Molecular glue concept solidifies

被引:43
作者
Baek, Kheewoong [1 ]
Schulman, Brenda A. [1 ]
机构
[1] Max Planck Inst Biochem, Dept Mol Machines & Signaling, Martinsried, Germany
关键词
SELECTIVE DEGRADATION; STRUCTURAL BASIS;
D O I
10.1038/s41589-019-0414-3
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Molecular-glue-mediated proximity-induced degradation now allows unprecedented therapeutic targeting of previously undruggable proteins. Structures showing how aryl-sulfonamides mediate recruitment of the splicing factor RBM39 to the E3 CRL4(DCAF15) broaden the mechanistic principles by which molecular glues target ubiquitylation.
引用
收藏
页码:2 / 3
页数:2
相关论文
共 9 条
[1]   Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex [J].
Bussiere, Dirksen E. ;
Xie, Lili ;
Srinivas, Honnappa ;
Shu, Wei ;
Burke, Ashley ;
Be, Celine ;
Zhao, Junping ;
Godbole, Adarsh ;
King, Dan ;
Karki, Rajeshri G. ;
Hornak, Viktor ;
Xu, Fangmin ;
Cobb, Jennifer ;
Carte, Nathalie ;
Frank, Andreas O. ;
Frommlet, Alexandra ;
Graff, Patrick ;
Knapp, Mark ;
Fazal, Aleem ;
Okram, Barun ;
Jiang, Songchun ;
Michellys, Pierre-Yves ;
Beckwith, Rohan ;
Voshol, Hans ;
Wiesmann, Christian ;
Solomon, Jonathan M. ;
Paulk, Joshiawa .
NATURE CHEMICAL BIOLOGY, 2020, 16 (01) :15-+
[2]   Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820 [J].
Du, Xinlin ;
Volkov, Oleg A. ;
Czerwinski, Robert M. ;
Tan, HuiLing ;
Huerta, Carlos ;
Morton, Emily R. ;
Rizzi, Jim P. ;
Wehn, Paul M. ;
Xu, Rui ;
Nijhawan, Deepak ;
Wallace, Eli M. .
STRUCTURE, 2019, 27 (11) :1625-+
[3]   Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15 [J].
Faust, Tyler B. ;
Yoon, Hojong ;
Nowak, Radoslaw P. ;
Donovan, Katherine A. ;
Li, Zhengnian ;
Cai, Quan ;
Eleuteri, Nicholas A. ;
Zhang, Tinghu ;
Gray, Nathanael S. ;
Fischer, Eric S. .
NATURE CHEMICAL BIOLOGY, 2020, 16 (01) :7-+
[4]   Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15 [J].
Han, Ting ;
Goralski, Maria ;
Gaskill, Nicholas ;
Capota, Emanuela ;
Kim, Jiwoong ;
Ting, Tabitha C. ;
Xie, Yang ;
Williams, Noelle S. ;
Nijhawan, Deepak .
SCIENCE, 2017, 356 (6336)
[5]   Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells [J].
Kroenke, Jan ;
Udeshi, Namrata D. ;
Narla, Anupama ;
Grauman, Peter ;
Hurst, Slater N. ;
McConkey, Marie ;
Svinkina, Tanya ;
Heckl, Dirk ;
Comer, Eamon ;
Li, Xiaoyu ;
Ciarlo, Christie ;
Hartman, Emily ;
Munshi, Nikhil ;
Schenone, Monica ;
Schreiber, Stuart L. ;
Carr, Steven A. ;
Ebert, Benjamin L. .
SCIENCE, 2014, 343 (6168) :301-305
[6]   Plasticity in binding confers selectivity in ligand-induced protein degradation [J].
Nowak, Radoslaw P. ;
DeAngelo, Stephen L. ;
Buckley, Dennis ;
He, Zhixiang ;
Donovan, Katherine A. ;
An, Jian ;
Safaee, Nozhat ;
Jedrychowski, Mark P. ;
Ponthier, Charles M. ;
Ishoey, Mette ;
Zhang, Tinghu ;
Mancias, Joseph D. ;
Gray, Nathanael S. ;
Bradner, James E. ;
Fischer, Eric S. .
NATURE CHEMICAL BIOLOGY, 2018, 14 (07) :706-+
[7]   Structural basis of lenalidomide-induced CK1α degradation by the CRL4CRBN ubiquitin ligase [J].
Petzold, Georg ;
Fischer, Eric S. ;
Thomae, Nicolas H. .
NATURE, 2016, 532 (7597) :127-+
[8]   Mechanism of auxin perception by the TIR1 ubiquitin ligase [J].
Tan, Xu ;
Calderon-Villalobos, Luz Irina A. ;
Sharon, Michal ;
Zheng, Changxue ;
Robinson, Carol V. ;
Estelle, Mark ;
Zheng, Ning .
NATURE, 2007, 446 (7136) :640-645
[9]   Selective degradation of splicing factor CAPERα by anticancer sulfonamides [J].
Uehara, Taisuke ;
Minoshima, Yukinori ;
Sagane, Koji ;
Sugi, Naoko Hata ;
Mitsuhashi, Kaoru Ogawa ;
Yamamoto, Noboru ;
Kamiyama, Hiroshi ;
Takahashi, Kentaro ;
Kotake, Yoshihiko ;
Uesugi, Mai ;
Yokoi, Akira ;
Inoue, Atsushi ;
Yoshida, Taku ;
Mabuchi, Miyuki ;
Tanaka, Akito ;
Owa, Takashi .
NATURE CHEMICAL BIOLOGY, 2017, 13 (06) :675-+