Results 151 to 160 of about 109,331 (244)

A Versatile DNA‐Encoded Library Platform for the Discovery of Highly Cooperative Chemical Inducers of Proximity

Advanced Science, EarlyView.
We present a versatile DNA‐encoded library (DEL) platform designed for rapid library synthesis and subsequent screening for chemical inducers of proximity (CIPs) across various presenter proteins of choice. Applying this approach, we discovered a novel molecular glue‐like compound mediating CRBN‐BRD9 ternary complex formation with remarkable ...
Bingqi Tong, Sunny A. Tang, Yifan Deng, Zhihan Nan, Alison X. Gao, Gregory A. Michaud, Simone Bonazzi, Frédéric Berst, Frédéric J. Zécri, Shuang Liu, William J. Gibson, Stuart L. Schreiber   +11 more
wiley   +1 more source

Granzyme B PET Imaging Reveals Lgmn+ Macrophage‐Mediated Immune Evasion and Guides Immunotherapy in EGFR‐TKI‐Resistant NSCLC

Advanced Science, EarlyView.
Graphical illustration of 68Ga‐GZB PET/CT imaging reveals immune dynamics post‐EGFR‐TKI resistance in NSCLC; Lgmn+ macrophages‐derived Lgmn‐containing extracellular vesicles inhibit glycolysis, induce CD8+ T cell exhaustion, and targeting Lgmn restores immunotherapy sensitivity.
Dongliang Wang, Wenqin Luo, Qiufang Liu, Wenxuan Tang, Bin Zhu, Jiwei Chen, Qian Zhou, Shuang Tang, Xiaoping Xu, Shaoli Song   +9 more
wiley   +1 more source

A guide to mapping ubiquitin and ubiquitin-like E3 ligases to their substrates. [PDF]

FEBS J
Merino-Cacho L, Guinea-Pérez C, Pozo-Rodríguez M, Cano-López S, Ramirez J, Barroso-Gomila O, Mayor U, Sutherland JD, Barrio R.   +8 more
europepmc   +1 more source

Nuclear Translocation of PFKFB3 Promotes Disuse‐Induced Muscle Atrophy via Scaffolding Nedd4‐Mediated JunB Ubiquitination

Advanced Science, EarlyView.
Disuse‐induced muscle atrophy is driven by a non‐metabolic, nuclear function of the enzyme PFKFB3. Acting as a scaffold, PFKFB3 facilitates Nedd4‐mediated ubiquitination and degradation of the anti‐atrophy transcription factor JunB. Inhibiting this novel PFKFB3–Nedd4–JunB signaling axis stabilizes JunB and alleviates muscle wasting, revealing a highly ...
Mengjun Ma, Yinliang Liu, Wangchang Wu, Biao Yang, Jiahao Zhuang, Haoye Yu, Rujia Mi, Yixuan Lu, Wen Yang, Hanting Yi, Chenglong Yuan, Yinfeng Gu, Hongyu Li   +12 more
wiley   +1 more source

E3 Ligases and Deubiquitinases in Controlling High-Mobility Group Box (HMGB) Protein Functions. [PDF]

Int J Mol Sci
Chikhirzhina EV, Tomilin AN, Tsimokha AS.   +2 more
europepmc   +1 more source

Epigenetic Silencing of CYYR1 Promotes Lung Adenocarcinoma Progression Through TRIM21‐Dependent Regulation of HMMR Stability

Advanced Science, EarlyView.
CYYR1 as an epigenetically dysregulated tumor‐suppressive factor that influences oncoprotein stability through TRIM21‐dependent HMMR regulation and reveals a potential therapeutic vulnerability in CYYR1‐deficient LUAD. The graphical illustration was created using FigDraw (www.figdraw.com).
Fengsheng Dai, Jingyi Tang, Huan Rong, Yu Wang, Xiangyi Zhou, Can Xu, Jianhua Wang, Lili Li, Yue Wu, Fei Deng, Dan Yang, Xiao Yang, Renyan Li, Yongzhong Wu, Dongxi Xiang, Tingxiu Xiang   +15 more
wiley   +1 more source

Exploring Novel E3 Ligases and Neosubstrates for Molecular Glue Degraders and Therapeutic Applications in Cancer. [PDF]

Oncol Res
Jang JH, Kim JY, Lee TJ.
europepmc   +1 more source

TROP2‐Targeting Chimeras (TRTACs) for Tumor Cell‐Selective Membrane Protein Degradation and Enhanced Drug Delivery

Advanced Science, EarlyView.
TROP2 is identified as a novel tumor‐selective lysosomal‐targeting receptor with established clinical relevance. TROP2‐targeting chimeras (TRTACs) are developed by genetically fusing a TROP2‐binding nanobody to nanobodies against specific target proteins.
Luping Chen, Xinying Fu, Wenqian Dong, Xiaobei Deng, Simin Chen, Fujun Wang, Jian Zhao, Shiqun Shao, Liqiang Fan, Jingyu Zhang, Lixin Zhang   +10 more
wiley   +1 more source

A structural code for assembly specificity in GID/CTLH-type E3 ligases. [PDF]

Elife
van Gen Hassend PM, Schindelin H.
europepmc   +1 more source

Degrading GPX4 via Biomimetic Nanoparticle‐Mediated In Situ Synthesis of Deep‐Learning‐Designed Binder‐Degron Chimeras for Prostate Cancer Therapy

Advanced Science, EarlyView.
A deep‐learning‐designed binder is fused to a combinatorial degron to create a binder‐degron chimera (bdC) that recruits the CUL2‐RING ubiquitin ligase complex. Encapsulation in a prostate‐cancer‐targeted, CD47‐camouflaged nanocarrier enables tumor‐specific in situ bdC expression, triggering GPX4 degradation and ferroptosis, thereby establishing a ...
Si‐Han Zhang, Ye An, Na Zeng, Mei‐Cheng Liu, Jian‐Xuan Sun, Xi Gong, Jin‐Zhou Xu, Shao‐Gang Wang, Qi‐Dong Xia   +8 more
wiley   +1 more source