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DNA-encoded chemical libraries

https://www.nature.com/articles/s43586-021-00084-5  Abstract DNA-encoded chemical library (DECL) technology is used by the pharmaceutical industry to discover small molecules capable of modulating biologically relevant targets. DECL synthesis starts with an oligonucleotide that contains a chemical linker moiety, and proceeds through iterative cycles of DNA barcode elongation and chemical synthesis. DECL selections require little protein, minimal assay development …Read More >

Resource Type: Publication
Resource Topic: Discovery Chemistry, DNA-Encoded Library (DEL), DRUG DISCOVERY AND INNOVATION, Hit Finding, Screening Libraries, Small Molecules, Target Identification and Validation

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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase

Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement of a phenyl with a pyridyl moiety in the chemical structure revealed a new binding mode for the inhibitors with subtle conformational change of the …Read More >

Resource Type: Publication
Resource Topic: Chemical Biology and Proteomics, Discovery Chemistry, Hit-to-Lead, Lead Optimization, Oncology, Small Molecules

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Resource Topics
× peptide, amino acid

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