synthesis and SAR of 1-hydroxy-1H-benzo[d]imidazol-2(3H)-ones as Inhibitors of D-Amino Acid Oxidase.

Berry JF, Ferraris DV, Duvall B, Hin N, Rais R, Alt J, Thomas AG, Rojas C, Hashimoto K, Slusher BS, Tsukamoto T.

ACS Med Chem Lett. 2012 Oct 11;3(10):839-843. Epub 2012 Sep 16.

16.

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
17.

Inhibition of xc⁻ transporter-mediated cystine uptake by sulfasalazine analogs.

Shukla K, Thomas AG, Ferraris DV, Hin N, Sattler R, Alt J, Rojas C, Slusher BS, Tsukamoto T.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6184-7. doi: 10.1016/j.bmcl.2011.07.081. Epub 2011 Aug 12.

PMID:
21889337
18.

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.

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