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Items: 40

1.

AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.

Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE.

Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Erratum in: Cancer Discov. 2019 Jul;9(7):980.

PMID:
30254093
2.

Discovery of AM-6226: A Potent and Orally Bioavailable GPR40 Full Agonist That Displays Efficacy in Nonhuman Primates.

Brown SP, Dransfield P, Vimolratana M, Zhu L, Luo J, Zhang J, Jiao X, Pattaropong V, Wong S, Zhuang R, Swaminath G, Houze JB, Lin DC.

ACS Med Chem Lett. 2018 Jun 6;9(7):757-760. doi: 10.1021/acsmedchemlett.8b00213. eCollection 2018 Jul 12.

3.

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.

4.

5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.

Kohn TJ, Du X, Lai S, Xiong Y, Komorowski R, Veniant M, Fu Z, Jiao X, Pattaropong V, Chow D, Cardozo M, Jin L, Conn M, DeWolf WE Jr, Kraser CF, Hinklin RJ, Boys ML, Medina JC, Houze J, Dransfield P, Coward P.

ACS Med Chem Lett. 2016 Jun 1;7(7):666-70. doi: 10.1021/acsmedchemlett.6b00145. eCollection 2016 Jul 14.

5.

Discovery of the imidazole-derived GPR40 agonist AM-3189.

Ma Z, Lin DC, Sharma R, Liu J, Zhu L, Li AR, Kohn T, Wang Y, Liu JJ, Bartberger MD, Medina JC, Zhuang R, Li F, Zhang J, Luo J, Wong S, Tonn GR, Houze JB.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):15-20. doi: 10.1016/j.bmcl.2015.11.050. Epub 2015 Nov 17.

PMID:
26620255
6.

C5-Alkyl-2-methylurea-Substituted Pyridines as a New Class of Glucokinase Activators.

Du X, Hinklin RJ, Xiong Y, Dransfield P, Park J, Kohn TJ, Pattaropong V, Lai S, Fu Z, Jiao X, Chow D, Jin L, Davda J, Veniant MM, Anderson DA, Baer BR, Bencsik JR, Boyd SA, Chicarelli MJ, Mohr PJ, Wang B, Condroski KR, DeWolf WE, Conn M, Tran T, Yang J, Aicher TD, Medina JC, Coward P, Houze JB.

ACS Med Chem Lett. 2014 Nov 22;5(12):1284-9. doi: 10.1021/ml500341w. eCollection 2014 Dec 11.

7.

Convenient route to secondary sulfinates: application to the stereospecific synthesis of α-C-chiral sulfonamides.

Johnson MG, Gribble MW Jr, Houze JB, Paras NA.

Org Lett. 2014 Dec 5;16(23):6248-51. doi: 10.1021/ol503208z. Epub 2014 Nov 21.

PMID:
25415837
8.

Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.

Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.

J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4.

PMID:
25384157
9.

Discovery of 2-pyridylureas as glucokinase activators.

Hinklin RJ, Aicher TD, Anderson DA, Baer BR, Boyd SA, Condroski KR, DeWolf WE Jr, Kraser CF, McVean M, Rhodes SP, Sturgis HL, Voegtli WC, Williams L, Houze JB.

J Med Chem. 2014 Oct 9;57(19):8180-6. doi: 10.1021/jm501204z. Epub 2014 Sep 17.

PMID:
25203462
10.

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.

11.

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.

12.

Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.

Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A, Liu Q, Murakoshi M, Nara F, Oda K, Okuyama R, Reagan JD, Watanabe N, Yamazaki M, Xiong Y, Zhang Y, Zhuang R, Lin DC, Houze JB, Medina JC, Li L.

ACS Med Chem Lett. 2013 May 1;4(9):829-34. doi: 10.1021/ml4000854. eCollection 2013 Sep 12.

13.

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.

14.

Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.

Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC.

J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27.

PMID:
24601644
15.

Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.

Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.

J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4.

