Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA‐Encoded Chemical Library
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201600573
Abstract: We have identified and characterized novel potent inhibitors of Bruton's tyrosine kinase (BTK) from a single DNA‐encoded library of over 110 million compounds by using multiple parallel selection conditions, including variation in target concentration and… read more here.
Keywords: potent; novel binding; btk; dna encoded ... See more keywords
Opportunities for Expanding Encoded Chemical Diversification and Improving Hit Enrichment in mRNA‐Displayed Peptide Libraries
Sign Up to like & getrecommendations! Published in 2022 at "Chembiochem"
DOI: 10.1002/cbic.202100685
Abstract: DNA‐encoded small‐molecule libraries and mRNA displayed peptide libraries both use numerically large pools of oligonucleotide‐tagged molecules to identify potential hits for protein targets. They differ dramatically, however, in the ‘drug‐likeness’ of the molecules that each… read more here.
Keywords: encoded small; mrna displayed; displayed peptide; dna encoded ... See more keywords
A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.04.022
Abstract: Natural products have been an invaluable source of drug discovery, but their targets remain largely unknown. Natural products enriched DNA-encoded chemical libraries (nDELs) empower the researchers to rapidly and economically screen numerous natural products against… read more here.
Keywords: poly adp; dna; natural products; dna encoded ... See more keywords
Photoredox cross-electrophile coupling in DNA-encoded chemistry.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.04.028
Abstract: A catalytic manifold that enables photoredox cross-electrophile coupling of alkyl bromides with DNA-tagged aryl iodides in aqueous solution is presented. This metallaphotoredox transformation was aided by the identification of a new pyridyl bis(carboxamidine) ligand, which… read more here.
Keywords: photoredox cross; cross electrophile; dna; chemistry ... See more keywords
Psoralen as an interstrand DNA crosslinker in the selection of DNA-Encoded dynamic chemical library.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.04.033
Abstract: DNA-encoded chemical library (DEL) has emerged as a powerful technology for ligand discovery in biomedical research. Recently, we have developed a DNA-encoded dynamic library (DEDL) approach by incorporating the concept of dynamic combinatorial library (DCL)… read more here.
Keywords: chemical library; interstrand dna; dna; dna encoded ... See more keywords
DNA-Compatible Synthesis of α,β-Epoxyketones for DNA-Encoded Chemical Libraries.
Sign Up to like & getrecommendations! Published in 2021 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.1c00567
Abstract: As a powerful platform in drug discovery, the DNA-encoded chemical library technique enables the generation of numerous chemical members with high structural diversity. Epoxides widely exist in a variety of approved drugs and clinical candidates,… read more here.
Keywords: dna; dna encoded; dna compatible; compatible synthesis ... See more keywords
Selecting a DNA-Encoded Chemical Library against Non-immobilized Proteins Using a "Ligate-Cross-Link-Purify" Strategy.
Sign Up to like & getrecommendations! Published in 2017 at "Bioconjugate chemistry"
DOI: 10.1021/acs.bioconjchem.7b00343
Abstract: DNA-encoded chemical libraries (DELs) have recently emerged and become an important technology platform in biomedical research and drug discovery. DELs containing large numbers of compounds can be prepared and selected against biological targets to discover… read more here.
Keywords: ligate cross; immobilized proteins; dna encoded; proteins using ... See more keywords
DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions.
Sign Up to like & getrecommendations! Published in 2020 at "Chemical reviews"
DOI: 10.1021/acs.chemrev.0c00789
Abstract: Click chemistry, proposed nearly 20 years ago, promised access to novel chemical space by empowering combinatorial library synthesis with a "few good reactions". These click reactions fulfilled key criteria (broad scope, quantitative yield, abundant starting… read more here.
Keywords: drug discovery; chemistry; good reactions; dna encoded ... See more keywords
A Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00688
Abstract: The activity of the secreted phosphodiesterase autotaxin produces the inflammatory signaling molecule LPA and has been associated with a number of human diseases including idiopathic pulmonary fibrosis (IPF). We screened a single DNA-encoded chemical library… read more here.
Keywords: idiopathic pulmonary; autotaxin; chemistry; dna encoded ... See more keywords
Identification and Validation of New Interleukin-2 Ligands Using DNA-Encoded Libraries.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01693
Abstract: Interleukin-2 (IL2) is a pro-inflammatory cytokine that plays a crucial role in immunity, which is increasingly being used for therapeutic applications. There is growing interest in developing IL2-based therapeutics which do not interact with the… read more here.
Keywords: new interleukin; identification validation; chemistry; dna encoded ... See more keywords
Synthetic Studies toward DNA-Encoded Heterocycles Based on the On-DNA Formation of α,β-Unsaturated Ketones.
Sign Up to like & getrecommendations! Published in 2021 at "Organic letters"
DOI: 10.1021/acs.orglett.0c04118
Abstract: Taking advantage of the diversity-oriented synthesis strategy with α,β-unsaturated carbonyl compounds, we have successfully established the DNA-compatible transformations for various heterocyclic scaffolds. The ring-closure reactions for pyrrole, pyrrolidine, pyrazole, pyrazoline, isoxazoline, pyridine, piperidine, cyclohexenone, and… read more here.
Keywords: studies toward; toward dna; encoded heterocycles; dna ... See more keywords