The one-bead-one-compound method gives access to millions of compounds that can be screened directly on the bead. Although characterization techniques are increasingly potent and reliable, problems can still be encountered in deciphering the sequence of the active compound because of sensitiveness or manipulation of the bead. ChemMatrix, a totally PEG-based resin, has resolved the synthesis of peptides of outstanding difficulty. Like other PEG-based resins, it permits on-bead screening because of its compatibility in aqueous media and has the further advantage of having a high loading, comparable to polystyrene resins. ChemMatrix beads previously swelled in water can be nicely divided into four parts that can be characterized using different analytical techniques or just stored for safety or for further testing. The four bead parts show high homogeneity and can thus be considered to be replicas.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/cc070012h | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Protein Catalyzed Capture (PCC) Agents for Antigen Targeting.
Methods Mol Biol
January 2022
Institute for Systems Biology, Seattle, WA, USA.
The protein catalyzed capture agent (PCC) method is a powerful combinatorial screening strategy for discovering synthetic macrocyclic peptide ligands, called PCCs, to designated protein epitopes. The foundational concept of the PCC method is the use of in situ click chemistry to survey large combinatorial libraries of peptides for ligands to designated biological targets. State-of-the-art PCC screens integrate synthetic libraries of constrained macrocyclic peptides with epitope-specific targeting strategies to identify high-affinity (<100 nM) binders de novo.
View Article and Find Full Text PDFSelections and screenings of DNA-encoded chemical libraries against enzyme and cellular targets.
Bioorg Med Chem Lett
May 2021
WuXi AppTec, Am Klopferspitz 19a, 82152 Martinsried, Germany.
The use of DNA-encoded libraries (DELs) has increased greatly over the last decade, and today a majority of pharmaceutical companies employ the technology. The technology may be applied to most soluble and purified targets. However, standard DEL technology has limitations; some targets are challenging to purify, and it is not possible to directly screen for cellular or biochemical activity.
View Article and Find Full Text PDFIncorporation of Fluorine into an OBOC Peptide Library by Copper-Free Click Chemistry toward the Discovery of PET Imaging Agents.
ACS Comb Sci
March 2020
Department of Chemistry, University of Western Ontario, 1151 Richmond Street, London, Ontario N6A 5B7, Canada.
A one-bead one-compound (OBOC) library of peptide-based imaging agents was developed where a F-containing moiety was added onto the N-terminus of octamer peptides through copper-free click chemistry prior to screening of the library. This created a library of complete imaging agents that was screened against CXCR4, a receptor of interest for cancer imaging. The screen directly resulted in the discovery of a peptide-based imaging agent with an IC of 138 μM.
View Article and Find Full Text PDFOff-DNA DNA-Encoded Library Affinity Screening.
ACS Comb Sci
January 2020
Roche Pharma Research and Early Development (pRED) , Roche Innovation Center Basel Hoffman-La Roche Ltd, Grenzacherstrasse 124 , CH-4070 Basel , Switzerland.
DNA-encoded library (DEL) technology is emerging as a key element of the small molecule discovery toolbox. Conventional DEL screens (i.e.
View Article and Find Full Text PDFRapid Discovery of Illuminating Peptides for Instant Detection of Opioids in Blood and Body Fluids.
Molecules
May 2019
Department of Biochemistry & Molecular Medicine, University of California Davis, Sacramento, CA 95817, USA.
The United States is currently experiencing an opioid crisis, with more than 47,000 deaths in 2017 due to opioid overdoses. Current approaches for opioid identification and quantification in body fluids include immunoassays and chromatographic methods (e.g.
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!