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Page 1
Discovery of potent, selective chymase inhibitors via fragment linking strategies.
Taylor SJ, Padyana AK, Abeywardane A, Liang S, Hao MH, De Lombaert S, Proudfoot J, Farmer BS 3rd, Li X, Collins B, Martin L, Albaugh DR, Hill-Drzewi M, Pullen SS, Takahashi H. Taylor SJ, et al. Among authors: padyana ak. J Med Chem. 2013 Jun 13;56(11):4465-81. doi: 10.1021/jm400138z. Epub 2013 Jun 4. J Med Chem. 2013. PMID: 23659209
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.
Taylor SJ, Abeywardane A, Liang S, Muegge I, Padyana AK, Xiong Z, Hill-Drzewi M, Farmer B, Li X, Collins B, Li JX, Heim-Riether A, Proudfoot J, Zhang Q, Goldberg D, Zuvela-Jelaska L, Zaher H, Li J, Farrow NA. Taylor SJ, et al. Among authors: padyana ak. J Med Chem. 2011 Dec 8;54(23):8174-87. doi: 10.1021/jm201129m. Epub 2011 Nov 9. J Med Chem. 2011. PMID: 22017539
Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).
Takahashi H, Riether D, Bartolozzi A, Bosanac T, Berger V, Binetti R, Broadwater J, Chen Z, Crux R, De Lombaert S, Dave R, Dines JA, Fadra-Khan T, Flegg A, Garrigou M, Hao MH, Huber J, Hutzler JM, Kerr S, Kotey A, Liu W, Lo HY, Loke PL, Mahaney PE, Morwick TM, Napier S, Olague A, Pack E, Padyana AK, Thomson DS, Tye H, Wu L, Zindell RM, Abeywardane A, Simpson T. Takahashi H, et al. Among authors: padyana ak. J Med Chem. 2015 Feb 26;58(4):1669-90. doi: 10.1021/jm501185j. Epub 2015 Feb 11. J Med Chem. 2015. PMID: 25671290
Correction to Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13.
Taylor SJ, Abeywardane A, Liang S, Muegge I, Padyana AK, Xiong Z, Hill-Drzewi M, Farmer B, Li X, Collins B, Li JX, Heim-Riether A, Proudfoot J, Zhang Q, Goldberg D, Zuvela-Jelaska L, Zaher H, Li J, Farrow NA. Taylor SJ, et al. Among authors: padyana ak. J Med Chem. 2015 Aug 13;58(15):6318. doi: 10.1021/acs.jmedchem.5b00962. Epub 2015 Jul 27. J Med Chem. 2015. PMID: 26214135 No abstract available.
Indole RSK inhibitors. Part 1: discovery and initial SAR.
Boyer SJ, Burke J, Guo X, Kirrane TM, Snow RJ, Zhang Y, Sarko C, Soleymanzadeh L, Swinamer A, Westbrook J, Dicapua F, Padyana A, Cogan D, Gao A, Xiong Z, Madwed JB, Kashem M, Kugler S, O'Neill MM. Boyer SJ, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2012. PMID: 22100312
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.
Konteatis Z, Travins J, Gross S, Marjon K, Barnett A, Mandley E, Nicolay B, Nagaraja R, Chen Y, Sun Y, Liu Z, Yu J, Ye Z, Jiang F, Wei W, Fang C, Gao Y, Kalev P, Hyer ML, DeLaBarre B, Jin L, Padyana AK, Dang L, Murtie J, Biller SA, Sui Z, Marks KM. Konteatis Z, et al. Among authors: padyana ak. J Med Chem. 2021 Apr 22;64(8):4430-4449. doi: 10.1021/acs.jmedchem.0c01895. Epub 2021 Apr 8. J Med Chem. 2021. PMID: 33829783 Free article.
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.
Li M, Konteatis Z, Nagaraja N, Chen Y, Zhou S, Ma G, Gross S, Marjon K, Hyer ML, Mandley E, Lein M, Padyana AK, Jin L, Tong S, Peters R, Murtie J, Travins J, Medeiros M, Liu P, Frank V, Judd ET, Biller SA, Marks KM, Sui Z, Reznik SK. Li M, et al. Among authors: padyana ak. J Med Chem. 2022 Mar 24;65(6):4600-4615. doi: 10.1021/acs.jmedchem.1c01595. Epub 2022 Mar 16. J Med Chem. 2022. PMID: 35293760
Crystal structure of human GDF11.
Padyana AK, Vaidialingam B, Hayes DB, Gupta P, Franti M, Farrow NA. Padyana AK, et al. Acta Crystallogr F Struct Biol Commun. 2016 Mar;72(Pt 3):160-4. doi: 10.1107/S2053230X16001588. Epub 2016 Feb 16. Acta Crystallogr F Struct Biol Commun. 2016. PMID: 26919518 Free PMC article.
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Konteatis Z, Artin E, Nicolay B, Straley K, Padyana AK, Jin L, Chen Y, Narayaraswamy R, Tong S, Wang F, Zhou D, Cui D, Cai Z, Luo Z, Fang C, Tang H, Lv X, Nagaraja R, Yang H, Su SM, Sui Z, Dang L, Yen K, Popovici-Muller J, Codega P, Campos C, Mellinghoff IK, Biller SA. Konteatis Z, et al. Among authors: padyana ak. ACS Med Chem Lett. 2020 Jan 22;11(2):101-107. doi: 10.1021/acsmedchemlett.9b00509. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071674 Free PMC article.
24 results