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Novel application of National Cancer Institute (NCI) compounds in inhibition of activity of HIV type 1 protease

A technology of compound and protease, which is applied in the field of compounds in the American Cancer Database, can solve problems such as no data showing inhibitory effect

Inactive Publication Date: 2014-09-10
NANKAI UNIV +1
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  • Application Information

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Problems solved by technology

[0008] The compound NSC121217 (methyl n-[(benzyloxy)carbonyl]serylleucyltyrosinate) is from the National Cancer Institute. This compound is currently used to screen for anti-tumor activity in vivo, but there is no data showing that the compound has an inhibitory effect on certain types of tumors

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  • Novel application of National Cancer Institute (NCI) compounds in inhibition of activity of HIV type 1 protease
  • Novel application of National Cancer Institute (NCI) compounds in inhibition of activity of HIV type 1 protease
  • Novel application of National Cancer Institute (NCI) compounds in inhibition of activity of HIV type 1 protease

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Embodiment Construction

[0024] In order to understand the present invention, the present invention is further illustrated below with examples, but it is not intended to limit the protection scope of the present invention.

[0025]In this study, using the principle of fluorescence resonance energy transfer (FRET), two fluorescent probe donors and acceptors were coupled to both ends of the HIV-1 protease substrate as FRET pairs, that is, the energy of the excited state was transferred by Donors at shorter wavelengths to acceptors covering the donor wavelengths such that the emitted photons of the donors for distance-dependent reactions are quenched. Under the action of HIV-1 protease, the substrate is cut off at the tyrosine (Tyr) and proline (Pro) residues, and the quenching group is separated from the fluorescent light-emitting group, releasing a strong fluorescent donor. Under the fluorescence microplate reader (excitation wavelength 490nm, emission wavelength 530nm), to quantitatively detect the ac...

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Abstract

The invention relates to novel application of NCI compounds, specifically to novel application of the NCI compounds with accession numbers of NSC111887 and NSC121217 in inhibition of the activity of HIV type 1 protease. According to the invention, through integration of conventional anti-HIV-1 protease drug and inhibitor data, computational simulation and an in-vitro compound screening method, molecules of the compounds with the accession numbers of NSC111887 and NSC121217 are found out for the first time, and the compound molecules have the structural characteristics of tripeptide derivatives, certain inhibition capability on the activity of HIV-1 protease and 50% inhibiting concentrations of 62 mu M and 162 mu M, respectively.

Description

technical field [0001] The invention relates to a new application of a compound of the National Cancer Institute (NCI) in anti-HIV-1 protease (HIV-1 Protease) activity. Background technique [0002] AIDS is a great threat to human health. There are currently more than 2 million young people aged 10 and 19 living with HIV worldwide. Due to the lack of effective and acceptable support services, young people report AIDS-related illnesses. The number of deaths has increased by 50%, and HIV has high variability, and its drug resistance and drug side effects are becoming more and more serious. Anti-AIDS research is of great significance in today's life science field. [0003] Human immunodeficiency virus type 1 (HIV-1) protease is one of the key enzymes in the process of HIV-1 genome replication, so it has become an important target in the research of anti-HIV-1 drugs. HIV-1 protease acts on the gag and gag-pol sites of the immature polyprotein to process the polyprotein into mat...

Claims

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Application Information

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IPC IPC(8): C07K5/08
Inventor 林建平黄伟强洪章勇李冬梅魏宇陈泽铭李金龙
Owner NANKAI UNIV
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