Industry News

07 August 2023

DEL for DNA- and RNA-Binding Proteins

While DNA-encoded library (DEL) selection has been applied to a variety of targets with multiple candidates progressed into different stages of drug development, the utilization of DEL in DNA- and RNA-binding proteins remains questionable. This is largely due to the fact that each DEL compound contains a long stretch of DNA barcode, which when used to screen against DNA- or RNA- binding proteins (transcription factors, DNA polymerases, helicases, DNases, RNases, chromatin modifying complexes, etc.) , would lead to significant false positives.
04 August 2023

DEL for GPCRs

G protein coupled receptors (GPCRs) are a family of multi-transmembrane proteins with typical 7 transmembrane regions. Many marketed drugs are known to target GPCRs.
31 July 2023

DEL for Protein Degradation

Protein degraders (most popularly known as PROTAC or Molecular Glue) utilize an event-driven process, recruit protein of interest (POI, or targeted protein) and E3 ligase directly or indirectly, induce poly-ubiquitination of POI and subsequent proteasome-mediated degradation. Unlike protein inhibitors, protein degraders do not require inhibitory activity to the protein, therefore, this modality of therapeutics applies to broader target classes including undruggable proteins, scaffold proteins, mutant proteins and etc.
04 December 2021

Richard Lerner Remembrance

It is with great sadness that we hear of the passing of Professor Richard A Lerner. Richard served as the director of the Scripps Research Institute from 1991 until 2012, and in 1992 published the seminal paper in PNAS describing the concept of recording a series of chemical transformations by a DNA “code” with his Scripps colleague and Nobel laureate Dr. Sidney Brenner (1927-2019).
29 December 2020

Exploring Aldol Reactions on DNA and Applications to Produce Diverse Structures: An Example of Expanding Chemical Space of DNA-Encoded Compounds by Diversity-Oriented Synthesis.

Chem. Asian J. 2020, 15, 4033 https://doi.org/10.1002/asia.202001105
03 December 2020

A Method for Estimating Binding Affinity From Primary DEL Selection Data

Biochemical and Biophysical Research Communications Volume 533, Issue 2 DOI: 10.1101/2020.05.04.077842
01 August 2020

A B2(OH)4-Mediated Synthesis of 2-Substituted Indazolone and Its Application in a DNA-Encoded Library

Org. Lett. 2020, 22, 16, 6277–6282 https://doi.org/10.1021/acs.orglett.0c02032
18 June 2020

A Simple Method for Determining Compound Affinity and Chemical Yield From DNA-encoded Library Selections

Biochemical and Biophysical Research Communications Volume 527, Issue 1, 18 June 2020, Pages 250-256 https://doi.org/10.1016/j.bbrc.2020.04.024
27 April 2020

Optimized Methods for IL-17A Refolding and anti-IL17A Fab Production for Co-Crystallization With Small Molecules

BIOTECHNIQUESVOL. 69, NO. 1 https://doi.org/10.2144/btn-2019-0170
10 April 2020

Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library

ACS Med. Chem. Lett. 2020, 11, 6, 1175–1184 https://doi.org/10.1021/acsmedchemlett.0c00029

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