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Page 1
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors.
Li D, Deng Y, Achab A, Bharathan I, Hopkins BA, Yu W, Zhang H, Sanyal S, Pu Q, Zhou H, Liu K, Lim J, Fradera X, Lesburg CA, Lammens A, Martinot TA, Cohen RD, Doty AC, Ferguson H, Nickbarg EB, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte KM, Vincent S, Sciammetta N, Pasternak A, Bennett DJ, Han Y. Li D, et al. Among authors: saradjian p. ACS Med Chem Lett. 2021 Feb 26;12(3):389-396. doi: 10.1021/acsmedchemlett.0c00525. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738066 Free PMC article.
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.
Yu W, Deng Y, Hopkins B, Huang X, Sloman D, Zhang H, Li D, McGowan MA, White C, Pu Q, Liu K, Fradera X, Lesburg CA, Martinot T, Doty A, Ferguson H, Nickbarg EB, Cheng M, Geda P, Song X, Smotrov N, Abeywickrema P, Andrews C, Chamberlin C, Mabrouk O, Curran P, Richards M, Saradjian P, Miller JR, Knemeyer I, Otte K, Vincent S, Sciammetta N, Bennett DJ, Han Y. Yu W, et al. Among authors: saradjian p. Bioorg Med Chem Lett. 2021 Sep 1;47:128214. doi: 10.1016/j.bmcl.2021.128214. Epub 2021 Jun 21. Bioorg Med Chem Lett. 2021. PMID: 34166782
Discovery of Selective RNA-Binding Small Molecules by Affinity-Selection Mass Spectrometry.
Rizvi NF, Howe JA, Nahvi A, Klein DJ, Fischmann TO, Kim HY, McCoy MA, Walker SS, Hruza A, Richards MP, Chamberlin C, Saradjian P, Butko MT, Mercado G, Burchard J, Strickland C, Dandliker PJ, Smith GF, Nickbarg EB. Rizvi NF, et al. Among authors: saradjian p. ACS Chem Biol. 2018 Mar 16;13(3):820-831. doi: 10.1021/acschembio.7b01013. Epub 2018 Feb 14. ACS Chem Biol. 2018. PMID: 29412640
Targeting RNA with Small Molecules: Identification of Selective, RNA-Binding Small Molecules Occupying Drug-Like Chemical Space.
Rizvi NF, Santa Maria JP Jr, Nahvi A, Klappenbach J, Klein DJ, Curran PJ, Richards MP, Chamberlin C, Saradjian P, Burchard J, Aguilar R, Lee JT, Dandliker PJ, Smith GF, Kutchukian P, Nickbarg EB. Rizvi NF, et al. Among authors: saradjian p. SLAS Discov. 2020 Apr;25(4):384-396. doi: 10.1177/2472555219885373. Epub 2019 Nov 8. SLAS Discov. 2020. PMID: 31701793 Free article.
Linking High-Throughput Screens to Identify MoAs and Novel Inhibitors of Mycobacterium tuberculosis Dihydrofolate Reductase.
Santa Maria JP Jr, Park Y, Yang L, Murgolo N, Altman MD, Zuck P, Adam G, Chamberlin C, Saradjian P, Dandliker P, Boshoff HIM, Barry CE 3rd, Garlisi C, Olsen DB, Young K, Glick M, Nickbarg E, Kutchukian PS. Santa Maria JP Jr, et al. Among authors: saradjian p. ACS Chem Biol. 2017 Sep 15;12(9):2448-2456. doi: 10.1021/acschembio.7b00468. Epub 2017 Aug 29. ACS Chem Biol. 2017. PMID: 28806050 Free PMC article.
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors.
Lacey BM, Xu Z, Chai X, Laskey J, Fradera X, Mittal P, Mishra S, Piesvaux J, Saradjian P, Shaffer L, Vassileva G, Gerdt C, Wang Y, Ferguson H, Smith DM, Ballard J, Wells S, Jain R, Mueller U, Addona G, Kariv I, Methot JL, Bittinger M, Ranganath S, Mcleod R, Pasternak A, Miller JR, Xu H. Lacey BM, et al. Among authors: saradjian p. SLAS Discov. 2021 Jan;26(1):88-99. doi: 10.1177/2472555220952071. Epub 2020 Aug 26. SLAS Discov. 2021. PMID: 32844715 Free article.
Integration of Affinity Selection-Mass Spectrometry and Functional Cell-Based Assays to Rapidly Triage Druggable Target Space within the NF-κB Pathway.
Kutilek VD, Andrews CL, Richards MP, Xu Z, Sun T, Chen Y, Hashke A, Smotrov N, Fernandez R, Nickbarg EB, Chamberlin C, Sauvagnat B, Curran PJ, Boinay R, Saradjian P, Allen SJ, Byrne N, Elsen NL, Ford RE, Hall DL, Kornienko M, Rickert KW, Sharma S, Shipman JM, Lumb KJ, Coleman K, Dandliker PJ, Kariv I, Beutel B. Kutilek VD, et al. Among authors: saradjian p. J Biomol Screen. 2016 Jul;21(6):608-19. doi: 10.1177/1087057116637353. Epub 2016 Mar 11. J Biomol Screen. 2016. PMID: 26969322
Structural characterization of nonactive site, TrkA-selective kinase inhibitors.
Su HP, Rickert K, Burlein C, Narayan K, Bukhtiyarova M, Hurzy DM, Stump CA, Zhang X, Reid J, Krasowska-Zoladek A, Tummala S, Shipman JM, Kornienko M, Lemaire PA, Krosky D, Heller A, Achab A, Chamberlin C, Saradjian P, Sauvagnat B, Yang X, Ziebell MR, Nickbarg E, Sanders JM, Bilodeau MT, Carroll SS, Lumb KJ, Soisson SM, Henze DA, Cooke AJ. Su HP, et al. Among authors: saradjian p. Proc Natl Acad Sci U S A. 2017 Jan 17;114(3):E297-E306. doi: 10.1073/pnas.1611577114. Epub 2016 Dec 30. Proc Natl Acad Sci U S A. 2017. PMID: 28039433 Free PMC article.
Assay Development for Protein Kinase Enzymes.
Glickman JF. Glickman JF. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. PMID: 22553863 Free Books & Documents. Review.
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