Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines

Autor: Gisele Nishiguchi, Lauren G. Mascibroda, Sarah M. Young, Elizabeth A. Caine, Sherif Abdelhamed, Jeffrey J. Kooijman, Darcie J. Miller, Sourav Das, Kevin McGowan, Anand Mayasundari, Zhe Shi, Juan M. Barajas, Ryan Hiltenbrand, Anup Aggarwal, Yunchao Chang, Vibhor Mishra, Shilpa Narina, Melvin Thomas, Allister J. Loughran, Ravi Kalathur, Kaiwen Yu, Suiping Zhou, Xusheng Wang, Anthony A. High, Junmin Peng, Shondra M. Pruett-Miller, Danette L. Daniels, Marjeta Urh, Anang A. Shelat, Charles G. Mullighan, Kristin M. Riching, Guido J. R. Zaman, Marcus Fischer, Jeffery M. Klco, Zoran Rankovic

Publikováno v: Nature Communications, Vol 15, Iss 1, Pp 1-17 (2024)

Abstract Molecular-glue degraders are small molecules that induce a specific interaction between an E3 ligase and a target protein, resulting in the target proteolysis. The discovery of molecular glue degraders currently relies mostly on screening ap

Externí odkaz: https://doaj.org/article/93a742dfa7284effac1e877a18d0d84e

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Phenyl Dihydrouracil: An Alternative Cereblon Binder for PROTAC Design

Autor: Jamie A. Jarusiewicz, Satoshi Yoshimura, Anand Mayasundari, Marisa Actis, Anup Aggarwal, Kevin McGowan, Lei Yang, Yong Li, Xiang Fu, Vibhor Mishra, Richard Heath, Shilpa Narina, Shondra M. Pruett-Miller, Gisele Nishiguchi, Jun J. Yang, Zoran Rankovic

Publikováno v: ACS Medicinal Chemistry Letters. 14:141-145

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::17e763d52cb06a3a95f14566fa22a1c0
https://doi.org/10.1021/acsmedchemlett.2c00436

Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.

Autor: Min, Jaeki¹ (AUTHOR), Mayasundari, Anand¹ (AUTHOR), Keramatnia, Fatemeh¹ (AUTHOR), Jonchere, Barbara² (AUTHOR), Yang, Seung Wook³ (AUTHOR), Jarusiewicz, Jamie¹ (AUTHOR), Actis, Marisa¹ (AUTHOR), Das, Sourav¹ (AUTHOR), Young, Brandon¹ (AUTHOR), Slavish, Jake¹ (AUTHOR), Yang, Lei¹ (AUTHOR), Li, Yong¹ (AUTHOR), Fu, Xiang¹ (AUTHOR), Garrett, Shalandus H.¹ (AUTHOR), Yun, Mi‐Kyung⁴ (AUTHOR), Li, Zhenmei⁴ (AUTHOR), Nithianantham, Stanley¹ (AUTHOR), Chai, Sergio¹ (AUTHOR), Chen, Taosheng¹ (AUTHOR), Shelat, Anang¹ (AUTHOR)

Publikováno v: Angewandte Chemie. 12/13/2021, Vol. 133 Issue 51, p26867-26874. 8p.

Rationally Designed Potent and Selective CK1α Degraders Exert Antiproliferative Activity Against a Broad Range of Human Cancer Cell Lines

Autor: Zoran Rankovic, Gisele Nishiguchi, Sherif Abdelhamed, Sarah Young, Elizabeth Caine, Lauren Mascibroda, Jeffrey Kooijman, Sourav Das, Darcie Miller, Kevin McGowan, Anand Mayasundari, Zhe Shi, Juan Barajas, Ryan Hiltenbrand, Anup Aggarwal, Yunchao Chang, Vibhor Mishra, Ravi Kalathur, Junmin Peng, Shondra Pruett-Miller, Danette Daniels, Marjeta Urh, Anang Shelat, Charles Mullighan, Kristin Riching, Guido Zaman, Marcus Fischer, Jeffery Klco, Shilpa Narina, Allister Loughran, Anthony High

While the PROTAC approach to targeted protein degradation greatly benefits from rational design, the discovery of molecular glue degraders currently relies on screening strategies. Here, we describe screening of a library containing 3,630 cereblon bi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::11f99fdfcf76b30197d41aed82ba9b1d
https://doi.org/10.21203/rs.3.rs-2883533/v1