Tian G - Search Results

1

The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors.

Tian G, Ghanekar SV, Aharony D, Shenvi AB, Jacobs RT, Liu X, Greenberg BD. Tian G, et al. J Biol Chem. 2003 Aug 1;278(31):28968-75. doi: 10.1074/jbc.M300905200. Epub 2003 Apr 28. J Biol Chem. 2003. PMID: 12719412 Free article.

Transition state analogs pepstatin methylester (PME) and L685458 have been shown to inhibit gamma-secretase non-competitively (Tian, G., Sobotka-Briner, C., Zysk, J., Liu, X., Birr, C., Sylvester, M. A., Edwards, P. ...

Transition state analogs pepstatin methylester (PME) and L685458 have been shown to inhibit gamma-secretase non-competitively (Tian, …

2

Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines.

Tian G, Sobotka-Briner CD, Zysk J, Liu X, Birr C, Sylvester MA, Edwards PD, Scott CD, Greenberg BD. Tian G, et al. J Biol Chem. 2002 Aug 30;277(35):31499-505. doi: 10.1074/jbc.M112328200. Epub 2002 Jun 18. J Biol Chem. 2002. PMID: 12072428 Free article.

3

Mechanism of gamma-secretase cleavage activation: is gamma-secretase regulated through autoinhibition involving the presenilin-1 exon 9 loop?

Knappenberger KS, Tian G, Ye X, Sobotka-Briner C, Ghanekar SV, Greenberg BD, Scott CW. Knappenberger KS, et al. Among authors: tian g. Biochemistry. 2004 May 25;43(20):6208-18. doi: 10.1021/bi036072v. Biochemistry. 2004. PMID: 15147205

4

Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.

Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. Among authors: tian g. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862

5

Neurokinin-3 receptor-specific antagonists talnetant and osanetant show distinct mode of action in cellular Ca2+ mobilization but display similar binding kinetics and identical mechanism of binding in ligand cross-competition.

Tian G, Wilkins D, Scott CW. Tian G, et al. Mol Pharmacol. 2007 Mar;71(3):902-11. doi: 10.1124/mol.106.029868. Epub 2006 Dec 15. Mol Pharmacol. 2007. PMID: 17172464

6

Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1.

Varnes JG, Forst JM, Hoerter TN, Holmquist CR, Wilkins DE, Tian G, Jonak G, Wang X, Potts WM, Wood MW, Alhambra C, Brugel TA, Albert JS. Varnes JG, et al. Among authors: tian g. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4878-81. doi: 10.1016/j.bmcl.2010.06.085. Epub 2010 Jun 19. Bioorg Med Chem Lett. 2010. PMID: 20637614

7

Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency.

Tian G, Paschetto KA, Gharahdaghi F, Gordon E, Wilkins DE, Luo X, Scott CW. Tian G, et al. Biochemistry. 2011 Aug 16;50(32):6867-78. doi: 10.1021/bi200552p. Epub 2011 Jul 22. Biochemistry. 2011. PMID: 21728345

8

Biochemical characterization and in vitro activity of AZ513, a noncovalent, reversible, and noncompetitive inhibitor of fatty acid amide hydrolase.

Scott CW, Tian G, Yu XH, Paschetto KA, Wilkins DE, Meury L, Cao CQ, Varnes J, Edwards PD. Scott CW, et al. Among authors: tian g. Eur J Pharmacol. 2011 Sep 30;667(1-3):74-9. doi: 10.1016/j.ejphar.2011.05.052. Epub 2011 Jun 1. Eur J Pharmacol. 2011. PMID: 21645511

9

Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.

Varnes JG, Geschwindner S, Holmquist CR, Forst J, Wang X, Dekker N, Scott CW, Tian G, Wood MW, Albert JS. Varnes JG, et al. Among authors: tian g. Bioorg Med Chem Lett. 2016 Jan 1;26(1):197-202. doi: 10.1016/j.bmcl.2015.10.100. Epub 2015 Nov 11. Bioorg Med Chem Lett. 2016. PMID: 26597534

10

Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.

Varnes JG, Xiong H, Forst JM, Holmquist CR, Ernst GE, Frietze W, Dembofsky B, Andisik DW, Palmer WE, Hinkley L, Steelman GB, Wilkins DE, Tian G, Jonak G, Potts WM, Wang X, Brugel TA, Alhambra C, Wood MW, Veale CA, Albert JS. Varnes JG, et al. Among authors: tian g. Bioorg Med Chem Lett. 2018 Apr 1;28(6):1043-1049. doi: 10.1016/j.bmcl.2018.02.029. Epub 2018 Feb 14. Bioorg Med Chem Lett. 2018. PMID: 29486970

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