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Items: 1 to 20 of 135

1.

LX2761, a Sodium/Glucose Cotransporter 1 Inhibitor Restricted to the Intestine, Improves Glycemic Control in Mice.

Powell DR, Smith MG, Doree DD, Harris AL, Greer J, DaCosta CM, Thompson A, Jeter-Jones S, Xiong W, Carson KG, Goodwin NC, Harrison BA, Rawlins DB, Strobel ED, Gopinathan S, Wilson A, Mseeh F, Zambrowicz B, Ding ZM.

J Pharmacol Exp Ther. 2017 Jul;362(1):85-97. doi: 10.1124/jpet.117.240820. Epub 2017 Apr 25.

PMID:
28442582
2.

Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.

Ahn S, Kahsai AW, Pani B, Wang QT, Zhao S, Wall AL, Strachan RT, Staus DP, Wingler LM, Sun LD, Sinnaeve J, Choi M, Cho T, Xu TT, Hansen GM, Burnett MB, Lamerdin JE, Bassoni DL, Gavino BJ, Husemoen G, Olsen EK, Franch T, Costanzi S, Chen X, Lefkowitz RJ.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713. doi: 10.1073/pnas.1620645114. Epub 2017 Jan 27.

3.

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.

Goodwin NC, Ding ZM, Harrison BA, Strobel ED, Harris AL, Smith M, Thompson AY, Xiong W, Mseeh F, Bruce DJ, Diaz D, Gopinathan S, Li L, O'Neill E, Thiel M, Wilson AG, Carson KG, Powell DR, Rawlins DB.

J Med Chem. 2017 Jan 26;60(2):710-721. doi: 10.1021/acs.jmedchem.6b01541. Epub 2017 Jan 17.

PMID:
28045524
4.

Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome.

Kulke MH, Hörsch D, Caplin ME, Anthony LB, Bergsland E, Öberg K, Welin S, Warner RR, Lombard-Bohas C, Kunz PL, Grande E, Valle JW, Fleming D, Lapuerta P, Banks P, Jackson S, Zambrowicz B, Sands AT, Pavel M.

J Clin Oncol. 2017 Jan;35(1):14-23. Epub 2016 Oct 28.

PMID:
27918724
5.

Norrin/Frizzled4 signalling in the preneoplastic niche blocks medulloblastoma initiation.

Bassett EA, Tokarew N, Allemano EA, Mazerolle C, Morin K, Mears AJ, McNeill B, Ringuette R, Campbell C, Smiley S, Pokrajac NT, Dubuc AM, Ramaswamy V, Northcott PA, Remke M, Monnier PP, Potter D, Paes K, Kirkpatrick LL, Coker KJ, Rice DS, Perez-Iratxeta C, Taylor MD, Wallace VA.

Elife. 2016 Nov 8;5. pii: e16764. doi: 10.7554/eLife.16764.

6.

Combined Deletion of Slc30a7 and Slc30a8 Unmasks a Critical Role for ZnT8 in Glucose-Stimulated Insulin Secretion.

Syring KE, Boortz KA, Oeser JK, Ustione A, Platt KA, Shadoan MK, McGuinness OP, Piston DW, Powell DR, O'Brien RM.

Endocrinology. 2016 Dec;157(12):4534-4541. Epub 2016 Oct 18.

PMID:
27754787
7.

Correction of lung inflammation in a F508del CFTR murine cystic fibrosis model by the sphingosine-1-phosphate lyase inhibitor LX2931.

Veltman M, Stolarczyk M, Radzioch D, Wojewodka G, De Sanctis JB, Dik WA, Dzyubachyk O, Oravecz T, de Kleer I, Scholte BJ.

Am J Physiol Lung Cell Mol Physiol. 2016 Nov 1;311(5):L1000-L1014. doi: 10.1152/ajplung.00298.2016. Epub 2016 Sep 23.

PMID:
27663991
8.

Dapagliflozin Binds Specifically to Sodium-Glucose Cotransporter 2 in the Proximal Renal Tubule.

Ghezzi C, Yu AS, Hirayama BA, Kepe V, Liu J, Scafoglio C, Powell DR, Huang SC, Satyamurthy N, Barrio JR, Wright EM.

J Am Soc Nephrol. 2017 Mar;28(3):802-810. doi: 10.1681/ASN.2016050510. Epub 2016 Sep 12.

PMID:
27620988
9.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

10.

Fatty acid desaturase 1 knockout mice are lean with improved glycemic control and decreased development of atheromatous plaque.

Powell DR, Gay JP, Smith M, Wilganowski N, Harris A, Holland A, Reyes M, Kirkham L, Kirkpatrick LL, Zambrowicz B, Hansen G, Platt KA, van Sligtenhorst I, Ding ZM, Desai U.

