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Page 1
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
Mitcheltree MJ, Li D, Achab A, Beard A, Chakravarthy K, Cheng M, Cho H, Eangoor P, Fan P, Gathiaka S, Kim HY, Lesburg CA, Lyons TW, Martinot TA, Miller JR, McMinn S, O'Neil J, Palani A, Palte RL, Saurí J, Sloman DL, Zhang H, Cumming JN, Fischer C. Mitcheltree MJ, et al. Among authors: palte rl. ACS Med Chem Lett. 2020 Mar 23;11(4):582-588. doi: 10.1021/acsmedchemlett.0c00058. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292567 Free PMC article.
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: palte rl. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).
Palte RL, Schneider SE, Altman MD, Hayes RP, Kawamura S, Lacey BM, Mansueto MS, Reutershan M, Siliphaivanh P, Sondey C, Xu H, Xu Z, Ye Y, Machacek MR. Palte RL, et al. ACS Med Chem Lett. 2020 Aug 7;11(9):1688-1693. doi: 10.1021/acsmedchemlett.9b00525. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944135 Free PMC article.
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
Quiroz RV, Reutershan MH, Schneider SE, Sloman D, Lacey BM, Swalm BM, Yeung CS, Gibeau C, Spellman DS, Rankic DA, Chen D, Witter D, Linn D, Munsell E, Feng G, Xu H, Hughes JME, Lim J, Saurí J, Geddes K, Wan M, Mansueto MS, Follmer NE, Fier PS, Siliphaivanh P, Daublain P, Palte RL, Hayes RP, Lee S, Kawamura S, Silverman S, Sanyal S, Henderson TJ, Ye Y, Gao Y, Nicholson B, Machacek MR. Quiroz RV, et al. Among authors: palte rl. J Med Chem. 2021 Apr 8;64(7):3911-3939. doi: 10.1021/acs.jmedchem.0c02083. Epub 2021 Mar 23. J Med Chem. 2021. PMID: 33755451
Cryo-EM structures of inhibitory antibodies complexed with arginase 1 provide insight into mechanism of action.
Palte RL, Juan V, Gomez-Llorente Y, Bailly MA, Chakravarthy K, Chen X, Cipriano D, Fayad GN, Fayadat-Dilman L, Gathiaka S, Greb H, Hall B, Handa M, Hsieh M, Kofman E, Lin H, Miller JR, Nguyen N, O'Neil J, Shaheen H, Sterner E, Strickland C, Sun A, Taremi S, Scapin G. Palte RL, et al. Commun Biol. 2021 Jul 29;4(1):927. doi: 10.1038/s42003-021-02444-z. Commun Biol. 2021. PMID: 34326456 Free PMC article.
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology.
Lu M, Zhang H, Li D, Childers M, Pu Q, Palte RL, Gathiaka S, Lyons TW, Palani A, Fan PW, Spacciapoli P, Miller JR, Cho H, Cheng M, Chakravarthy K, O'Neil J, Eangoor P, Beard A, Kim HY, Saurí J, Gunaydin H, Sloman DL, Siliphaivanh P, Cumming J, Fischer C. Lu M, et al. Among authors: palte rl. ACS Med Chem Lett. 2021 Jul 16;12(9):1380-1388. doi: 10.1021/acsmedchemlett.1c00195. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34527178 Free PMC article.
Author Correction: Cryo-EM structures of inhibitory antibodies complexed with arginase 1 provide insight into mechanism of action.
Palte RL, Juan V, Gomez-Llorente Y, Bailly MA, Chakravarthy K, Chen X, Cipriano D, Fayad GN, Fayadat-Dilman L, Gathiaka S, Greb H, Hall B, Handa M, Hsieh M, Kofman E, Lin H, Miller JR, Nguyen N, O'Neil J, Shaheen H, Sterner E, Strickland C, Sun A, Taremi S, Scapin G. Palte RL, et al. Commun Biol. 2021 Nov 15;4(1):1310. doi: 10.1038/s42003-021-02832-5. Commun Biol. 2021. PMID: 34782734 Free PMC article. No abstract available.
Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.
Li D, Zhang H, Lyons TW, Lu M, Achab A, Pu Q, Childers M, Mitcheltree MJ, Wang J, Martinot TA, McMinn SE, Sloman DL, Palani A, Beard A, Nogle L, Gathiaka S, Saurí J, Kim HY, Adpressa D, Spacciapoli P, Miller JR, Palte RL, Lesburg CA, Cumming J, Fischer C. Li D, et al. Among authors: palte rl. ACS Med Chem Lett. 2021 Oct 13;12(11):1678-1688. doi: 10.1021/acsmedchemlett.1c00258. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795856 Free PMC article.
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Keylor MH, Gulati A, Kattar SD, Johnson RE, Chau RW, Margrey KA, Ardolino MJ, Zarate C, Poremba KE, Simov V, Morriello GJ, Acton JJ, Pio B, Yan X, Palte RL, McMinn SE, Nogle L, Lesburg CA, Adpressa D, Lin S, Neelamkavil S, Liu P, Su J, Hegde LG, Woodhouse JD, Faltus R, Xiong T, Ciaccio PJ, Piesvaux J, Otte KM, Wood HB, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Fuller PH. Keylor MH, et al. Among authors: palte rl. J Med Chem. 2022 Jan 13;65(1):838-856. doi: 10.1021/acs.jmedchem.1c01968. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967623
16 results