A selective inhibitor of the UFM1-activating enzyme, UBA5

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 18, 2016, Pages 4542-4547

  da Silva, Sara R ^a   Paiva, Stacey Lynn ^a   Bancerz, Matthew ^a   Geletu, Mulu ^a   Lewis, Andrew M ^a   Chen, Jijun ^b   Cai, Yafei ^b   Lukkarila, Julie L ^b   Li, Honglin ^b   Gunning, Patrick T ^a  

^a UNIVERSITY OF TORONTO   (Canada)

^b MEDICAL COLLEGE OF GEORGIA   (United States)

Author keywords

E1 activating enzyme; Noncompetitive inhibition; UBA5; Ubiquitin like protein; UFM1

Indexed keywords

ADENOSINE; ANTINEOPLASTIC AGENT; ENZYME; ENZYME INHIBITOR; MOLECULAR SCAFFOLD; UBIQUITIN FOLD MODIFIER 1 ACTIVATING E1 ENZYME; UBIQUITIN FOLD MODIFIER 1 ACTIVATING E1 ENZYME INHIBITOR; UNCLASSIFIED DRUG; ZINC; UBA5 PROTEIN, HUMAN; UBIQUITIN PROTEIN LIGASE;

ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER CELL; CONJUGATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG SELECTIVITY; ENZYME INHIBITION; IC50; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; HUMAN; TUMOR CELL LINE;

CELL LINE, TUMOR; ENZYME INHIBITORS; HUMANS; UBIQUITIN-ACTIVATING ENZYMES;

EID: 84982292067     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.10.015     Document Type: Article

References (18)

1. 1 Herscko, A., Heller, H., Elias, S., Ciechanover, A., J. Biol. Chem., 258, 1983, 8206.
2. 2 Bedford, L., Lowe, J., Dick, L.R., Mayer, R.J., Brownell, J.E., Nat. Rev. Drug Disc., 10, 2011, 29.
3. 3 Schulman, B.A., Harper, J.W., Nat. Rev. Mol. Cell Biol., 10, 2009, 319.
4. 4 Mahajan, R., Delphin, C., Guan, T., Gerace, L., Melchior, F., Cell, 88, 1997, 97.
5. 5 Liakopoulus, D., Doenges, G., Matuschewski, K., Jentsch, S., EMBO J., 17, 1998, 2208.
6. 6 Komatsu, M., Chiba, T., Tatsumi, K., Iemura, S., Tanida, I., Okazaki, N., Ueno, T., Kominami, E., Natsume, T., Tanaka, K., EMBO J., 2004, 1977, 23.
7. 7 Tatsumi, K., Yamamoto-Mukai, H., Shimizu, R., Waguri, S., Sou, Y.S., Sakamoto, A., Taya, C., Shitara, H., Hara, T., Chung, C.H., Tanaka, K., Yamamoto, M., Komatsu, M., Nat. Commun., 2, 2011, 181, 10.1038/ncomms1182.
8. 8 Lemaire, K., Moura, R.F., Granvik, M., Igoillo-Esteve, M., Hohmeier, H.E., Hendrick, N., Newgard, C.B., Waelkens, E., Cnop, M., Schuit, F., PLoS ONE, 6, 2011, e18517.
9. 9 Yoo, H.M., Kang, S.H., Kim, J.Y., Lee, J.E., Seong, M.W., Lee, S.W., Ka, S.H., Sou, Y.-S., Komatsu, M., Tanaka, K., Lee, S.T., Noh, D.Y., Baek, S.H., Jeon, Y.J., Chung, C.H., Mol. Cell, 56, 2014, 261.
10. 10 Daniel, J., Liebau, E., Cells, 3, 2014, 627.
11. 11 Gavin, J.M., Hoar, K., Xu, Q., Ma, J., Lin, Y., Chen, J., Chen, W., Bruzzese, F.J., Harrison, S., Mallender, W.D., Bump, N.J., Sintchak, M.D., Bence, N.F., Li, P., Dick, L.R., Gould, A.E., Chen, J.J., J. Biol. Chem., 289, 2014, 22648.
12. 12 Tatsumi, K., Sou, Y.-S., Tada, N., Nakamura, E., Iemura, S.-I., Natsume, T., Kang, S.H., Chung, C.H., Kasahara, M., Kominami, E., Yamamoto, M., Takana, K., Komatsu, M., J. Biol. Chem., 285, 2010, 5417.
13. 13 Soucy, T.A., Smith, P.G., Milhollen, M.A., Berger, A.J., Gavin, J.M., Adhikari, S., Brownell, J.E., Burke, K.E., Cardin, D.P., Critchley, S., Cullis, C.A., Doucette, A., Garnsey, J.J., Gaulin, J.L., Gershman, R.E., Lublinsky, A.R., McDonald, A., Mizutani, H., Narayanan, U., Olhava, E.J., Peluso, S., Rezaei, M., Sintchak, M.D., Talreja, T., Thomas, M.P., Traore, T., Vyskocil, S., Weatherhead, G.S., Yu, J., Zhang, J., Dick, L.R., Claiborne, C.F., Rolfe, M., Bolen, J.B., Langston, S.P., Nature, 458, 2009, 732.
14. 14 Brownell, J.E., Sintchak, M.D., Gavin, J.M., Liao, H., Bruzzese, F.J., Bump, N.J., Soucy, T.A., Milhollen, M.A., Yang, X., Burkhardt, A.L., Ma, J., Loke, H.-K., Lingaraj, T., Wu, D., Hamman, K.B., Spelman, J.J., Cullis, C.A., Langston, S.P., Vyzkocil, S., Sells, T.B., Mallender, W.D., Visiers, I., Li, P., Claiborne, C.F., Rolfe, M., Bolen, J.B., Dick, L.R., Mol. Cell, 37, 2010, 102.
15. 15 Bacik, J.-P., Walker, J.R., Ali, M., Schimmer, A.D., Dhe-Paganon, S., J. Biol. Chem., 285, 2010, 20273.
16. 16 Lake, M.W., Wuebbens, M.M., Rajagopalan, K.V., Schindelin, H., Nature, 414, 2001, 325.
17. 17 Lukkarila, J.L., da Silva, S.R., Ali, M., Shahani, V.M., Xu, G.W., Berman, J., Roughton, A., Dhe-Paganon, S., Schimmer, A.D., Gunning, P.T., ACS Med. Chem. Lett., 2, 2011, 577.
18. 18 Davis, M.I., Hunt, J.P., Herrgard, S., Ciceri, P., Wodicka, L.M., Pallares, G., Hocker, M., Treiber, D.K., Zarrinkar, P.P., Nat. Biotech., 29, 2011, 1046.