Table 2.
Peptide-based fusion inhibitors targeting gp41 and gp120.
Peptide Name | Sequence | Derived from | Target | IC50 (nM) | Assay Format Tested | Phase | Reference |
---|---|---|---|---|---|---|---|
pV2α-Tys | KVQKEY(SO3H)ALFY(SO3H)-ELDIVPID | CCR5 N-terminus | Gp120 variable loops | 50,000 | CCR5-binding assay | Pre-clinical | [40] |
pCCR5-Tys | MDYQVSSPIY(SO3H)DIANY(SO3H)YTSEPSQK | CCR5 N-terminus | Gp120 variable loops | 50,000 | CCR5-binding assay | Pre-clinical | [40] |
E1P47 | WILEYLWKVPFDFWRGVI | GB virus C E1 protein | gp41 FP | 8200 | Competitive ELISA, fluorescence resonance energy transfer, haemolysis assays | Pre-clinical | [72] |
SC29EK | WEEWDKKIEEYTKKIEELIKKSEEQQKKN | gp41 | Gp41 NHR | 9.6 | multinuclear activation of galactosidase indicator (MAGI) assays | Pre-clinical | [147] |
FB006M | Ac-WEEWDREINNYTK (MPA)LIHELIEESQNQQEKNEQELL-CONH2 | Gp41 CHR | Gp41 NHR | 2.7 | peripheral blood mononuclear cell (PBMC) assay, ELISA | Approved | [222] |
CP32M | VEWNEMTWMEWEREIENYTKLIYKILEESQEQ | gp41 CHR | Gp41 NHR | 65 | Native Polyacrylamide Gel Electrophoresis (N-PAGE) Assay, Cell–Cell Fusion Assay | Pre-clinical | [85] |
HP23 | EMTWEEWEKK IEEYTKKIEEILK | Gp41 CHR | Gp41 NHR | 4.7 | Cell-cell fusion assay, Pierce firefly luciferase glow assay | Pre-clinical | [223] |
AP3 | KKISEEQKKIQEEIKKILEESKKILEEIKKDWEEWTM | artificial peptide | Gp41 NHR | 13∼90 | ELISA | Pre-clinical | [234] |
N36Fd | SGIVQQQNNLLRAIEAQQHLLQLTVWGIKQLQARILGYIPEAPRDGQAYVRKDGEWVLLSTFL | Gp41 NHR | Gp41 CHR | 99 | Cell-Cell Fusion, ELISA, luciferase assay | Pre-clinical | [100] |
N28Fd | IEAQQHLLQLTVEGIKQLQARILAVERYGYIPEAPRDGQAYVRKDGEWVLISTFL | Gp41 NHR | Gp41 CHR | 39 | Cell-Cell Fusion, ELISA, luciferase assay | Pre-clinical | [100] |