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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: lammens a. 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.
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.
Hopkins B, Zhang H, Bharathan I, Li D, Pu Q, Zhou H, Martinot TA, Fradera X, Lammens A, Lesburg CA, Cohen RD, Ballard J, Knemeyer I, Otte K, Vincent S, Miller JR, Solban N, Cheng M, Geda P, Smotrov N, Song X, Bennett DJ, Han Y. Hopkins B, et al. Among authors: lammens a. ACS Med Chem Lett. 2021 Aug 18;12(9):1435-1440. doi: 10.1021/acsmedchemlett.1c00265. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34531952 Free PMC article.
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Pu Q, Zhang H, Guo L, Cheng M, Doty AC, Ferguson H, Fradera X, Lesburg CA, McGowan MA, Miller JR, Geda P, Song X, Otte K, Sciammetta N, Solban N, Yu W, Sloman DL, Zhou H, Lammens A, Neumann L, Bennett DJ, Pasternak A, Han Y. Pu Q, et al. Among authors: lammens a. ACS Med Chem Lett. 2020 Jul 15;11(8):1548-1554. doi: 10.1021/acsmedchemlett.0c00195. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832022 Free PMC article.
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: lammens a. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV-1 Infected Cells.
Moore KP, Schwaid AG, Tudor M, Park S, Beshore DC, Converso A, Shipe WD, Anand R, Lan P, Moningka R, Rothman DM, Sun W, Chi A, Cornella-Taracido I, Adam GC, Bahnck-Teets C, Carroll SS, Fay JF, Goh SL, Lusen J, Quan S, Rodriguez S, Xu M, Andrews CL, Song C, Filzen T, Li J, Hollenstein K, Klein DJ, Lammens A, Lim UM, Fang Z, McHale C, Li Y, Lu M, Diamond TL, Howell BJ, Zuck P, Balibar CJ. Moore KP, et al. Among authors: lammens a. ACS Chem Biol. 2022 Sep 16;17(9):2595-2604. doi: 10.1021/acschembio.2c00515. Epub 2022 Aug 31. ACS Chem Biol. 2022. PMID: 36044633
Discovery of a Potent, Orally Bioavailable PI4KIIIβ Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo.
Reuberson J, Horsley H, Franklin RJ, Ford D, Neuss J, Brookings D, Huang Q, Vanderhoydonck B, Gao LJ, Jang MY, Herdewijn P, Ghawalkar A, Fallah-Arani F, Khan AR, Henshall J, Jairaj M, Malcolm S, Ward E, Shuttleworth L, Lin Y, Li S, Louat T, Waer M, Herman J, Payne A, Ceska T, Doyle C, Pitt W, Calmiano M, Augustin M, Steinbacher S, Lammens A, Allen R. Reuberson J, et al. Among authors: lammens a. J Med Chem. 2018 Aug 9;61(15):6705-6723. doi: 10.1021/acs.jmedchem.8b00521. Epub 2018 Jul 19. J Med Chem. 2018. PMID: 29952567
Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry.
Guilinger JP, Archna A, Augustin M, Bergmann A, Centrella PA, Clark MA, Cuozzo JW, Däther M, Guié MA, Habeshian S, Kiefersauer R, Krapp S, Lammens A, Lercher L, Liu J, Liu Y, Maskos K, Mrosek M, Pflügler K, Siegert M, Thomson HA, Tian X, Zhang Y, Konz Makino DL, Keefe AD. Guilinger JP, et al. Among authors: lammens a. Bioorg Med Chem. 2021 Jul 15;42:116223. doi: 10.1016/j.bmc.2021.116223. Epub 2021 May 19. Bioorg Med Chem. 2021. PMID: 34091303 Free article.
Data for the crystal structure of APRIL-BAFF-BAFF heterotrimer.
Maskos K, Lammens A, Tan SL, Hess H, Palinsky W, Schneider P, Jiang X. Maskos K, et al. Among authors: lammens a. Data Brief. 2015 Dec 18;6:438-44. doi: 10.1016/j.dib.2015.12.024. eCollection 2016 Mar. Data Brief. 2015. PMID: 26870754 Free PMC article.
Stoichiometry of Heteromeric BAFF and APRIL Cytokines Dictates Their Receptor Binding and Signaling Properties.
Schuepbach-Mallepell S, Das D, Willen L, Vigolo M, Tardivel A, Lebon L, Kowalczyk-Quintas C, Nys J, Smulski C, Zheng TS, Maskos K, Lammens A, Jiang X, Hess H, Tan SL, Schneider P. Schuepbach-Mallepell S, et al. Among authors: lammens a. J Biol Chem. 2015 Jun 26;290(26):16330-42. doi: 10.1074/jbc.M115.661405. Epub 2015 May 7. J Biol Chem. 2015. PMID: 25953898 Free PMC article.
32 results