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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. Schreiber SL, et al. Among authors: yu h. Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Cell. 2015. PMID: 26046436 Free PMC article. Review.
Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.
Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB. Wang HR, et al. Among authors: yu h. ACS Chem Biol. 2011 Aug 19;6(8):845-56. doi: 10.1021/cb200146a. Epub 2011 Jun 13. ACS Chem Biol. 2011. PMID: 21615117 Free PMC article.
The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.
Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, Dawson ES, Li M, McManus O, Jones CK, Daniels JS, Hopkins CR, Xie XS, Conn PJ, Weaver CD, Lindsley CW. Xiang Z, et al. Among authors: yu h. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742. doi: 10.1021/cn200090z. ACS Chem Neurosci. 2011. PMID: 22368764 Free PMC article.
Modulation of hERG potassium channel gating normalizes action potential duration prolonged by dysfunctional KCNQ1 potassium channel.
Zhang H, Zou B, Yu H, Moretti A, Wang X, Yan W, Babcock JJ, Bellin M, McManus OB, Tomaselli G, Nan F, Laugwitz KL, Li M. Zhang H, et al. Among authors: yu h. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11866-71. doi: 10.1073/pnas.1205266109. Epub 2012 Jun 28. Proc Natl Acad Sci U S A. 2012. PMID: 22745159 Free PMC article.
Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Cheung YY, Yu H, Xu K, Zou B, Wu M, McManus OB, Li M, Lindsley CW, Hopkins CR. Cheung YY, et al. Among authors: yu h. J Med Chem. 2012 Aug 9;55(15):6975-9. doi: 10.1021/jm300700v. Epub 2012 Jul 26. J Med Chem. 2012. PMID: 22793372 Free PMC article.
Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Mattmann ME, Yu H, Lin Z, Xu K, Huang X, Long S, Wu M, McManus OB, Engers DW, Le UM, Li M, Lindsley CW, Hopkins CR. Mattmann ME, et al. Among authors: yu h. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5936-41. doi: 10.1016/j.bmcl.2012.07.060. Epub 2012 Aug 2. Bioorg Med Chem Lett. 2012. PMID: 22910039 Free PMC article.
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