Results 81 to 90 of about 33,100 (295)

VCP‐Regulated LMF2 Stabilizes the Cholesterol Biosynthesis Enzyme HMGCS1 to Drive Cancer Progression and Confer Capecitabine Resistance in Triple‐Negative Breast Cancer

Advanced Science, EarlyView.
LMF2 drives progression and capecitabine resistance in triple‐negative breast cancer (TNBC). Mechanistically, VCP prevents NBR1‐mediated autophagic degradation of LMF2, thereby stabilizing it. Stabilized LMF2 subsequently suppresses NDP52‐mediated autophagic degradation of HMGCS1, a rate‐limiting cholesterol biosynthesis enzyme.
Qian Zhao, Lisa Andriani, Yin‐Ling Zhang, Shao‐Ying Yang, Yun‐Xiao Ling, Min‐Ying Huang, Jia‐Yang Cai, Fang‐Lin Zhang, Xin Hu, A‐Yong Cao, Zhi‐Min Shao, Guang‐Yu Liu, Da‐Qiang Li   +12 more
wiley   +1 more source

Downsizing Electrophilic MAX‐Derived Helical Zipper Peptides to Covalently Bind and Degrade Oncogenic MYC

Angewandte Chemie, EarlyView.
Oncogenic MYC is a transcription factor that is difficult to inhibit. However, precise positioning of an acrylamide electrophile in MAX to covalently bond to the unique Cys438 in MYC, enabled shortening and optimizing of MAX‐derived, helix‐constrained peptides with high‐affinity and selectivity.
Aline Dantas de Araujo, Lei Luo, Mahan Azad, Miao Yu, Jody M. Mason, Junxian Lim, Timothy A. Hill, David P. Fairlie   +7 more
wiley   +2 more sources

New prodrugs against tuberculosis

, 2017
Among the antitubercular agents, most are defined as “prodrugs” such as isoniazid and ethionamide. Adrien Albert was the first to introduce this term in 1958.
PASCA, MARIA ROSALIA, RICCARDI, GIOVANNA, MORI, GIORGIA, CHIARELLI, LAURENT   +3 more
core   +1 more source

Tubocapsenolide A Overcomes Oxaliplatin Resistance in Colorectal Cancer by Targeting PLK1 to Impair CEP55–ESCRT‐Associated Vesicular Damage Clearance

Advanced Science, EarlyView.
Oxaliplatin‐resistant colorectal cancer cells utilize a previously unappreciated PLK1‐CEP55‐ESCRT‐driven vesicular extrusion mechanism to clear L‐OHP‐induced cellular damage. The natural withanolide Tubocapsenolide A directly targets and inhibits PLK1 to disrupt this specific damage‐clearance machinery. This blockade induces severe nucleolar stress and
Yueying Yang, Jing Liang, Lu Wang, Hongyan Zhang, Zhiruo Zhang, Yang Liu, Rui Zhu, Wen Xu, Shaohua Xu, Dejuan Sun, Ke Xiang, Yali Wang, Zhimin Fan, Zheng Wang, Hua Li, Lixia Chen   +15 more
wiley   +1 more source

Photoactivated Platinum Complexes: Targeting Membrane Proteins and Organelles for Precision Cancer Therapy

Angewandte Chemie, EarlyView.
This review highlights an emerging anticancer approach integrating platinum agents into photodynamic therapy (PDT) and photoactivated chemotherapy (PACT) systems, further augmented by cancer cell membrane‐ and organelle‐targeting. By directing photoactivated platinum complexes from nontargeted distribution to cancer cells or defined subcellular sites ...
Shu Chen, Qiyuan Zhou, Jiaqian Xu, Guangyu Zhu   +3 more
wiley   +2 more sources

Engineered human adipose-derived stem cells delivering carboxylesterase and TRAIL for castration-resistant prostate cancer: Translational synthesis [PDF]

Investigative and Clinical Urology
Castration-resistant prostate cancer (CRPC) remains poorly controlled after sequential androgen receptor–targeted agents, taxanes, and radiopharmaceuticals. Tumor-tropic adipose-derived mesenchymal stem cells (ADSCs) offer a compelling platform for local
Jae Heon Kim, Sang Hun Lee, Yun Seob Song   +2 more
doaj   +1 more source

Synthesis of novel prodrugs for antiviral therapy [PDF]

, 2017
This bachelor thesis is dedicated to preparation of prodrugs derived from 2'-C- methyladenosine, which is a potent inhibitor of the RNA dependent RNA polymerase of flaviviruses.
Štefek, Milan
core  

An Oral Antiviral Combination Against Severe COVID‐19 Enabled by the Synergistic Mechanisms of Action of Auranofin and Remdesivir

Advanced Science, EarlyView.
FDA‐approved anti‐inflammatory drug Auranofin inhibits SARS‐CoV‐2 replication by inhibiting viral Main protease activity and Spike processing required for viral entry. It shows strong synergy with nucleoside analogue Remdesivir, due to non‐overlapping mechanisms.
Oyahida Khatun, Rohan Narayan, Santhosh Kambaiah Nagaraj, Rishad Shiraz, Abinaya Kaliappan, Sumandeep Kaur, Ankur Singh, Siva Shanmugam Selvaraj, Gudepalya Renukaiah Rudramurthy, Chakenahalli Naveenkumar, Shridhar Narayanan, Radha Krishan Shandil, Shailly Tomar, Shashank Tripathi   +13 more
wiley   +1 more source

Adapting the plant defense systems’ toolbox of Michael acceptors to electrophilic drug development [PDF]

Exploration of Drug Science
Plant metabolites are an invaluable source of bioactive molecules, and a high percentage of them can react covalently with their targets. Lipid-derived α,β-unsaturated systems (Michael acceptors), which are present in all plants, regulate signaling ...
Monika I. Konaklieva, Balbina J. Plotkin
doaj   +1 more source

Harnessing Methylselenol (CH3SeH): A Highly Effective Platform for Stimuli‐Responsive Delivery With Therapeutic Potential

Advanced Science, EarlyView.
Tools for controlled selenol delivery are crucial for exploring Se‐related biology and medicine, but compound platforms for triggerable release of CH3SeH remain lacking. Herein, we report the first general triggered platform (TD‐MSe) for efficient cyclization release of CH3SeH in live cells.
Wenfang Liang, Liyue Wang, Xuan Wang, Xinran Li, Hao Xing, Lu Sun, Zhen Xi, Long Yi   +7 more
wiley   +1 more source