Results 41 to 50 of about 3,370 (187)

Profiling the Antimalarial Mechanism of Artemisinin by Identifying Crucial Target Proteins

open access: yesEngineering, 2023
The widespread use of artemisinin (ART) and its derivatives has significantly reduced the global burden of malaria; however, malaria still poses a serious threat to global health.
Peng Gao   +10 more
doaj   +1 more source

Canagliflozin Alleviates Diabetic Glomerular Endothelial Injury via Melibiose in a Microbiota‐Dependent Manner

open access: yesAdvanced Science, EarlyView.
Canagliflozin treatment reshapes the gut microbiota in DKD and elevates levels of melibiose, a metabolite derived from Roseburia intestinalis. Melibiose directly binds to and enhances the enzymatic activity of glyoxalase 1, leading to decreased methylglyoxal accumulation.
Wei Zhang   +32 more
wiley   +1 more source

Determination of Ligand-Target Interaction in vitro by Cellular Thermal Shift Assay and Isothermal Dose-response Fingerprint Assay

open access: yesBio-Protocol
The cellular thermal shift assay (CETSA) and isothermal dose-response fingerprint assay (ITDRF CETSA) have been introduced as powerful tools for investigating target engagement by measuring ligand-triggered thermodynamic stabilization of cellular target ...
Danyu Du, Shengtao Yuan, Jing Xiong
doaj   +1 more source

Chemoproteomic Identification of AKT2 as a Paclitaxel‐Binding Protein via C─C Bond‐Linked Probe PTX‐4 in Paclitaxel‐Resistant Breast Cancer

open access: yesAdvanced Science, EarlyView.
ABSTRACT Breast cancer remains one of the most prevalent malignancies among women, and taxane‐based chemotherapies such as paclitaxel and docetaxel are central to standard treatment regimens. However, drug resistance in breast cancer limits therapeutic efficacy and contributes to recurrence and metastasis.
Kai Wang   +7 more
wiley   +1 more source

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil [PDF]

open access: yesNature Communications, 2016
AbstractTarget engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on biophysical measurements of intracellular target binding, exemplified by human ...
Helena Almqvist   +10 more
openaire   +7 more sources

Interactions of Destruxin A with Silkworms’ Arginine tRNA Synthetase and Lamin-C Proteins

open access: yesToxins, 2020
Destruxin A (DA), a cyclodepsipeptidic mycotoxin produced by entomopathogenic fungus Metarhizium anisopliae, has good insecticidal activity and potential to be a new pesticide. However, the mechanism of action is still obscure.
Jingjing Wang   +3 more
doaj   +1 more source

HNRNPU K181 Lactylation Drives Cervical Cancer Growth by Upregulating PHGDH and Reprogramming Serine Metabolism

open access: yesAdvanced Science, EarlyView.
Lactate in cervical cancer induces HNRNPU K181 lactylation, opposed by NAA50‐mediated acetylation and suppressed by Pazopanib. This lactylation enhances HNRNPU binding to PHGDH pre‐mRNA exon 1, maintaining exon 1‐containing transcripts and mRNA stability, thereby activating serine metabolism.
Chang Zhang   +6 more
wiley   +1 more source

Selenium Nanoparticles Selectively Target KRAS G13D to Inhibit Colorectal Cancer

open access: yesAdvanced Science, EarlyView.
The mechanisms of SeNPs therapy in cancer treatment, encompass three parallel actions: (1) seleno‐amino acids, key metabolites, upregulate GPX2 expression, thereby inhibiting tumor metastasis via the GPX2‐HIF1α‐VEGF signaling pathway; (2) selenite (SeO32−), an inorganic metabolite, forms hydrogen bonds with amino acid residues 13–17 of the KRAS G13D ...
Xiaoting Liu   +13 more
wiley   +1 more source

An efficient proteome-wide strategy for discovery and characterization of cellular nucleotide-protein interactions.

open access: yesPLoS ONE, 2018
Metabolite-protein interactions define the output of metabolic pathways and regulate many cellular processes. Although diseases are often characterized by distortions in metabolic processes, efficient means to discover and study such interactions ...
Yan Ting Lim   +15 more
doaj   +1 more source

Cissus subtetragona Planch. Ameliorates Inflammatory Responses in LPS-induced Macrophages, HCl/EtOH-induced Gastritis, and LPS-induced Lung Injury via Attenuation of Src and TAK1

open access: yesMolecules, 2021
Several Cissus species have been used and reported to possess medicinal benefits. However, the anti-inflammatory mechanisms of Cissus subtetragona have not been described.
Laily Rahmawati   +15 more
doaj   +1 more source

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