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Page 1
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
White C, McGowan MA, Zhou H, Sciammetta N, Fradera X, Lim J, Joshi EM, Andrews C, Nickbarg EB, Cowley P, Trewick S, Augustin M, von Köenig K, Lesburg CA, Otte K, Knemeyer I, Woo H, Yu W, Cheng M, Spacciapoli P, Geda P, Song X, Smotrov N, Curran P, Heo MR, Abeywickrema P, Miller JR, Bennett DJ, Han Y. White C, et al. Among authors: geda p. ACS Med Chem Lett. 2020 Mar 10;11(4):550-557. doi: 10.1021/acsmedchemlett.0c00010. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292563 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: geda p. 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.
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: geda 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: geda 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
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: geda p. 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 MK-4688: an Efficient Inhibitor of the HDM2-p53 Protein-Protein Interaction.
Reutershan MH, Machacek MR, Altman MD, Bogen S, Cai M, Cammarano C, Chen D, Christopher M, Cryan J, Daublain P, Fradera X, Geda P, Goldenblatt P, Hill AD, Kemper RA, Kutilek V, Li C, Martinez M, McCoy M, Nair L, Pan W, Thompson CF, Scapin G, Shizuka M, Spatz ML, Steinhuebel D, Sun B, Voss ME, Wang X, Yang L, Yeh TC, Dussault I, Marshall CG, Trotter BW. Reutershan MH, et al. Among authors: geda p. J Med Chem. 2021 Nov 11;64(21):16213-16241. doi: 10.1021/acs.jmedchem.1c01524. Epub 2021 Oct 29. J Med Chem. 2021. PMID: 34714078
Development of Anti-CD74 Antibody-Drug Conjugates to Target Glucocorticoids to Immune Cells.
Brandish PE, Palmieri A, Antonenko S, Beaumont M, Benso L, Cancilla M, Cheng M, Fayadat-Dilman L, Feng G, Figueroa I, Firdos J, Garbaccio R, Garvin-Queen L, Gately D, Geda P, Haines C, Hseih S, Hodges D, Kern J, Knudsen N, Kwasnjuk K, Liang L, Ma H, Manibusan A, Miller PL, Moy LY, Qu Y, Shah S, Shin JS, Stivers P, Sun Y, Tomazela D, Woo HC, Zaller D, Zhang S, Zhang Y, Zielstorff M. Brandish PE, et al. Among authors: geda p. Bioconjug Chem. 2018 Jul 18;29(7):2357-2369. doi: 10.1021/acs.bioconjchem.8b00312. Epub 2018 Jul 2. Bioconjug Chem. 2018. PMID: 29923706
Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody-Drug Conjugates.
Kern JC, Cancilla M, Dooney D, Kwasnjuk K, Zhang R, Beaumont M, Figueroa I, Hsieh S, Liang L, Tomazela D, Zhang J, Brandish PE, Palmieri A, Stivers P, Cheng M, Feng G, Geda P, Shah S, Beck A, Bresson D, Firdos J, Gately D, Knudsen N, Manibusan A, Schultz PG, Sun Y, Garbaccio RM. Kern JC, et al. Among authors: geda p. J Am Chem Soc. 2016 Feb 3;138(4):1430-45. doi: 10.1021/jacs.5b12547. Epub 2016 Jan 25. J Am Chem Soc. 2016. PMID: 26745435
Characterizing Pharmacokinetic-Pharmacodynamic Relationships and Efficacy of PI3Kδ Inhibitors in Respiratory Models of TH2 and TH1 Inflammation.
McLeod RL, Gil MA, Chen D, Cabal A, Katz J, Methot J, Woodhouse JD, Dorosh L, Geda P, Mehta K, Cicmil M, Baltus GA, Bass A, Houshyar H, Caniga M, Yu H, Gervais F, Alves S, Shah S. McLeod RL, et al. Among authors: geda p. J Pharmacol Exp Ther. 2019 May;369(2):223-233. doi: 10.1124/jpet.118.252551. Epub 2019 Feb 25. J Pharmacol Exp Ther. 2019. PMID: 30804001
The PTPN2/PTPN1 inhibitor ABBV-CLS-484 unleashes potent anti-tumour immunity.
Baumgartner CK, Ebrahimi-Nik H, Iracheta-Vellve A, Hamel KM, Olander KE, Davis TGR, McGuire KA, Halvorsen GT, Avila OI, Patel CH, Kim SY, Kammula AV, Muscato AJ, Halliwill K, Geda P, Klinge KL, Xiong Z, Duggan R, Mu L, Yeary MD, Patti JC, Balon TM, Mathew R, Backus C, Kennedy DE, Chen A, Longenecker K, Klahn JT, Hrusch CL, Krishnan N, Hutchins CW, Dunning JP, Bulic M, Tiwari P, Colvin KJ, Chuong CL, Kohnle IC, Rees MG, Boghossian A, Ronan M, Roth JA, Wu MJ, Suermondt JSMT, Knudsen NH, Cheruiyot CK, Sen DR, Griffin GK, Golub TR, El-Bardeesy N, Decker JH, Yang Y, Guffroy M, Fossey S, Trusk P, Sun IM, Liu Y, Qiu W, Sun Q, Paddock MN, Farney EP, Matulenko MA, Beauregard C, Frost JM, Yates KB, Kym PR, Manguso RT. Baumgartner CK, et al. Among authors: geda p. Nature. 2023 Oct;622(7984):850-862. doi: 10.1038/s41586-023-06575-7. Epub 2023 Oct 4. Nature. 2023. PMID: 37794185 Free PMC article.
12 results