Non-small molecule PROTACs (NSM-PROTACs): Protein degradation kaleidoscope
Sinan Ma,Jian-Ai Ji,Yuanyuan Tong,Yuxuan Zhu,Junwei Dou,Xian Zhang,Shicheng Xu,Tianbao Zhu,Xiao-Li Xu,Qidong You,Zheng-Yu Jiang +10 more
Reads0
Chats0
TLDR
In this article , the authors introduce the types of non-small molecule PROTACs, describe the advantages of NSM-PROTACs and summarize the development of NMT-PROPACs so far in detail.About:
This article is published in Acta Pharmaceutica Sinica B.The article was published on 2022-02-01 and is currently open access. It has received 7 citations till now. The article focuses on the topics: Medicine.read more
Citations
More filters
Journal ArticleDOI
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.
TL;DR: This work will summarize the latest development of representative PROTACs focusing on research mainly in past 10 years and discuss their advantages and disadvantages, as well as the outlook and perspectives on the associated challenges and future directions.
Journal ArticleDOI
Discovery of novel protein degraders based on bioorthogonal reaction-driven intracellular self-assembly strategy.
TL;DR: In this paper , a bio-orthogonal reaction-driven self-assembly strategy was proposed to improve the degradation performance of PROTACs in living cells, and the results demonstrated that a highly specific bio-on-off reaction driven intracellular selfassembly strategy could be utilized to improve degradation performance.
Journal ArticleDOI
Construction of lncRNA- and circRNA-associated ceRNA networks in the prostatic urethra of rats after simulating transurethral laser prostatectomy (TULP).
TL;DR: Wang et al. as mentioned in this paper constructed the lncRNA- and circRNA-associated ceRNA regulatory networks related to wound repair after TULP in rats, and provided theoretical support for the repair of post-prostatectomy wound.
Journal ArticleDOI
Stimuli-activatable PROTACs for precise protein degradation and cancer therapy.
Jing Gao,Lei Yang,Shumin Lei,Fengqi Zhou,Huijun Nie,Bo Peng,Tianfeng Xu,Xiaohua Chen,Xiaobao Yang,Chunquan Sheng,Yu Rao,Kanyi Pu,Jian Jin,Zhiai Xu,Haijun Yu +14 more
TL;DR: In this paper , the authors summarized the cutting-edge advances of the stimuli-activatable PROTAC prodrugs and discussed the progress of PROTAC-based nanomedicine to improve PROTAC delivery to the tumors and precise POI degradation in the targeted cells.
Journal ArticleDOI
Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design.
TL;DR: The current status of E3 ligases and corresponding ligands for PROTACs design with a focus on their discovery history, design principles, application benefits, and potential defects are summarized in this paper .
References
More filters
Journal ArticleDOI
Recurrent Fusion of TMPRSS2 and ETS Transcription Factor Genes in Prostate Cancer
Scott A. Tomlins,Daniel R. Rhodes,Sven Perner,Saravana M. Dhanasekaran,Rohit Mehra,Xiao-Wei Sun,Sooryanarayana Varambally,Xuhong Cao,Joelle Tchinda,Rainer Kuefer,Charles Lee,James E. Montie,Rajal B. Shah,Kenneth J. Pienta,Mark A. Rubin,Arul M. Chinnaiyan +15 more
TL;DR: In this article, the authors used a bioinformatics approach to discover candidate oncogenic chromosomal aberrations on the basis of outlier gene expression and identified recurrent gene fusions of the 5' untranslated region of TMPRSS2 to ERG or ETV1.
Journal ArticleDOI
Peptide therapeutics: current status and future directions.
Keld Fosgerau,Torsten Hoffmann +1 more
TL;DR: The current status, strengths, and weaknesses of peptides as medicines and the emerging new opportunities in peptide drug design and development are discussed.
Journal ArticleDOI
The Human Transcription Factors.
Samuel A. Lambert,Arttu Jolma,Laura F. Campitelli,Pratyush Kumar Das,Yimeng Yin,Mihai Albu,Xiaoting Chen,Jussi Taipale,Jussi Taipale,Jussi Taipale,Timothy P. Hughes,Matthew T. Weirauch,Matthew T. Weirauch +12 more
TL;DR: This review considers how TFs are identified and functionally characterized, principally through the lens of a catalog of over 1,600 likely human TFs and binding motifs for two-thirds of them, highlighting the importance of continued effort to understand TF-mediated gene regulation.
Journal ArticleDOI
HaloTag: A Novel Protein Labeling Technology for Cell Imaging and Protein Analysis
Georgyi V. Los,Lance P. Encell,Mark McDougall,Danette Hartzell,Natasha Karassina,Chad Zimprich,Monika G. Wood,Randy Learish,Rachel Friedman Ohana,Marjeta Urh,Daniel J. Simpson,Jacqui Méndez,Kris Zimmerman,Paul Otto,Gediminas Vidugiris,Ji Zhu,Aldis Darzins,Dieter Klaubert,Robert F. Bulleit,Keith V. Wood +19 more
TL;DR: The utility of this modular protein tagging system for cellular imaging and protein immobilization is demonstrated by analyzing multiple molecular processes associated with NF-kappaB-mediated cellular physiology, including imaging of subcellular protein translocation and capture of protein--protein and protein--DNA complexes.
Journal ArticleDOI
Impaired degradation of mutant α-synuclein by chaperone-mediated autophagy
TL;DR: It is found that wild-type α-synuclein was selectively translocated into lysosomes for degradation by the chaperone-mediated autophagy pathway, which may underlie the toxic gain-of-function by the A53T and A30P mutants.