A naturally occurring homoisoflavonoid, cremastranone (1) inhibited angiogenesis in vitro and in vivo. We developed an analogue SH-11037 (2) which is more potent than cremastranone in human retinal microvascular endothelial cells (HRECs) and blocks neovascularization in animal models. Despite their efficacy, the mechanism of these compounds is not yet fully known. In the course of building on a strong foundation of SAR and creating a novel chemical tool for target identification of homoisoflavonoid-binding proteins, various types of photoaffinity probes were designed and synthesized in which benzophenone and biotin were attached to homoisoflavanonoids using PEG linkers on either the C-3' or C-7 position. Notably, the photoaffinity probes linking on the phenol group of the C-3' position retain excellent activity of inhibiting retinal endothelial cell proliferation with up to 72nM of GI50.
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http://dx.doi.org/10.1016/j.bmcl.2016.07.043 | DOI Listing |
J Agric Food Chem
December 2024
School of Biotechnology and Food Engineering, Changshu Institute of Technology, Suzhou 215500, China.
Chlorogenic acid (CA) is an abundant plant secondary metabolite with promising allelopathic effects on weed growth. However, the molecular targets and mechanism of action of CA in plants remain elusive. Here, we report the employment of a clickable photoaffinity probe in identifying the protein targets of CA in seedling proteomes.
View Article and Find Full Text PDFChembiochem
December 2024
CNR: Consiglio Nazionale delle Ricerche, Istituto di Scienze e Tecnologie Chimiche (SCITEC) 'Giulio Natta', ITALY.
Human antigen R (HuR) is an RNA binding protein (RBP) belonging to the ELAV (Embryonic Lethal Abnormal Vision) family, which stabilizes mRNAs and regulates the expression of multiple genes. Its altered expression or localization is related to pathological features such as cancer or inflammation. Dihydrotanshinone I (DHTS I) is a naturally occurring, tetracyclic ortho-quinone inhibitor of the HuR-mRNA interaction.
View Article and Find Full Text PDFFitoterapia
January 2025
State Key Laboratory of Southwest Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, Sichuan, PR China. Electronic address:
Diabetes mellitus is a global chronic metabolic disease and the prevalence of diabetes mellitus is increasing dramatically every year. Berberine (BBR) from Coptidis Rhizoma has potent hypoglycemic effects, however, the specific proteins targeted by berberine that contribute to its hypoglycemic action remain to be elucidated. In this work, TIGAR (TP53-induced glycolysis and apoptosis regulator) was identified as a direct target protein for berberine using activity-based protein profiling (ABPP) and other chemical proteomics techniques with active photoaffinity probes as chemical tools.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
December 2024
The Province and Ministry Co-sponsored Collaborative Innovation Center for Medical Epigenetics, Key Laboratory of Immune Microenvironment and Disease (Ministry of Education), Tianjin Key Laboratory of Medical Epigenetics, Department of Biochemistry and Molecular Biology, Tianjin Medical University, Tianjin 300070, China.
Chem Commun (Camb)
December 2024
Department of Pharmaceutics, College of Pharmacy, Nanchang University, Nanchang 330006, Jiangxi, China.
Piperine (PIP) has attracted extensive attention due to its diverse biological activities. In this study, we developed two photoaffinity probes PIP-1 and PIP-2, which are biologically safe and retain PIP's bioactivity, to investigate its protein targets . Using labeling and cell imaging, we were able to effectively detect and visualize the drug targets of PIP with our probes.
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