PMID:
24548297
16.

Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.

Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC.

J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5.

PMID:
24456472
17.

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.

PMID:
23403053
18.

Discovery of INT131: a selective PPARγ modulator that enhances insulin sensitivity.

Taygerly JP, McGee LR, Rubenstein SM, Houze JB, Cushing TD, Li Y, Motani A, Chen JL, Frankmoelle W, Ye G, Learned MR, Jaen J, Miao S, Timmermans PB, Thoolen M, Kearney P, Flygare J, Beckmann H, Weiszmann J, Lindstrom M, Walker N, Liu J, Biermann D, Wang Z, Hagiwara A, Iida T, Aramaki H, Kitao Y, Shinkai H, Furukawa N, Nishiu J, Nakamura M.

Bioorg Med Chem. 2013 Feb 15;21(4):979-92. doi: 10.1016/j.bmc.2012.11.058. Epub 2012 Dec 10.

PMID:
23294830
19.

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.

20.

Evaluating insulin secretagogues in a humanized mouse model with functional human islets.

Luo J, Nguyen K, Chen M, Tran T, Hao J, Tian B, Rulifson IC, Zhang Y, Tian L, Zhang Y, Lopez E, Lin DC, Wang Y, Ma Z, Houze J, Guo Z.

Metabolism. 2013 Jan;62(1):90-9. doi: 10.1016/j.metabol.2012.07.010. Epub 2012 Sep 13.

PMID:
22982177
21.

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.

22.

Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.

Du X, Kim YJ, Lai S, Chen X, Lizarzaburu M, Turcotte S, Fu Z, Liu Q, Zhang Y, Motani A, Oda K, Okuyama R, Nara F, Murakoshi M, Fu A, Reagan JD, Fan P, Xiong Y, Shen W, Li L, Houze J, Medina JC.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6218-23. doi: 10.1016/j.bmcl.2012.08.015. Epub 2012 Aug 10. Erratum in: Bioorg Med Chem Lett. 2012 Dec 15;22(24):7750.

PMID:
22926069
23.

Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.

Lizarzaburu M, Turcotte S, Du X, Duquette J, Fu A, Houze J, Li L, Liu J, Murakoshi M, Oda K, Okuyama R, Nara F, Reagan J, Yu M, Medina JC.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5942-7. doi: 10.1016/j.bmcl.2012.07.063. Epub 2012 Jul 23.

PMID:
22884988
24.

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.

25.

AMG 837: a potent, orally bioavailable GPR40 agonist.

Houze JB, Zhu L, Sun Y, Akerman M, Qiu W, Zhang AJ, Sharma R, Schmitt M, Wang Y, Liu J, Liu J, Medina JC, Reagan JD, Luo J, Tonn G, Zhang J, Lu JY, Chen M, Lopez E, Nguyen K, Yang L, Tang L, Tian H, Shuttleworth SJ, Lin DC.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70. doi: 10.1016/j.bmcl.2011.10.118. Epub 2011 Nov 6.

PMID:
22217876
26.

AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents.

Lin DC, Zhang J, Zhuang R, Li F, Nguyen K, Chen M, Tran T, Lopez E, Lu JY, Li XN, Tang L, Tonn GR, Swaminath G, Reagan JD, Chen JL, Tian H, Lin YJ, Houze JB, Luo J.

PLoS One. 2011;6(11):e27270. doi: 10.1371/journal.pone.0027270. Epub 2011 Nov 8.

27.

Optimization of triazoles as novel and potent nonphlorizin SGLT2 inhibitors.

Du X, Lizarzaburu M, Turcotte S, Lee T, Greenberg J, Shan B, Fan P, Ling Y, Medina JC, Houze J.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3774-9. doi: 10.1016/j.bmcl.2011.04.053. Epub 2011 Apr 20.

PMID:
21565497
28.

[Spontaneous hepatic rupture during an uncomplicated twin pregnancy].

