Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyl transferase was written by Wang, You;Xu, Feng;Nichols, Connie B.;Shi, Yuqian;Hellinga, Homme W.;Alspaugh, J. Andrew;Distefano, Mark D.;Beese, Lorena S.. And the article was included in Journal of Medicinal Chemistry in 2022.Related Products of 76-83-5 This article mentions the following:
Compounds that prevent farnesylation of Cryptoccoccus neoformans Ras protein by inhibiting protein farnesyl transferase with 3-4 nanomolar affinities was developed . Farnesylation directs Ras to the cell membrane and was required for infectivity of this lethal pathogenic fungus. Our high-affinity compounds inhibit fungal growth with 3-6 micromolar min. inhibitory concentrations (MICs), 4- to 8-fold better than Fluconazole, an antifungal commonly used in the clinic. Compounds bound with distinct inhibition mechanisms at two alternative, partially overlapping binding sites, accessed via different inhibitor conformations. Antifungal potency depends critically on the selected inhibition mechanism because this determines the efficacy of an inhibitor at low in vivo levels of enzyme and farnesyl substrate was showed. How chem. modifications of the antifungals encode desired inhibitor conformation and concomitant inhibitory mechanism was elucidated. In the experiment, the researchers used many compounds, for example, (Chloromethanetriyl)tribenzene (cas: 76-83-5Related Products of 76-83-5).
(Chloromethanetriyl)tribenzene (cas: 76-83-5) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Related Products of 76-83-5
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics