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Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.
Wallace-Povirk A, Tong N, Wong-Roushar J, O'Connor C, Zhou X, Hou Z, Bao X, Garcia GE, Li J, Kim S, Dann CE 3rd, Matherly LH, Gangjee A. Wallace-Povirk A, et al. Bioorg Med Chem. 2021 May 1;37:116093. doi: 10.1016/j.bmc.2021.116093. Epub 2021 Feb 26. Bioorg Med Chem. 2021. PMID: 33773393 Free PMC article.
A new structural paradigm in copper resistance in Streptococcus pneumoniae.
Fu Y, Tsui HC, Bruce KE, Sham LT, Higgins KA, Lisher JP, Kazmierczak KM, Maroney MJ, Dann CE 3rd, Winkler ME, Giedroc DP. Fu Y, et al. Nat Chem Biol. 2013 Mar;9(3):177-83. doi: 10.1038/nchembio.1168. Epub 2013 Jan 27. Nat Chem Biol. 2013. PMID: 23354287 Free PMC article.
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.
Wang L, Wallace A, Raghavan S, Deis SM, Wilson MR, Yang S, Polin L, White K, Kushner J, Orr S, George C, O'Connor C, Hou Z, Mitchell-Ryan S, Dann CE 3rd, Matherly LH, Gangjee A. Wang L, et al. J Med Chem. 2015 Sep 10;58(17):6938-59. doi: 10.1021/acs.jmedchem.5b00801. Epub 2015 Aug 28. J Med Chem. 2015. PMID: 26317331 Free PMC article.
Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.
Golani LK, Wallace-Povirk A, Deis SM, Wong J, Ke J, Gu X, Raghavan S, Wilson MR, Li X, Polin L, de Waal PW, White K, Kushner J, O'Connor C, Hou Z, Xu HE, Melcher K, Dann CE 3rd, Matherly LH, Gangjee A. Golani LK, et al. J Med Chem. 2016 Sep 8;59(17):7856-76. doi: 10.1021/acs.jmedchem.6b00594. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27458733 Free PMC article.