Results 1 to 10 of about 1,110,261 (265)
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties
Sarath Ramachandran +10 more
doaj +1 more source
Background LINC00173 had been reported as a cisplatin (cis-diamminedichloroplatinum, DDP) chemotherapy-resistant inducer in small-cell lung cancer (SCLC) and lung squamous cell carcinoma (LUSC). This study aimed to display reverse data for LINC00173 as a
Xingyu Tao +10 more
doaj +1 more source
A core‐shell‐structured Cu2O@Mn3Cu3O8 (CMCO) nanozyme is constructed to serve as a tumor microenvironment (TME)‐activated copper ionophore to achieve safe and efficient cuproptosis.
Wei Chen +6 more
doaj +1 more source
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
Qingzi Chen +12 more
doaj +1 more source
CHD1L augments autophagy-mediated migration of hepatocellular carcinoma through targeting ZKSCAN3
Autophagy is an important biological process in normal cells. However, how it affects tumor progression still remains poorly understood. Herein, we demonstrated that the oncogenic protein Chromodomain-helicase-DNA-binding-protein 1-like gene (CHD1L ...
Xiaofeng Zhang +14 more
doaj +1 more source
Gambogic Acid Is a Tissue-Specific Proteasome Inhibitor In Vitro and In Vivo
Gambogic acid (GA) is a natural compound derived from Chinese herbs that has been approved by the Chinese Food and Drug Administration for clinical trials in cancer patients; however, its molecular targets have not been thoroughly studied.
Xiaofen Li +28 more
doaj +1 more source
Background Acquired imatinib (IM) resistance is frequently characterized by Bcr-Abl mutations that affect IM binding and kinase inhibition in patients with chronic myelogenous leukemia (CML).
Xiaoying Lan +13 more
doaj +1 more source
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally ...
Christiane Kofink +29 more
doaj +1 more source
Background Ovarian carcinoma is one of the most aggressive gynecological malignant neoplasms and makes up 25–30% of all cancer cases of the female genital tract.
Hongbiao Huang +14 more
doaj +1 more source
UPRmt and coordinated UPRER in type 2 diabetes
The mitochondrial unfolded protein response (UPRmt) is a molecular mechanism that maintains mitochondrial proteostasis under stress and is closely related to various metabolic diseases, such as type 2 diabetes (T2D).
Zhanfang Kang +6 more
doaj +1 more source

