Results 221 to 230 of about 4,518,745 (345)

Discovery of SKP2‐Recruiting PROTACs for Target Protein Degradation

Advanced Science, EarlyView.
Based on the SKP2‐targeting ligand SL1, we designed non‐covalent PROTACs by linking it with the BRD4 inhibitor JQ1 and the AR antagonist AL through a linker. These PROTACs successfully induced the ubiquitination of BRD4 and AR, followed by proteasome‐mediated degradation.
Guanjun Dong, Aima Huang, Ziqing Zhao, Bikai Lai, Xin Pan, Huiyu Yang, Xiaohan Xu, Tianwei Wang, Fangchen Zhao, Zhimin Zhang, Yongbo Xue, Guanjun Deng, Wenbin Deng, Jianwei Chen   +13 more
wiley   +1 more source

Improved analysis of in vivo drug combination experiments with a comprehensive statistical framework and web-tool. [PDF]

Nat Commun
Romero-Becerra R, Zhao Z, Nebdal D, Müller E, Bergholtz H, Norum JH, Aittokallio T.   +6 more
europepmc   +1 more source

Phase Separation of NFIB Suppresses SLC3A2‐Mediated Ferroptosis in Castration‐Resistant Prostate Cancer

Advanced Science, EarlyView.
Castration‐resistant prostate cancer (CRPC) remains sensitive to ferroptosis, but its intrinsic resistance is poorly understood. Here, we identify NFIB as a master suppressor. SIRT7‐mediated NFIB acetylation drives its liquid–liquid phase separation, which promotes SLC3A2 transcription to inhibit ferroptosis.
Qiunuo Li, Danyang Chen, Yongzhen Xia, Yili Long, Nan Huang, Rongna Li, Mengting Shi, Mairehaba Kadier, Huafeng Luo, Xiaohui Chen, Hao Liu, Guanmin Jiang   +11 more
wiley   +1 more source

In vitro Screening for Synergistic Polymyxin B-Based Combinations Against KPC- Producing Carbapenem-Resistant <i>Klebsiella pneumoniae</i>. [PDF]

Drug Des Devel Ther
Lv M, Yi H, Liu Y, Xie Y, Cheng Z, Xie F, Li S.   +6 more
europepmc   +1 more source

Cuproptosis and Disulfidptosis Converge to Empower PD‐L1 Checkpoint Therapy via Cadict‐Induced PD‐L1 Translation

Advanced Science, EarlyView.
This study introduces Cadict, an EGFR‐targeted nanodrug that co‐delivers cuproptosis and disulfidptosis inducers to overcome immune resistance. Cadict synergistically enhances tumor cytotoxicity and sensitizes cancers to ICIs by upregulating PD‐L1 via an Eif5b‐dependent translation mechanism, fostering a potent antitumor immune response and ...
Shaoqing Huang, Shiyao Song, Xinhua Zhang, Jialing Gao, Ruihan Pu, Jiatong Dai, Xiaoxue Wu, Lulu Chen, Qinghai Li, Xiaoting Liu, Qi Zhou, Mei Song, Weiling He   +12 more
wiley   +1 more source

Dissecting the role of mineralocorticoid receptors in binge-like alcohol drinking in mice: Finerenone as a potential pharmacotherapy. [PDF]

Psychopharmacology (Berl)
Wilkinson CS, Bruns N, Pince CL, McGinn MA, Farokhnia M, Leggio L, Vendruscolo LF.   +6 more
europepmc   +1 more source

De Novo Design and Directed Evolution Refinement of Mirror‐Image Protein Binders Targeting Interleukin‐4

Advanced Science, EarlyView.
This study presents the de novo design and directed evolution of a mirror‐image D‐protein inhibitor targeting human interleukin‐4 (IL‐4). The engineered molecule exhibits nanomolar binding affinity for IL‐4 and effectively inhibits IL‐4–mediated signaling.
Liqing Xu, Yuxiang Ren, Tongyue Wang, Hongyong Li, Yue Yao, Lei Liu, Ke Sun, Peilong Lu   +7 more
wiley   +1 more source

Kappa-Opioid Receptor Antagonism Prolongs the Antidepressant Effects of Ketamine in Adult Mice with Depression-like Behavior Induced by Adolescent Chronic Unpredictable Stress. [PDF]

Int J Mol Sci
Zivanovic A, Mitic M, Lukic I, Glavonic E, Adzic M, Ivkovic S.   +5 more
europepmc   +1 more source

Deciphering and Targeting the Schwannoma‐Neuron‐Macrophage Crosstalk for the Treatment of Schwannomatosis and Associated Pain

Advanced Science, EarlyView.
We established patient‐derived SWN cell lines and orthotopic PDX models that recapitulate patient pain phenotypes, alongside a novel intravital DRG imaging platform to track macrophage infiltration and neuronal pain responses. Using these models, we define HMGB1–CCL2–IL‐6 signaling crosstalk driving pain and identify EGF signaling as a key regulator of
Zhenzhen Yin, Limeng Wu, Yanling Zhang, Yao Sun, Grace Y. Lee, Simeng Lu, Xing Gao, John W. Chen, Sonu Subudhi, William Ho, Chao Zhu, Jun Ren, Gino B. Ferraro, Alona Muzikansky, Anat Stemmer‐Rachamimov, Jianren Mao, Scott R. Plotkin, Lei Xu   +17 more
wiley   +1 more source

Targeting Growth Hormone Receptor to Overcome Therapy Resistance in Non-Small Cell Lung Cancer. [PDF]

Int J Mol Sci
Ahmad A, Basu R, Fyffe C, Geiger R, Walsh C, Minto D, Brenya E, Alur AV, Neggers SJCMM, Kopchick JJ.   +9 more
europepmc   +1 more source