HIV-1 new target small molecule drug candidate found

Prior to the successful development of AIDS vaccines, anti-HIV drugs were the most effective means to prevent AIDS. According to news from the Kunming Institute of Zoology, Chinese Academy of Sciences, the research team has recently found a candidate HIV-1 new target drug candidate. The results have been published in the authoritative publication "Science Report."

The team worked with the team of Academician Sun Handong of the Kunming Institute of Botany, Chinese Academy of Sciences to systematically screen and study the natural small molecule compounds including Schisandra sphenanthera, Schizandra sphenanthera, and Flos sphenulae Schisandra. They discovered the lignin compounds derived from Schizandra schisandrae SM- 10 has good anti-HIV activity. Through in-depth research, they unexpectedly discovered that the activity of synthetic intermediate SJP-L-5 is far superior to that of SM-10.

A few days ago, the research team collaborated with the research team of Xiao Weilie, a key laboratory of the Department of Education for Natural Resources Medicinal Chemistry of the Yunnan University, to conduct an in-depth study of the anti-HIV mechanism of SJP-L-5 and found that SJP-L-5 can effectively inhibit the late course of reverse transcription. They used a high-sensitivity probe for Southern blot hybridization to confirm that SJP-L-5 inhibited the synthesis of positive-stranded viral DNA and disrupted the structure of the viral cPPT flap, leading to the appearance of 5 downstream positive stranded DNA. Fragmented replication products. Since the cPPT flap is a requirement for virus entry into the nucleus, its absence results in the inability of viral DNA to enter the nucleus. Both genotypic resistance and phenotypic resistance experiments showed that there are two genes that are important sites for the binding of SJP-L-5 to reverse enzymes, and that are the structural basis for the new mechanism of this compound. This study confirms for the first time that the cPPT flap is a new anti-HIV virus target, and SJP-L-5 is a new small molecule drug candidate acting on this new target. Research provides anti-HIV drugs for the development of new targets. New ideas. (Reporter Zhao Hanbin)


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