Although a number of genomic and biochemical technologies are now used to elucidate the mechanisms of action of bioactive small molecules, affinity-based isolation of molecular targets is a classic, but still powerful, approach. This review highlights recent cases where biochemical isolation of target proteins of bioactive small molecules highlighted general strategies for a successful isolation and identification of molecular targets. This review is intended to be both an update on the most recent findings for those already active in the field of forward chemical genetics and a guide for scientists entering this burgeoning field.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.chembiol.2010.05.015 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Construction of Nanohydroxyapatite/Poly(sodium lipoate)-Based Bioactive Hydrogels for Cranial Bone Regeneration.
Biomacromolecules
December 2024
School of Chemistry, Xi'an Jiaotong University, Xi'an 710049, China.
Persistent oxidative stress following bone defects significantly impedes the repair of bone tissue. Designing an antioxidative hydrogel with a suitable mechanical strength can help alter the local microenvironment and promote bone defect healing. In this work, α-lipoic acid (LA), a natural antioxidant small molecule, was chemically cross-linked with lipoic acid-functionalized poly(ethylene glycol) (PEG, = 6k or 10k) in sodium bicarbonate solution, to prepare LA-PEG hydrogels (LP, = 6k or 10k).
View Article and Find Full Text PDFA Prodrug Nanodevice Co-delivering Docetaxel and ROR1 siRNA for Enhanced Triple Negative Breast Cancer Therapy.
Acta Biomater
December 2024
Lingang Laboratory, Shanghai 200031, China. Electronic address:
Triple-negative breast cancer (TNBC) has been a clinical challenge due to its high recurrence and metastasis rates. Chemotherapy remains the primary treatment for TNBC after surgery ablation, but it lacks targeted specificity and causes side effects in normal tissues. Receptor tyrosine kinase-like orphan receptor 1 (ROR1) is significantly expressed in TNBC cells, and small interference RNA (siRNA) targeting ROR1 can effectively suppress ROR1 gene expression, thereby inhibiting proliferation and metastasis.
View Article and Find Full Text PDFIn situ production and precise release of bioactive GM-CSF and siRNA by engineered bacteria for macrophage reprogramming in cancer immunotherapy.
Biomaterials
December 2024
School of Life Sciences, Faculty of Medicine, Tianjin Engineering Center of Micro-Nano Biomaterials and Detection-Treatment Technology, Tianjin Key Laboratory of Function and Application of Biological Macromolecular Structures, Tianjin University, Tianjin, 300072, China.
In the immunosuppressive tumor microenvironment (TME), tumor-associated macrophages (TAMs) predominantly exhibit an immunosuppressive M2 phenotype, which facilitates tumor proliferation and metastasis. Although current strategies aimed at reprogramming TAMs hold promise, their sustainability and effectiveness are limited due to repeated injections. Herein, a bacterial therapy platform containing two engineered strains was developed.
View Article and Find Full Text PDFStudy on the antioxidant and antiosteoporotic activities of the oyster peptides prepared by ultrasound-assisted enzymatic hydrolysis.
Ultrason Sonochem
December 2024
Shenzhen Key Laboratory of Food Nutrition and Health, Guangdong Engineering Technology Research Center of Aquatic Food Processing and Safety Control, School of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen 518060, China. Electronic address:
In this study, the effects of ultrasound-assisted enzymatic hydrolysis on the production of antioxidant and antiosteoporotic peptides derived from oysters were investigated. Results showed that ultrasound-assisted enzymatic hydrolysis significantly enhanced the peptide content, free radical scavenging ability, and ferric reducing antioxidant power of total oyster protein hydrolysate (TOPH), with optimal results achieved at 200 W (TOPH-200). Correspondingly, ultrasound treatment at 200 W increased the exposure of hydrophobic regions, reduced α-helix content, and facilitated the generation of small molecular weight peptides in TOPH.
View Article and Find Full Text PDFTarget protein identification in live cells and organisms with a non-diffusive proximity tagging system.
Elife
December 2024
Department of Neurology, Medical Research Institute, Zhongnan Hospital of Wuhan University, Wuhan University, Wuhan, China.
Identifying target proteins for bioactive molecules is essential for understanding their mechanisms, developing improved derivatives, and minimizing off-target effects. Despite advances in target identification (target-ID) technologies, significant challenges remain, impeding drug development. Most target-ID methods use cell lysates, but maintaining an intact cellular context is vital for capturing specific drug-protein interactions, such as those with transient protein complexes and membrane-associated proteins.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!