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Page 1
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.
Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS. Cheung M, et al. Among authors: eidam hs. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523109 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: eidam hs. 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.
Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.
Kallander LS, Washburn D, Hilfiker MA, Eidam HS, Lawhorn BG, Prendergast J, Fox R, Dowdell S, Manns S, Hoang T, Zhao S, Ye G, Hammond M, Holt DA, Roethke T, Hong X, Reid RA, Gampe R, Zhang H, Diaz E, Rendina AR, Quinn AM, Willette B. Kallander LS, et al. Among authors: eidam hs. ACS Med Chem Lett. 2018 Jul 2;9(7):736-740. doi: 10.1021/acsmedchemlett.8b00173. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034610 Free PMC article.
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: eidam hs. 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: eidam hs. 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.
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: eidam hs. Neurogastroenterol Motil. 2019 Apr;31(4):e13479. doi: 10.1111/nmo.13479. Epub 2018 Oct 12. Neurogastroenterol Motil. 2019. PMID: 30311722
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: eidam hs. 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.
Targeting IRAK4 for Degradation with PROTACs.
Nunes J, McGonagle GA, Eden J, Kiritharan G, Touzet M, Lewell X, Emery J, Eidam H, Harling JD, Anderson NA. Nunes J, et al. ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085. doi: 10.1021/acsmedchemlett.9b00219. eCollection 2019 Jul 11. ACS Med Chem Lett. 2019. PMID: 31312412 Free PMC article.
12 results