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Page 1
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
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. 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
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
A kinase-cGAS cascade to synthesize a therapeutic STING activator.
McIntosh JA, Liu Z, Andresen BM, Marzijarani NS, Moore JC, Marshall NM, Borra-Garske M, Obligacion JV, Fier PS, Peng F, Forstater JH, Winston MS, An C, Chang W, Lim J, Huffman MA, Miller SP, Tsay FR, Altman MD, Lesburg CA, Steinhuebel D, Trotter BW, Cumming JN, Northrup A, Bu X, Mann BF, Biba M, Hiraga K, Murphy GS, Kolev JN, Makarewicz A, Pan W, Farasat I, Bade RS, Stone K, Duan D, Alvizo O, Adpressa D, Guetschow E, Hoyt E, Regalado EL, Castro S, Rivera N, Smith JP, Wang F, Crespo A, Verma D, Axnanda S, Dance ZEX, Devine PN, Tschaen D, Canada KA, Bulger PG, Sherry BD, Truppo MD, Ruck RT, Campeau LC, Bennett DJ, Humphrey GR, Campos KR, Maddess ML. McIntosh JA, et al. Among authors: cumming jn. Nature. 2022 Mar;603(7901):439-444. doi: 10.1038/s41586-022-04422-9. Epub 2022 Mar 16. Nature. 2022. PMID: 35296845
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. 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.
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: cumming jn. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW. Cumming JN, et al. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22390835
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. 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.
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
31 results