DRAVP ID  DRAVPe00079

Peptide Name   Vpr-1 R8

Sequence  LQQLLFRRRRRRRR

Sequence Length  14

UniProt ID  No entry found

Source  Synthetic construct(derived from HIV-1 gene products(Vpr))

Target Organism  HIV

Assay  Luciferase assay

Activity 

• [Ref.20586421]HIV-1:Inhibition of 3′-end processing catalyzed by integrase(IC50=6.1±1.1 µM);inhibition of strand transfer catalyzed by integrase(IC50>11 µM).

Hemolytic Activity  No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity 

• No cytotoxicity information or data found in the reference(s) presented in this entry

Binding Target  Integrase

Mechanism  IN is an essential enzyme for the stable infection of host cells because it catalyzes the insertion of viral DNA inside the pre-integration complex (PIC) into the genome of host cells in two successive reactions, designated as strand transfer and 3′-end-processing. The peptide could inhibit the activity of integrase and thus inhibit virus replication.

PDB ID  None

Predicted Structure Download  DRAVPe00079

Linear/Cyclic  Linear

N-terminal Modification  Acetylation

C-terminal Modification  Amidation

Other Modification  None

Stereochemistry  L

Literature 1

Title   Peptide HIV-1 integrase inhibitors from HIV-1 gene products.

Pubmed ID   20586421

Reference   J Med Chem. 2010 Jul 22;53(14):5356-60.

Author   Suzuki S, Urano E, Hashimoto C, Tsutsumi H, Nakahara T, Tanaka T, Nakanishi Y, Maddali K, Han Y, Hamatake M, Miyauchi K, Pommier Y, Beutler JA, Sugiura W, Fuji H, Hoshino T, Itotani K, Nomura W, Narumi T, Yamamoto N, Komano JA, Tamamura H. 

DOI   10.1021/jm1003528