Results 181 to 190 of about 69,829 (264)

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source

Engineering Synergistic Intra‐/Intermolecular Conformational Locking via Side‐Chain Branching: A β‐Sheet‐Inspired Strategy for Planar NIR‐II Phototheranostic Aggregates

Advanced Science, EarlyView.
A bio‐inspired side‐chain branching strategy is developed to orchestrate a dual noncovalent conformational locking (NoCL) network, enabling the construction of perfectly planar NIR‐II phototheranostic aggregates. Such structural precision maximizes light‐harvesting efficiency and optimizes exciton dynamics, ensuring synchronized enhancements in NIR‐II ...
Cheng Lu, Qian Jia, Bo Wu, Chao Li, Ryan T. K. Kwok, Tie‐Gen Chen, Jianwei Sun, Zheng Zhao, Teng‐Teng Chen, Zhongliang Wang, Jacky W. Y. Lam, Ben Zhong Tang   +11 more
wiley   +1 more source

Role of IRE1α/XBP1/CHOP/NLRP3 Signalling Pathway in Neonicotinoid Imidacloprid-Induced Pancreatic Dysfunction in Rats and Antagonism of Lycopene: In Vivo and Molecular Docking Simulation Approaches. [PDF]

Toxics
El Gazzar WB, Bayoumi H, Youssef HS, Ibrahim TA, Abdelfatah RM, Gamil NM, Iskandar MK, Abdel-Kareim AM, Abdelrahman SM, Gebba MA, Mohamed MA, Mokhtar MM, Kharboush TG, Bayoumy NM, Alomar HA, Farag AA.   +15 more
europepmc   +1 more source

Anti-aging Effects of Mangosteen Peel Extract and Its Phytochemical Compounds: Antioxidant Activity, Enzyme Inhibition and Molecular Docking Simulation. [PDF]

Trop Life Sci Res, 2020
Widowati W, Ginting CN, Lister INE, Girsang E, Amalia A, Wibowo SHB, Kusuma HSW, Rizal.   +7 more
europepmc   +1 more source

Cancer‐Associated BCL‐2 Mutants Reveal Mechanisms Towards Venetoclax Resistance

Advanced Science, EarlyView.
Venetoclax (VEN) resistance in chronic lymphocytic leukemia arises from diverse BCL2 mutations. We map mechanisms contributing to VEN resistance across common BCL‐2 variants. G101V and D103Y reduce drug binding and increase sequestration of pro‐apoptotic proteins. V156D blocks VEN allosterically.
Jonas Aufdermauer, Ian de Ridder, Mahjoobeh Ehsani, Marasim Khan, Justin Kale, Lukas P. Frenzel, David Andrews, Spyridoula Karamanou, Ana J. Garcia‐Saez, Geert Bultynck   +9 more
wiley   +1 more source

SPSB1 Promotes Subcutaneous Adipose Hyperplasia in Facial Port‐Wine Stains by Controlling HDAC1 Degradation and Stability Through Two Distinct Proteolytic Pathways

Advanced Science, EarlyView.
In PWS‐ASPCs, FOSL1 drives the expression of SPSB1. SPSB1, as part of the ESC complex, further binds to HDAC1 and promotes K29‐linked and K48‐linked polyubiquitination of HDAC1. These modifications facilitate the degradation of HDAC1 through the ALP and UPS pathways, respectively.
Hongrui Chen, Bin Sun, Yajing Qiu, Chen Hua, Xiaoxi Lin, Wei Gao   +5 more
wiley   +1 more source

Pyrazole‐Derived Antibacterial Compounds Effectively Treat Methicillin‐Resistant Staphylococcus Aureus Infections by Inhibiting Aspartate Transcarbamoylase

Advanced Science, EarlyView.
This study unveils a novel antibacterial mechanism against MRSA, in which the compound Py‐27 selectively targets and inhibits aspartate transcarbamoylase (ATCase), a key enzyme in pyrimidine synthesis. This inhibition disrupts DNA replication, induces oxidative damage, leading to potent bactericidal activity.
Xiaorong Yang, Xinyuan Cao, Lixia Dai, Feng Yang, Jing Wang, Yudong Ma, Tong Bu, Zile Gong, Xueyan Liu, Changcai Bai, Xiaolou Miao, Xiaofei Shang   +11 more
wiley   +1 more source

Ahcy Acts as an Effector of Hnf4a‐Driven Super‐Enhancer Activation to Alleviate MASLD During Intermittent Fasting

Advanced Science, EarlyView.
Our study identifies an Hnf4a‐driven super‐enhancer of hepatic Ahcy that mediates the protective effects of intermittent fasting against MASLD. Disruption of the Ahcy super‐enhancer reduces Ahcy expression and exacerbates lipid accumulation. This pathway prevents aberrant promoter hypermethylation by maintaining the SAM/SAH balance, as exemplified by ...
Huafeng Chen, Shilin Zhang, Xiaojie Deng, Wenqiang Xie, Fen Xu, Jie Shen, Hua Liang   +6 more
wiley   +1 more source

A density functional theory study on silver and bis-silver complexes with lighter tetrylene: are silver and bis-silver carbenes candidates for SARS-CoV-2 inhibition? Insight from molecular docking simulation. [PDF]

RSC Adv, 2020
Bui TQ, Phuong Loan HT, Ai My TT, Quang DT, Phuong Thuy BT, Nhan VD, Quy PT, Van Tat P, Dao DQ, Trung NT, Huynh LK, Ai Nhung NT.   +11 more
europepmc   +1 more source

Interference of ATP‐Binding Cassette Transporter by Functional Nano‐Delivery System for High Efficiency Management of Insecticide‐Resistant Nilaparvata lugens

Advanced Science, EarlyView.
A ZIF‐90 nanocarrier delivers dinotefuran and suppresses NlABCG3 and NlABCH1 in resistant Nilaparvata lugens. This system combines pH/ATP‐triggered release with enhanced foliar retention, improving efficacy while sparing honeybees and promoting rice growth, offering a promising resistance‐breaking strategy.
Chengshuai He, Hejun Ren, Shuo Zhang, Jikang Cheng, Hui Zhang, Jiao Liu, Sijie Wang, Congfen Gao, Yanchao Zhang, Yunhao Gao   +9 more
wiley   +1 more source