Publications

2016 | 2015 | 2012 | 2011 | 2010 | 2009

2016

Kugel S, Sebastián C, Fitamant J, Ross KN, Saha SK, Jain E, Gladden A, Arora KS, Kato Y, Rivera MN, Ramaswamy S, Sadreyev RI, Goren A, Deshpande V, Bardeesy N & Mostoslavsky R. SIRT6 suppresses pancreatic cancer through control of Lin28b. Cell. 2016. 165(6):1401-15.

2015

*Wilson MR, *Kugel S, Huang J, Wilson LJ, Wloszczynski PA, Ye J, Matherly LH & Hou Z. Structural determinants of human proton-coupled folate transporter oligomerization: role of GXXXG motifs and identification of oligomeric interfaces at transmembrane domains 3 and 6. Biochemical Journal. 2015. 469(1):33-44. *These authors contributed equally to this work.

*Kugel S, *Feldman JL, Klein AM, Silberman DM, Sebastián C, Dobersch S, Clark AR, Getz G, Denu JM & Mostoslavsky R. Identification and molecular basis for SIRT6 loss-of-function point mutations in cancer. Cell Reports. 2015. 13(3):479-88. *These authors contributed equally to this work.

Etchegaray JP, Chavez L, Huang Y, Ross KN, Choi J, Martinez-Pastor B, Walsh RM, Sommer CA, Lienhard M, Gladden A, Kugel S, Silberman DM, Ramaswamy S, Mostoslavsky G, Hochedlinger K, Goren A, Rao A & Mostoslavsky R. The histone deacetylase SIRT6 controls embryonic stem cell fate via Tet-mediated production of 5-hydroxymethylcytosine. Nat. Cell Biol. 2015. 17, 545-557.

2012

Hou Z, Kugel S, Etnyre E, Olive M, Hsiung, B, Cherian C, Wloszczynski PA, Moin K, & Matherly LH. Identification and functional impact of homo-oligomers of the human proton-coupled folate transporter. J Biol Chem. 2012. 287(7): 4982-95.

Wang L, Cherian C, Kugel S, Mitchell-Ryan S, Hou Z, Matherly LH & Gangjee A. Synthesis and biological activity of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier. J Med Chem. 2012. 55(4): 1758-70.

Kugel S, Wang L, Polin P, White K, Kushner J, Stout M, Hou Z, Cherian C, Gangjee A & Matherly LH. Functional loss of the reduced folate carrier enhances the antitumor activities of novel antifolates with selective uptake by the proton-coupled folate transporter. Mol Pharmacol. 2012. 82(4): 591-600.

Cherian C, Kugel S, Wang L, Polin L, White K, Kushner J, Stout M, Hou Z, Gangjee A & Matherly LH. Therapeutic targeting malignant mesothelioma with a novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate via its selective uptake by the proton-coupled folate transporter. Cancer Chemother Pharmacol. 2012. 71(4): 999-1011.

2011

*Wang L, *Kugel S, Cherian C, Polin L, White K, Kushner J, Fulterer A, Chang MH, Mitchell-Ryan S, Stout M, Romero MF, Hou Z, Matherly LH. & Gangjee A. Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase. J Med Chem. 2011. 54(20): 7150-64. *These authors contributed equally to this work.

Kugel S, Wang L, Polin P, White K, Kushner J, Hales E, Stout M, Hou Z, Cherian C, Gangjee A & Matherly LH. Therapeutic targeting of a novel 6-substituted pyrrolo[2,3d]pyrimidine thienoyl antifolate to human solid tumors based on selective uptake by the proton-coupled folate transporter. Mol Pharmacol. 2011. 80(6): 1096-107.

2010

Wang, L., Cherian, C., Kugel Desmoulin, S., Polin, L., Deng, Y., Wu, J., Hou, Z., White, K., Kushner, J., Matherly, L.H. & Gangjee, A. Synthesis and biological activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry. J Med Chem. 2010. 53(3): 1306-18.

Kugel S, Wang Y, Wu J, Stout M, Hou Z, Fulterer A, Chang MH, Romero MF, Cherian C, Gangjee A. & Matherly LH. Targeting the proton-coupled folate transporter for selective delivery of 6-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of de novo purine biosynthesis in the chemotherapy of solid tumors. Mol Pharmacol. 2010. 78(4): 577-87.

2009

Larson Gedman A, Chen Q, Kugel S, Ge Y, LaFiura K, Haska CL, Cherian C, Devidas M, Linda SB, Taub J.W. & Matherly, L.H. The impact of NOTCH1, FBW7 and PTEN mutations on prognosis and downstream signaling in pediatric T-cell acute lymphoblastic leukemia: a report from the Children’s Oncology Group. Leukemia. 2009. 23(8): 1417-1425.

Deng Y, Zhou X, Kugel S, Wu J, Cherian C, Hou Z, Matherly LH & Ganjee A. Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry. J. Med. Chem. 2009. 52(9): 2940-2951.