Yang, Jianhong; Li, Yong; Qiu, Qiang; Wang, Ruihan; Yan, Wei; Yu, Yamei; Niu, Lu; Pei, Heying; Wei, Haoche; Ouyang, Liang; Ye, Haoyu; Xu, Dingguo; Wei, Yuquan; Chen, Qiang; Chen, Lijuan published an article in 2022. The article was titled 《Small Molecules Promote Selective Denaturation and Degradation of Tubulin Heterodimers through a Low-Barrier Hydrogen Bond》, and you may find the article in Journal of Medicinal Chemistry.Recommanded Product: H-Trp-OMe.HCl The information in the text is summarized as follows:
A mechanism to selectively degrade target proteins. 3-(3-Phenoxybenzyl)amino-β-carboline (PAC), a tubulin inhibitor, promotes selective degradation of αβ-tubulin heterodimers was reported. Biochem. studies have revealed that PAC specifically denatures tubulin, making it prone to aggregation that predisposes it to ubiquitinylation and then degradation The degradation is mediated by a single hydrogen bond formed between the pyridine nitrogen of PAC and βGlu198, which is identified as a low-barrier hydrogen bond (LBHB). In contrast, another two tubulin inhibitors that only form normal hydrogen bonds with βGlu198 exhibit no degradation effect. Thus, the LBHB accounts for the degradation Compounds capable of forming an LBHB with βGlu198 and demonstrated that BML284, a Wnt signaling activator, also promotes tubulin heterodimer degradation through the LBHB were screened. This study provided a unique example of LBHB function and identified a novel approach to obtain tubulin degraders. In the experiment, the researchers used many compounds, for example, H-Trp-OMe.HCl(cas: 7524-52-9Recommanded Product: H-Trp-OMe.HCl)
H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Recommanded Product: H-Trp-OMe.HCl
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