Diabetes Metab Syndr Obes. 2016 Jun 22;9:185-99. doi: 10.2147/DMSO.S106653. eCollection 2016.

11.

Efficacy and Safety of Proton-Pump Inhibitors in High-Risk Cardiovascular Subsets of the COGENT Trial.

Vaduganathan M, Cannon CP, Cryer BL, Liu Y, Hsieh WH, Doros G, Cohen M, Lanas A, Schnitzer TJ, Shook TL, Lapuerta P, Goldsmith MA, Laine L, Bhatt DL; COGENT Investigators.

Am J Med. 2016 Sep;129(9):1002-5. doi: 10.1016/j.amjmed.2016.03.042. Epub 2016 Apr 30.

PMID:
27143321
12.

Sphingosine-1-phosphate phosphatase 2 promotes disruption of mucosal integrity, and contributes to ulcerative colitis in mice and humans.

Huang WC, Liang J, Nagahashi M, Avni D, Yamada A, Maceyka M, Wolen AR, Kordula T, Milstien S, Takabe K, Oravecz T, Spiegel S.

FASEB J. 2016 Aug;30(8):2945-58. doi: 10.1096/fj.201600394R. Epub 2016 Apr 29.

13.

Ischemic preconditioning, retinal neuroprotection and histone deacetylase activities.

Fan J, Alsarraf O, Chou CJ, Yates PW, Goodwin NC, Rice DS, Crosson CE.

Exp Eye Res. 2016 May;146:269-75. doi: 10.1016/j.exer.2016.03.026. Epub 2016 Apr 6.

14.

Patient-reported Symptom Experiences in Patients With Carcinoid Syndrome After Participation in a Study of Telotristat Etiprate: A Qualitative Interview Approach.

Gelhorn HL, Kulke MH, O'Dorisio T, Yang QM, Jackson J, Jackson S, Boehm KA, Law L, Kostelec J, Auguste P, Lapuerta P.

Clin Ther. 2016 Apr;38(4):759-68. doi: 10.1016/j.clinthera.2016.03.002. Epub 2016 Mar 31.

15.

Revisiting the physiological roles of SGLTs and GLUTs using positron emission tomography in mice.

Sala-Rabanal M, Hirayama BA, Ghezzi C, Liu J, Huang SC, Kepe V, Koepsell H, Yu A, Powell DR, Thorens B, Wright EM, Barrio JR.

J Physiol. 2016 Aug 1;594(15):4425-38. doi: 10.1113/JP271904. Epub 2016 May 10.

16.

Proton-Pump Inhibitors Reduce Gastrointestinal Events Regardless of Aspirin Dose in Patients Requiring Dual Antiplatelet Therapy.

Vaduganathan M, Bhatt DL, Cryer BL, Liu Y, Hsieh WH, Doros G, Cohen M, Lanas A, Schnitzer TJ, Shook TL, Lapuerta P, Goldsmith MA, Laine L, Cannon CP; COGENT Investigators.

J Am Coll Cardiol. 2016 Apr 12;67(14):1661-71. doi: 10.1016/j.jacc.2015.12.068. Epub 2016 Mar 21.

17.

Dentin Dysplasia in Notum Knockout Mice.

Vogel P, Read RW, Hansen GM, Powell DR, Kantaputra PN, Zambrowicz B, Brommage R.

Vet Pathol. 2016 Jul;53(4):853-62. doi: 10.1177/0300985815626778. Epub 2016 Feb 29.

PMID:
26926082
18.

Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase.

Tarver JE Jr, Pabba PK, Barbosa J, Han Q, Gardyan MW, Brommage R, Thompson AY, Schmidt JM, Wilson AGE, He W, Lombardo VK, Carson KG.

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1525-1528. doi: 10.1016/j.bmcl.2016.02.021. Epub 2016 Feb 10.

PMID:
26897593
19.

4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.

Han Q, Pabba PK, Barbosa J, Mabon R, Healy JP, Gardyan MW, Terranova KM, Brommage R, Thompson AY, Schmidt JM, Wilson AG, Xu X, Tarver JE Jr, Carson KG.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1184-7. doi: 10.1016/j.bmcl.2016.01.038. Epub 2016 Jan 18.

PMID:
26821819
20.

Spinster 2, a sphingosine-1-phosphate transporter, plays a critical role in inflammatory and autoimmune diseases.

Donoviel MS, Hait NC, Ramachandran S, Maceyka M, Takabe K, Milstien S, Oravecz T, Spiegel S.

FASEB J. 2015 Dec;29(12):5018-28. doi: 10.1096/fj.15-274936. Epub 2015 Aug 31.

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