In 2002, the National Cancer Institute created the Initiative for Chemical Genetics (ICG), to enable public research using small molecules to accelerate the discovery of cancer-relevant small-molecule probes. The ICG is a public-access research facility consisting of a tightly integrated team of synthetic and analytical chemists, assay developers, high-throughput screening and automation engineers, computational scientists, and software developers. The ICG seeks to facilitate the cross-fertilization of synthetic chemistry and cancer biology by creating a research environment in which new scientific collaborations are possible. To date, the ICG has interacted with 76 biology laboratories from 39 institutions and more than a dozen organic synthetic chemistry laboratories around the country and in Canada. All chemistry and screening data are deposited into the ChemBank web site (http://chembank.broad.harvard.edu/) and are available to the entire research community within a year of generation. ChemBank is both a data repository and a data analysis environment, facilitating the exploration of chemical and biological information across many different assays and small molecules. This report outlines how the ICG functions, how researchers can take advantage of its screening, chemistry and informatic capabilities, and provides a brief summary of some of the many important research findings.
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http://dx.doi.org/10.1158/0008-5472.CAN-06-2552 | DOI Listing |
Biochim Biophys Acta Rev Cancer
January 2025
Kunming University of Science and Technology, Medical School, Kunming 650500, China.
SUMOylation is a protein modification process that involves the covalent attachment of a small ubiquitin-like modifier (SUMO) to a specific lysine residue on the target protein. This modification can influence the function, localization, stability, and interactions of proteins, thereby regulating various cellular processes. Altering the SUMOylation of certain proteins is expected to be a potential approach for treating specific cancers and diseases.
View Article and Find Full Text PDFComput Biol Med
January 2025
Drug Design and Discovery Lab, Helmy Institute of Medical Sciences, Zewail City of Science, Technology and Innovation, Giza, 12578, Egypt; Biomedical Sciences Program, University of Science and Technology, Zewail City of Science, Technology and Innovation, Giza, 12578, Egypt. Electronic address:
Epidermal growth factor receptor (EGFR) is amongst the earliest targeted kinases by small-molecule inhibitors for the management of EGFR-positive cancer types. While a few inhibitors are granted FDA approval for clinical use, discovery of new inhibitors is still of merit to enhance ligand-binding stability and subsequent enzyme inhibition. Thus, a structure-based design approach was adopted to devise a new series of twenty-nine N3-substituted quinazolin-4-ones as type I ATP-competitive inhibitors targeting the deep hydrophobic pocket of EGFR.
View Article and Find Full Text PDFTalanta
January 2025
Ministry of Education Key Laboratory of Analytical Science for Food Safety and Biology, Fujian Provincial Key Laboratory of Analysis and Detection Technology for Food Safety, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350108, China. Electronic address:
Matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) has become a robust tool for analyzing a variety of biomacromolecules. However, the strong background interference produced by conventional organic matrices hinders the detection of small molecule analytes, which restricts the widespread application of MALDI-MS in metabolomics studies. Consequently, developing new organic matrices is urgently needed to overcome these issues.
View Article and Find Full Text PDFJ Colloid Interface Sci
January 2025
Chemical Engineering College, Inner Mongolia University of Technology, Aimin street 49 Xincheng District, Hohhot 010051 PR China; Inner Mongolia Engineering Research Center for CO2 Capture and Utilization, Aimin street 49, Xincheng District, Hohhot 010051 PR China; Key Laboratory of CO2 Resource Utilization at Universities of Inner Mongolia Autonomous Region, Aimin street 49 Xincheng District, Hohhot 010051 PR China. Electronic address:
Ligand engineering has proven to be an effective strategy for tuning and controlling the microenvironment of coordinated metal centers, highlighting the critical bridge between the activity and structural features of catalysts during electrocatalytic CO reduction reactions (eCORR). However, the limited availability of diverse organic ligands has hindered the development of novel high-performing electrocatalysts. In contrast, small organic molecules have been widely used in the fabrication of metal complexes due to their well-defined functionalities, low cost, and easy accessibility.
View Article and Find Full Text PDFBiosens Bioelectron
December 2024
National Research Council (CNR), Institute of Applied Sciences and Intelligent Systems, I-80131, Naples, Italy. Electronic address:
Spectrochemical analysis of trace elements in complex matrices is crucial across various fields of science, industry, and technology. However, this analysis is often hindered by background interference and the challenge of detecting ultralow analyte concentrations. Surface Enhanced Infrared Absorption (SEIRA) spectroscopy is emerging as a viable technique to address these challenges as it can successfully reveal soluble and unmodified analytes in a label-free manner through their interactions with a bioreceptor following site-specific labeling with small infrared-active probes.
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