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Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
Gopalsamy A, Narayanan A, Liu S, Parikh MD, Kyne RE Jr, Fadeyi O, Tones MA, Cherry JJ, Nabhan JF, LaRosa G, Petersen DN, Menard C, Foley TL, Noell S, Ren Y, Loria PM, Maglich-Goodwin J, Rong H, Jones LH. Gopalsamy A, et al. Among authors: rong h. J Med Chem. 2017 Apr 13;60(7):3094-3108. doi: 10.1021/acs.jmedchem.7b00124. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28257199
Discovery of a novel Kv7 channel opener as a treatment for epilepsy.
Davoren JE, Claffey MM, Snow SL, Reese MR, Arora G, Butler CR, Boscoe BP, Chenard L, DeNinno SL, Drozda SE, Duplantier AJ, Moine L, Rogers BN, Rong S, Schuyten K, Wright AS, Zhang L, Serpa KA, Weber ML, Stolyar P, Whisman TL, Baker K, Tse K, Clark AJ, Rong H, Mather RJ, Lowe JA 3rd. Davoren JE, et al. Among authors: rong s, rong h. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4941-4944. doi: 10.1016/j.bmcl.2015.04.074. Epub 2015 May 1. Bioorg Med Chem Lett. 2015. PMID: 25987375
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. Stock NS, et al. Among authors: rong h. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).
Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF. Hutchinson JH, et al. Among authors: rong h. J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d. J Med Chem. 2009. PMID: 19739647
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Stock N, Baccei C, Bain G, Broadhead A, Chapman C, Darlington J, King C, Lee C, Li Y, Lorrain DS, Prodanovich P, Rong H, Santini A, Zunic J, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: rong h. Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31. Bioorg Med Chem Lett. 2010. PMID: 19914828
Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition.
Chang C, Fonseca KR, Li C, Horner W, Zawadzke LE, Salafia MA, Welch KA, Strick CA, Campbell BM, Gernhardt SS, Rong H, Sawant-Basak A, Liras J, Dounay A, Tuttle JB, Verhoest P, Maurer TS. Chang C, et al. Among authors: rong h. Mol Pharmacol. 2018 Aug;94(2):823-833. doi: 10.1124/mol.118.111625. Epub 2018 May 31. Mol Pharmacol. 2018. PMID: 29853495
In vitro and in vivo effects of 2,4 diaminoquinazoline inhibitors of the decapping scavenger enzyme DcpS: Context-specific modulation of SMN transcript levels.
Cherry JJ, DiDonato CJ, Androphy EJ, Calo A, Potter K, Custer SK, Du S, Foley TL, Gopalsamy A, Reedich EJ, Gordo SM, Gordon W, Hosea N, Jones LH, Krizay DK, LaRosa G, Li H, Mathur S, Menard CA, Patel P, Ramos-Zayas R, Rietz A, Rong H, Zhang B, Tones MA. Cherry JJ, et al. Among authors: rong h. PLoS One. 2017 Sep 25;12(9):e0185079. doi: 10.1371/journal.pone.0185079. eCollection 2017. PLoS One. 2017. PMID: 28945765 Free PMC article.
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