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Page 1
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.
Tang H, Walsh SP, Yan Y, de Jesus RK, Shahripour A, Teumelsan N, Zhu Y, Ha S, Owens KA, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest BT, Bailey T, Brochu R, Alonso-Galicia M, Kaczorowski GJ, Roy S, Yang L, Mills SG, Garcia ML, Pasternak A. Tang H, et al. Among authors: de jesus rk. ACS Med Chem Lett. 2012 Mar 28;3(5):367-72. doi: 10.1021/ml3000066. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900480 Free PMC article.
Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.
Tang H, Yan Y, Feng Z, de Jesus RK, Yang L, Levorse DA, Owens KA, Akiyama TE, Bergeron R, Castriota GA, Doebber TW, Ellsworth KP, Lassman ME, Li C, Wu MS, Zhang BB, Chapman KT, Mills SG, Berger JP, Pasternak A. Tang H, et al. Among authors: de jesus rk. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6088-92. doi: 10.1016/j.bmcl.2010.08.047. Epub 2010 Aug 20. Bioorg Med Chem Lett. 2010. PMID: 20832306
Pharmacologic inhibition of the renal outer medullary potassium channel causes diuresis and natriuresis in the absence of kaliuresis.
Garcia ML, Priest BT, Alonso-Galicia M, Zhou X, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Liu J, Swensen A, Pai LY, Xiao J, Hernandez M, Hoagland K, Owens K, Tang H, de Jesus RK, Roy S, Kaczorowski GJ, Pasternak A. Garcia ML, et al. Among authors: de jesus rk. J Pharmacol Exp Ther. 2014 Jan;348(1):153-64. doi: 10.1124/jpet.113.208603. Epub 2013 Oct 18. J Pharmacol Exp Ther. 2014. PMID: 24142912
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
Pasternak A, Feng Z, de Jesus R, Ye Z, He S, Dobbelaar P, Bradley SA, Chicchi GG, Tsao KL, Trusca D, Eiermann GJ, Li C, Feng Y, Wu M, Shao Q, Zhang BB, Nargund R, Mills SG, Howard AD, Yang L, Zhou YP. Pasternak A, et al. ACS Med Chem Lett. 2012 Feb 27;3(4):289-93. doi: 10.1021/ml200272z. eCollection 2012 Apr 12. ACS Med Chem Lett. 2012. PMID: 24900466 Free PMC article.
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900499 Free PMC article.
Selective small-molecule inhibition of an RNA structural element.
Howe JA, Wang H, Fischmann TO, Balibar CJ, Xiao L, Galgoci AM, Malinverni JC, Mayhood T, Villafania A, Nahvi A, Murgolo N, Barbieri CM, Mann PA, Carr D, Xia E, Zuck P, Riley D, Painter RE, Walker SS, Sherborne B, de Jesus R, Pan W, Plotkin MA, Wu J, Rindgen D, Cummings J, Garlisi CG, Zhang R, Sheth PR, Gill CJ, Tang H, Roemer T. Howe JA, et al. Nature. 2015 Oct 29;526(7575):672-7. doi: 10.1038/nature15542. Epub 2015 Sep 30. Nature. 2015. PMID: 26416753
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.
Walsh SP, Shahripour A, Tang H, de Jesus RK, Teumelsan N, Zhu Y, Frie J, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Garcia ML, Pasternak A. Walsh SP, et al. Among authors: de jesus rk. Bioorg Med Chem Lett. 2016 May 1;26(9):2339-43. doi: 10.1016/j.bmcl.2016.03.035. Epub 2016 Mar 12. Bioorg Med Chem Lett. 2016. PMID: 27017115
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A. Zhu Y, et al. Among authors: de jesus rk. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27839686
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J. Mandal M, et al. J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28322556
24 results