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An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.
Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN. Thorneloe KS, et al. Among authors: cheung m. Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276. Sci Transl Med. 2012. PMID: 23136043
TRPV4 inhibition counteracts edema and inflammation and improves pulmonary function and oxygen saturation in chemically induced acute lung injury.
Balakrishna S, Song W, Achanta S, Doran SF, Liu B, Kaelberer MM, Yu Z, Sui A, Cheung M, Leishman E, Eidam HS, Ye G, Willette RN, Thorneloe KS, Bradshaw HB, Matalon S, Jordt SE. Balakrishna S, et al. Among authors: cheung m. Am J Physiol Lung Cell Mol Physiol. 2014 Jul 15;307(2):L158-72. doi: 10.1152/ajplung.00065.2014. Epub 2014 May 16. Am J Physiol Lung Cell Mol Physiol. 2014. PMID: 24838754 Free PMC article.
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Brooks CA, Barton LS, Behm DJ, Eidam HS, Fox RM, Hammond M, Hoang TH, Holt DA, Hilfiker MA, Lawhorn BG, Patterson JR, Stoy P, Roethke TJ, Ye G, Zhao S, Thorneloe KS, Goodman KB, Cheung M. Brooks CA, et al. Among authors: cheung m. ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. doi: 10.1021/acsmedchemlett.9b00274. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413810 Free PMC article.
Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.
Goodman KB, Bury MJ, Cheung M, Cichy-Knight MA, Dowdell SE, Dunn AK, Lee D, Lieby JA, Moore ML, Scherzer DA, Sha D, Suarez DP, Murphy DJ, Harpel MR, Manas ES, McNulty DE, Annan RS, Matico RE, Schwartz BK, Trill JJ, Sweitzer TD, Wang DY, Keller PM, Krawiec JA, Jaye MC. Goodman KB, et al. Among authors: cheung m. Bioorg Med Chem Lett. 2009 Jan 1;19(1):27-30. doi: 10.1016/j.bmcl.2008.11.033. Epub 2008 Nov 14. Bioorg Med Chem Lett. 2009. PMID: 19058966
Exploring the Potential of RET Kinase Inhibition for Irritable Bowel Syndrome: A Preclinical Investigation in Rodent Models of Colonic Hypersensitivity.
Russell JP, Mohammadi E, Ligon CO, Johnson AC, Gershon MD, Rao M, Shen Y, Chan CC, Eidam HS, DeMartino MP, Cheung M, Oliff AI, Kumar S, Greenwood-Van Meerveld B. Russell JP, et al. Among authors: cheung m. J Pharmacol Exp Ther. 2019 Feb;368(2):299-307. doi: 10.1124/jpet.118.252973. Epub 2018 Nov 9. J Pharmacol Exp Ther. 2019. PMID: 30413627 Free PMC article.
Enteric RET inhibition attenuates gastrointestinal secretion and motility via cholinergic signaling in rat colonic mucosal preparations.
Russell JP, Mohammadi E, Ligon C, Latorre R, Johnson AC, Hoang B, Krull D, Ho MW, Eidam HS, DeMartino MP, Cheung M, Oliff AI, Kumar S, Greenwood-Van Meerveld B. Russell JP, et al. Among authors: cheung m. Neurogastroenterol Motil. 2019 Apr;31(4):e13479. doi: 10.1111/nmo.13479. Epub 2018 Oct 12. Neurogastroenterol Motil. 2019. PMID: 30311722
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: cheung m. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
2,108 results