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Page 1
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: cumming j. 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.
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.
Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ. Stamford AW, et al. Among authors: cumming jn. ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. doi: 10.1021/ml3001165. Epub 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 23412139 Free PMC article.
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: cumming jn. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
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: cumming jn. 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.
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: cumming j. 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.
STimulator of INterferon Genes Agonism Accelerates Antitumor Activity in Poorly Immunogenic Tumors.
Perera SA, Kopinja JE, Ma Y, Muise ES, Laskey J, Chakravarthy K, Chen Y, Cui L, Presland J, Sathe M, Javaid S, Minnihan EC, Ferguson HM, Piesvaux J, Pan BS, Zhao S, Sharma SK, Woo HC, Pucci V, Knemeyer I, Cemerski S, Cumming J, Trotter BW, Tse A, Khilnani A, Ranganath S, Long BJ, Bennett DJ, Addona GH. Perera SA, et al. Among authors: cumming j. Mol Cancer Ther. 2022 Feb;21(2):282-293. doi: 10.1158/1535-7163.MCT-21-0136. Epub 2021 Nov 23. Mol Cancer Ther. 2022. PMID: 34815361
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN. Taoka BM, et al. Among authors: cumming jn. Bioorg Med Chem Lett. 2022 Jan 15;56:128463. doi: 10.1016/j.bmcl.2021.128463. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838652
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Chang W, Altman MD, Lesburg CA, Perera SA, Piesvaux JA, Schroeder GK, Wyss DF, Cemerski S, Chen Y, DiNunzio E, Haidle AM, Ho T, Kariv I, Knemeyer I, Kopinja JE, Lacey BM, Laskey J, Lim J, Long BJ, Ma Y, Maddess ML, Pan BS, Presland JP, Spooner E, Steinhuebel D, Truong Q, Zhang Z, Fu J, Addona GH, Northrup AB, Parmee E, Tata JR, Bennett DJ, Cumming JN, Siu T, Trotter BW. Chang W, et al. Among authors: cumming jn. J Med Chem. 2022 Apr 14;65(7):5675-5689. doi: 10.1021/acs.jmedchem.1c02197. Epub 2022 Mar 25. J Med Chem. 2022. PMID: 35332774
An orally available non-nucleotide STING agonist with antitumor activity.
Pan BS, Perera SA, Piesvaux JA, Presland JP, Schroeder GK, Cumming JN, Trotter BW, Altman MD, Buevich AV, Cash B, Cemerski S, Chang W, Chen Y, Dandliker PJ, Feng G, Haidle A, Henderson T, Jewell J, Kariv I, Knemeyer I, Kopinja J, Lacey BM, Laskey J, Lesburg CA, Liang R, Long BJ, Lu M, Ma Y, Minnihan EC, O'Donnell G, Otte R, Price L, Rakhilina L, Sauvagnat B, Sharma S, Tyagarajan S, Woo H, Wyss DF, Xu S, Bennett DJ, Addona GH. Pan BS, et al. Among authors: cumming jn. Science. 2020 Aug 21;369(6506):eaba6098. doi: 10.1126/science.aba6098. Science. 2020. PMID: 32820094
Genomic Discovery and Structure-Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors.
Davison JR, Hadjithomas M, Romeril SP, Choi YJ, Bentley KW, Biggins JB, Chacko N, Castaldi MP, Chan LK, Cumming JN, Downes TD, Eisenhauer EL, Fei F, Fontaine BM, Endalur Gopinarayanan V, Gurnani S, Hecht A, Hosford CJ, Ibrahim A, Jagels A, Joubran C, Kim JN, Lisher JP, Liu DD, Lyles JT, Mannara MN, Murray GJ, Musial E, Niu M, Olivares-Amaya R, Percuoco M, Saalau S, Sharpe K, Sheahan AV, Thevakumaran N, Thompson JE, Thompson DA, Wiest A, Wyka SA, Yano J, Verdine GL. Davison JR, et al. Among authors: cumming jn. J Med Chem. 2024 Aug 8;67(15):13147-13173. doi: 10.1021/acs.jmedchem.4c01095. Epub 2024 Jul 30. J Med Chem. 2024. PMID: 39078366 Free PMC article.
458 results