Category: 1525619-20-8

Doelle, Anja et al. published new progress in experiments with the help of cas: 1525619-20-8

Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Electric Literature of C6H7BrN2Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs.

Doelle, Anja;Adhikari, Bikash;Kraemer, Andreas;Weckesser, Janik;Berner, Nicola;Berger, Lena-Marie;Diebold, Mathias;Szewczyk, Magdalena M.;Barsyte-Lovejoy, Dalia;Arrowsmith, Cheryl H.;Gebel, Jakob;Loehr, Frank;Doetsch, Volker;Eilers, Martin;Heinzlmeir, Stephanie;Kuster, Bernhard;Sotriffer, Christoph;Wolf, Elmar;Knapp, Stefan published 《Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders》. The research results were published in《Journal of Medicinal Chemistry》 in 2021.Electric Literature of C6H7BrN2 The article conveys some information:

Histone H3K4 methylation serves as a post-translational hallmark of actively transcribed genes and is introduced by histone methyltransferase (HMT) and its regulatory scaffolding proteins. One of these is the WD-repeat-containing protein 5 (WDR5) that has also been associated with controlling long noncoding RNAs and transcription factors including MYC. The wide influence of dysfunctional HMT complexes and the typically upregulated MYC levels in diverse tumor types suggested WDR5 as an attractive drug target. Indeed, protein-protein interface inhibitors for two protein interaction interfaces on WDR5 have been developed. While such compounds only inhibit a subset of WDR5 interactions, chem. induced proteasomal degradation of WDR5 might represent an elegant way to target all oncogenic functions. This study presents the design, synthesis, and evaluation of two diverse WDR5 degrader series based on two WIN site binding scaffolds and shows that linker nature and length strongly influence degradation efficacy.2-Bromo-5H,6H,7H-pyrrolo[1,2-a]imidazole (cas: 1525619-20-8) were involved in the experimental procedure.

Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Electric Literature of C6H7BrN2Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs.

Reference:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem