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Lead optimization toward proof-of-concept tools for Huntington's disease within a 4-(1H-pyrazol-4-yl)pyrimidine class of pan-JNK inhibitors.
Wityak J, McGee KF, Conlon MP, Song RH, Duffy BC, Clayton B, Lynch M, Wang G, Freeman E, Haber J, Kitchen DB, Manning DD, Ismail J, Khmelnitsky Y, Michels P, Webster J, Irigoyen M, Luche M, Hultman M, Bai M, Kuok ID, Newell R, Lamers M, Leonard P, Yates D, Matthews K, Ongeri L, Clifton S, Mead T, Deupree S, Wheelan P, Lyons K, Wilson C, Kiselyov A, Toledo-Sherman L, Beconi M, Muñoz-Sanjuan I, Bard J, Dominguez C. Wityak J, et al. Among authors: kiselyov a. J Med Chem. 2015 Apr 9;58(7):2967-87. doi: 10.1021/jm5013598. Epub 2015 Mar 19. J Med Chem. 2015. PMID: 25760409
Imaging Mutant Huntingtin Aggregates: Development of a Potential PET Ligand.
Liu L, Prime ME, Lee MR, Khetarpal V, Brown CJ, Johnson PD, Miranda-Azpiazu P, Chen X, Clark-Frew D, Coe S, Davis R, Dickie A, Ebneth A, Esposito S, Gadouleau E, Gai X, Galan S, Green S, Greenaway C, Giles P, Halldin C, Hayes S, Herbst T, Herrmann F, Heßmann M, Jia Z, Kiselyov A, Kotey A, Krulle T, Mangette JE, Marston RW, Menta S, Mills MR, Monteagudo E, Nag S, Nibbio M, Orsatti L, Schaertl S, Scheich C, Sproston J, Stepanov V, Svedberg M, Takano A, Taylor M, Thomas W, Toth M, Vaidya D, Vanräs K, Weddell D, Wigginton I, Wityak J, Mrzljak L, Munoz-Sanjuan I, Bard JA, Dominguez C. Liu L, et al. Among authors: kiselyov a. J Med Chem. 2020 Aug 13;63(15):8608-8633. doi: 10.1021/acs.jmedchem.0c00955. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32662649
Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates.
Herrmann F, Hessmann M, Schaertl S, Berg-Rosseburg K, Brown CJ, Bursow G, Chiki A, Ebneth A, Gehrmann M, Hoeschen N, Hotze M, Jahn S, Johnson PD, Khetarpal V, Kiselyov A, Kottig K, Ladewig S, Lashuel H, Letschert S, Mills MR, Petersen K, Prime ME, Scheich C, Schmiedel G, Wityak J, Liu L, Dominguez C, Muñoz-Sanjuán I, Bard JA. Herrmann F, et al. Among authors: kiselyov a. Sci Rep. 2021 Sep 9;11(1):17977. doi: 10.1038/s41598-021-97334-z. Sci Rep. 2021. PMID: 34504195 Free PMC article.
N-Aryl-gamma-lactams as integrin alphavbeta3 antagonists.
Xi N, Arvedson S, Eisenberg S, Han N, Handley M, Huang L, Huang Q, Kiselyov A, Liu Q, Lu Y, Nunez G, Osslund T, Powers D, Tasker AS, Wang L, Xiang T, Xu S, Zhang J, Zhu J, Kendall R, Dominguez C. Xi N, et al. Among authors: kiselyov a. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2905-9. doi: 10.1016/j.bmcl.2004.03.033. Bioorg Med Chem Lett. 2004. PMID: 15125957
Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis.
Sandanayaka V, Mamat B, Mishra RK, Winger J, Krohn M, Zhou LM, Keyvan M, Enache L, Sullins D, Onua E, Zhang J, Halldorsdottir G, Sigthorsdottir H, Thorlaksdottir A, Sigthorsson G, Thorsteinnsdottir M, Davies DR, Stewart LJ, Zembower DE, Andresson T, Kiselyov AS, Singh J, Gurney ME. Sandanayaka V, et al. Among authors: kiselyov as. J Med Chem. 2010 Jan 28;53(2):573-85. doi: 10.1021/jm900838g. J Med Chem. 2010. PMID: 19950900
91 results