融合抑制剂 （fusion inhibitor），又称为 进入抑制剂 （entry inhibitor），是一种 抗艾滋病 靶向药物，能夠防止 艾滋病病毒 （HIV）与 质膜 融合從而阻断HIV 感染 CD4+ T细胞。 融合抑制剂不仅能避免HIV感染人体、防止患上 获得性免疫缺陷综合症 （AIDS，即艾滋病），还能使HIV携带者或艾滋病患者体内的HIV生命周期在这一步阻断，控制病情 [1][2]。 截至2019年， 美国食品药品监督管理局 （FDA）一共批准三种融合抑制剂类药物上市： 恩夫韦地 （enfuvirtide，商品 …

By specific delivery of C37 to its target and possibly increasing the local concentration of C37 on the cell surface, the chimeric inhibitors block HIV more efficiently than C37 alone. We report here the success of a strategy to covalently link potent CCR5-binding proteins with …

As a test of this hypothesis, the potent HIV entry inhibitor griffithsin was covalently linked via a 16-amino-acid peptide linker with the gp41-binding peptide C37 to form “Griff37.” Cell-cell fusion assays represent a common method of determining the antiviral potencies of many compounds.

2022年10月31日 · The resulting CCL5 5p12 5m-C37 fusion protein was expressed in E. coli and proved to be capable of inhibiting R5 HIV-1 strains with low to sub-picomolar IC 50, maintaining its antagonism toward CCR5. In addition, CCL5 5p12 5m-C37 inhibits R5/X4 and X4 HIV-1 strains in the picomolar concentration range.

2001年1月5日 · The identity of C37-H6 was confirmed by mass spectrometry [MALDI-TOF (matrix-assisted laser desorption/ionization–time-of-flight), PerSeptive]. Like C34, C37-H6 is a potent inhibitor of HIV-1 membrane fusion, with an IC 50 ≈ 1 nM in the cell-cell fusion assay (M. J. Root, P. S. Kim, unpublished results).

2009年11月26日 · Our model predicts that C37 inhibition of HIV-1 entry is reversible if the peptide dissociates before gp41 deactivates. To test this prediction, we developed an inhibitor-washout viral infectivity assay.

The C37 binding site is targeted by both C37-KYI and di-C37, while the 5-Helix binding site is targeted by both 5H WT and 5H LAVA. In mediating HIV-1 entry, Env undergoes a series of coordinated structural transformations initiated when gp120 binds cellular CD4 [13–15].

four potent protein HIV inhibitors, 5P12-RANTES, 5P12-RANTES-L-C37, Grft, and Grft-L-C37 can be formulated into silk fibroin (SF) disks and remain functional for 14 months at 25, 37, and 50 °C. These HIV inhibitor-encapsulated SF disks show excellent inhibition properties in PBMC and in human colorectal and cervical tissue explants, and do ...

Employing a series of C37 and 5-Helix variants, we investigated the physical properties of gp41 inhibition, including the ability of inhibitor-bound gp41 to recover its fusion activity once inhibitor was removed from solution. Our results indicated that antiviral activity critically depended upon irreversible deactivation of inhibitor-bound gp41.

Employing a series of C37 and 5-Helix variants, we investigated the physical properties of gp41 inhibition, including the ability of inhibitor-bound gp41 to recover its fusion activity once inhibitor was removed from solution. Our results indicated that antiviral activity critically depended upon irreversible deactivation of inhibitor-bound gp41.