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Items: 11


Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394.

Dransfield PJ, Pattaropong V, Lai S, Fu Z, Kohn TJ, Du X, Cheng A, Xiong Y, Komorowski R, Jin L, Conn M, Tien E, DeWolf WE Jr, Hinklin RJ, Aicher TD, Kraser CF, Boyd SA, Voegtli WC, Condroski KR, Veniant-Ellison M, Medina JC, Houze J, Coward P.

ACS Med Chem Lett. 2016 May 23;7(7):714-8. doi: 10.1021/acsmedchemlett.6b00140. eCollection 2016 Jul 14.


Optimization of GPR40 Agonists for Type 2 Diabetes.

Liu JJ, Wang Y, Ma Z, Schmitt M, Zhu L, Brown SP, Dransfield PJ, Sun Y, Sharma R, Guo Q, Zhuang R, Zhang J, Luo J, Tonn GR, Wong S, Swaminath G, Medina JC, Lin DC, Houze JB.

ACS Med Chem Lett. 2014 Feb 6;5(5):517-21. doi: 10.1021/ml400501x. eCollection 2014 May 8.


Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.

Du X, Dransfield PJ, Lin DC, Wong S, Wang Y, Wang Z, Kohn T, Yu M, Brown SP, Vimolratana M, Zhu L, Li AR, Su Y, Jiao X, Liu JJ, Swaminath G, Tran T, Luo J, Zhuang R, Zhang J, Guo Q, Li F, Connors R, Medina JC, Houze JB.

ACS Med Chem Lett. 2014 Feb 3;5(4):384-9. doi: 10.1021/ml4005123. eCollection 2014 Apr 10.


Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.

Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC.

ACS Med Chem Lett. 2013 May 7;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13.


Activation of FFA1 mediates GLP-1 secretion in mice. Evidence for allosterism at FFA1.

Xiong Y, Swaminath G, Cao Q, Yang L, Guo Q, Salomonis H, Lu J, Houze JB, Dransfield PJ, Wang Y, Liu JJ, Wong S, Schwandner R, Steger F, Baribault H, Liu L, Coberly S, Miao L, Zhang J, Lin DC, Schwarz M.

Mol Cell Endocrinol. 2013 Apr 30;369(1-2):119-29. doi: 10.1016/j.mce.2013.01.009. Epub 2013 Feb 9.


A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.

Luo J, Swaminath G, Brown SP, Zhang J, Guo Q, Chen M, Nguyen K, Tran T, Miao L, Dransfield PJ, Vimolratana M, Houze JB, Wong S, Toteva M, Shan B, Li F, Zhuang R, Lin DC.

PLoS One. 2012;7(10):e46300. doi: 10.1371/journal.pone.0046300. Epub 2012 Oct 9.


Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.

Brown SP, Dransfield PJ, Vimolratana M, Jiao X, Zhu L, Pattaropong V, Sun Y, Liu J, Luo J, Zhang J, Wong S, Zhuang R, Guo Q, Li F, Medina JC, Swaminath G, Lin DC, Houze JB.

ACS Med Chem Lett. 2012 Aug 15;3(9):726-30. doi: 10.1021/ml300133f. eCollection 2012 Sep 13.


Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.

Lin DC, Guo Q, Luo J, Zhang J, Nguyen K, Chen M, Tran T, Dransfield PJ, Brown SP, Houze J, Vimolratana M, Jiao XY, Wang Y, Birdsall NJ, Swaminath G.

Mol Pharmacol. 2012 Nov;82(5):843-59. doi: 10.1124/mol.112.079640. Epub 2012 Aug 2.


Highly regioselective Diels-Alder reactions toward oroidin alkaloids: use of a tosylvinyl moiety as a nitrogen masking group with adjustable electronics.

Dransfield PJ, Wang S, Dilley A, Romo D.

Org Lett. 2005 Apr 28;7(9):1679-82. Erratum in: Org Lett. 2005 Sep 1;7(18):4065.


Preparation and reactivity of imino glycals: stereocontrolled, divergent approach to imino sugars.

Dransfield PJ, Gore PM, Prokes I, Shipman M, Slawin AM.

Org Biomol Chem. 2003 Aug 7;1(15):2723-33.


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