Fat BC, Terzibachian JJ, Grisey A, Houzé JP, Faller JP, Leung F, de Lapparent T, Maillet R, Riethmuller D.

Gynecol Obstet Fertil. 2011 Jan;39(1):e7-e10. doi: 10.1016/j.gyobfe.2010.08.003. Epub 2010 Dec 22. French.

PMID:
21183383
29.

Colonoscopy-related esophageal perforation: report of two cases.

Chalumeau C, Facy O, Radais F, Hueber T, Houzé JP, Ortega-Deballon P.

Endoscopy. 2009;41 Suppl 2:E261. doi: 10.1055/s-0029-1215158. Epub 2009 Oct 28. No abstract available.

PMID:
19866419
30.

[A most unusual foreign body in the cecum].

Fennich S, Sader Z, Houzé JP, Kahi S, Picard A, Chazelet C, Febvey JC.

J Chir (Paris). 2008 Nov-Dec;145(6):608-9. French.

PMID:
19106896
31.

[Chronic familial pancreatitis presenting as major pleuro-pulmonary complications].

Houzé JP, Aljundi A, Kahi S, Fennich S, Picard A.

J Chir (Paris). 2006 Jul-Aug;143(4):268-70. French. No abstract available.

PMID:
17088733
32.

Optimization of 2-aminothiazole derivatives as CCR4 antagonists.

Wang X, Xu F, Xu Q, Mahmud H, Houze J, Zhu L, Akerman M, Tonn G, Tang L, McMaster BE, Dairaghi DJ, Schall TJ, Collins TL, Medina JC.

Bioorg Med Chem Lett. 2006 May 15;16(10):2800-3. Epub 2006 Feb 23.

PMID:
16497499
33.

Effects of peroxisome proliferator-activated receptor alpha/delta agonists on HDL-cholesterol in vervet monkeys.

Wallace JM, Schwarz M, Coward P, Houze J, Sawyer JK, Kelley KL, Chai A, Rudel LL.

J Lipid Res. 2005 May;46(5):1009-16. Epub 2005 Feb 16.

34.

[Malignant thymoma: a strange goiter].

Forterre O, Houzé JP, Picard A.

J Chir (Paris). 2001 Aug;138(4):232. French. No abstract available.

PMID:
11557903
35.

[A case of acute colonic-sigmoidorectal invagination in the adult].

Mattei F, Houze JP, Bacon, Herve L, Marsilj C.

Chirurgie. 1973 Nov 13;99(11):827-9. French. No abstract available.

PMID:
4792559
36.

[Perforation of Wirsung's duct during chronic calcifying pancreatitis. A case].

Sarles JC, Giuly J, Houze JP.

Nouv Presse Med. 1972 Jun 24;1(26):1777-9. French. No abstract available.

PMID:
5054017
37.

[Hemorrhages from duodenal ulcers. Etiological and therapeutic considerations. (Apropos of 133 cases of moderate and extensive loss)].

Bourde J, Assadourian R, Raynaud B, Houze JP, Randrianonimandimby J, Lamy J.

J Chir (Paris). 1972 May-Jun;103(5):465-78. French. No abstract available.

PMID:
4653424
38.

Carotid sinus nerve stimulation in angina pectoris.

Courbier R, Torresani J, Houzé J, Jouve A, Henry E.

J Cardiovasc Surg (Torino). 1971 May-Jun;12(3):231-4. No abstract available.

PMID:
4997075
39.

[Surgical problems raised by stimulation of the carotid sinus].

Jausseran JM, Houze JP, Courbier R, Henry E.

Ann Cardiol Angeiol (Paris). 1971 Mar-Apr;20(2):123-5. French. No abstract available.

PMID:
5575556
40.

[Aortic orifice in the diaphragm].

Mambrini A, Argême M, Houzé JP, Isman H.

C R Assoc Anat. 1970 Sep;148:433-41. French. No abstract available.

PMID:
5004441

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