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Literature
  1. Adhikari, B., Bozilovic, J., Diebold, M., Schwarz, J. D., Hofstetter, J., Schröder, M., Wanior, M., Narain, A., Vogt, M., Dudvarski Stankovic, N., et al. (2020). PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nature Chemical Biology 16, 1179-1188.

  2. Bai, L., Zhou, B., Yang, C.-Y., Ji, J., McEachern, D., Przybranowski, S., Jiang, H., Hu, J., Xu, F., Zhao, Y., et al. (2017). Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Research 77, 2476-2487.

  3. Banik, S. M., Pedram, K., Wisnovsky, S., Ahn, G., Riley, N. M., and Bertozzi, C. R. (2020). Lysosome-targeting chimaeras for degradation of extracellular proteins. Nature 584, 291-297.

  4. Chan, K.-H., Zengerle, M., Testa, A., and Ciulli, A. (2017). Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. Journal of Medicinal Chemistry 61, 504-513.

  5. Duan, Y., Guan, Y., Qin, W., Zhai, X., Yu, B., and Liu, H. (2018). Targeting Brd4 for cancer therapy: inhibitors and degraders. MedChemComm 9, 1779-1802.

  6. Gadd, M. S., Testa, A., Lucas, X., Chan, K.-H., Chen, W., Lamont, D. J., Zengerle, M., and Ciulli, A. (2017). Structural basis of PROTAC cooperative recognition for selective protein degradation. Nature Chemical Biology 13, 514-521.

  7. Gechijian, L. N., Buckley, D. L., Lawlor, M. A., Reyes, J. M., Paulk, J., Ott, C. J., Winter, G. E., Erb, M. A., Scott, T. G., Xu, M., et al. (2018). Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nature Chemical Biology 14, 405-412.

  8. Khan, S., Zhang, X., Lv, D., Zhang, Q., He, Y., Zhang, P., Liu, X., Thummuri, D., Yuan, Y., Wiegand, J. S., et al. (2019). A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nature Medicine 25, 1938-1947.

  9. Lebraud, H., Wright, D. J., Johnson, C. N., and Heightman, T. D. (2016). Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras. ACS Central Science 2, 927-934.

  10. Lu, J., Qian, Y., Altieri, M., Dong, H., Wang, J., Raina, K., Hines, J., Winkler, James D., Crew, Andrew P., Coleman, K., and Crews, Craig M. (2015). Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chemistry & Biology 22, 755-763.

  11. Mayor-Ruiz, C., Bauer, S., Brand, M., Kozicka, Z., Siklos, M., Imrichova, H., Kaltheuner, I. H., Hahn, E., Seiler, K., Koren, A., et al. (2020). Rational discovery of molecular glue degraders via scalable chemical profiling. Nature Chemical Biology 16, 1199-1207.

  12. Posternak, G., Tang, X., Maisonneuve, P., Jin, T., Lavoie, H., Daou, S., Orlicky, S., Goullet de Rugy, T., Caldwell, L., Chan, K., et al. (2020). Functional characterization of a PROTAC directed against BRAF mutant V600E. Nature Chemical Biology 16, 1170-1178.

  13. Raina, K., Lu, J., Qian, Y., Altieri, M., Gordon, D., Rossi, A. M. K., Wang, J., Chen, X., Dong, H., Siu, K., et al. (2016). PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences 113, 7124-7129.

  14. 14.Remillard, D., Buckley, D. L., Paulk, J., Brien, G. L., Sonnett, M., Seo, H.-S., Dastjerdi, S., Wühr, M., Dhe-Paganon, S., Armstrong, S. A., and Bradner, J. E. (2017). Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angewandte Chemie International Edition 56, 5738-5743.

  15. Savitski, M. M., Zinn, N., Faelth-Savitski, M., Poeckel, D., Gade, S., Becher, I., Muelbaier, M., Wagner, A. J., Strohmer, K., Werner, T., et al. (2018). Multiplexed Proteome Dynamics Profiling Reveals Mechanisms Controlling Protein Homeostasis. Cell 173, 260-274.e225.

  16. Słabicki, M., Yoon, H., Koeppel, J., Nitsch, L., Roy Burman, S. S., Di Genua, C., Donovan, K. A., Sperling, A. S., Hunkeler, M., Tsai, J. M., et al. (2020). Small-molecule-induced polymerization triggers degradation of BCL6. Nature 588, 164-168.

  17. Wurz, R. P., Dellamaggiore, K., Dou, H., Javier, N., Lo, M.-C., McCarter, J. D., Mohl, D., Sastri, C., Lipford, J. R., and Cee, V. J. (2017). A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation. Journal of Medicinal Chemistry 61, 453-461.

  18. Zengerle, M., Chan, K.-H., and Ciulli, A. (2015). Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chemical Biology10, 1770-1777.

  19. Zhou, B., Hu, J., Xu, F., Chen, Z., Bai, L., Fernandez-Salas, E., Lin, M., Liu, L., Yang, C.-Y., Zhao, Y., et al. (2017). Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. Journal of Medicinal Chemistry61, 462-481.

  20. Zoppi, V., Hughes, S. J., Maniaci, C., Testa, A., Gmaschitz, T., Wieshofer, C., Koegl, M., Riching, K. M., Daniels, D. L., Spallarossa, A., and Ciulli, A. (2018). Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. Journal of Medicinal Chemistry 62, 699-726.




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