The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1.sub.LAI gp41 protein, and fragments, analogs and homologs of DP178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.

Claims

75 · 3 independent · depth 6

75 granted claims

›1.independentAn isolated peptide consisting of an amino acid sequence of a 16 to 39 amino acid residue region of an HIV-1 or HIV-2 retrovirus protein wherein said …+23

›3.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein group X is a hydrophobic group.d2+1

›5.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein group Z is a hydrophobic group.d2+1

›7.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein group X is a macromolecular carrier group.d2+3

›9.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein the group Z is a macromolecular carrier group.d2+5

›11.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein at least one bond linking adjacent amino acid residues of the peptide is a non-peptide bond.d2+1

›13.↳ 1multiple · 1, 2The peptide of claim 1 or 2 wherein at least one amino acid residue of the peptide is in a D-isomer configuration.d2

›14.↳ 1multiple · 1, 2The peptide of claim 1 or 2, wherein X is an acetyl group, and Z is an amido group.d2

›65.↳ 1The peptide of claim 1, wherein the region of the HIV-1 or HIV-2 retrovirus protein is a region of 28 amino acid residues identified by the ALLMOTI5 m…d2

›66.↳ 1The peptide of claim 1, wherein the region of the HIV-1 or HIV-2 retrovirus protein is a region of 35 amino acid residues identified by the ALLMOTI5 m…d2

›67.↳ 1The peptide of claim 1, wherein the region of the HIV-1 or HIV-2 retrovirus protein is a region of 28 amino acid residues identified by the 107.times.…d2

›68.↳ 1The peptide of claim 1, wherein the region of the HIV-1 or HIV-2 retrovirus protein is a region of 35 amino acid residues identified by the 107.times.…d2

›69.↳ 1The peptide of claim 1, wherein the region of the HIV-1 or HIV-2 retrovirus protein is identified by the PLZIP motif.d2

›2.independentAn isolated peptide having the formula: X-NKSLEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO:210); X-SLEQIWNNMTWMEWDREINNYTSLIH…+49

An isolated peptide having the formula: X-NKSLEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO:210); X-SLEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQ-Z (SEQ. ID. NO. 211); X-LEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQE-Z (SEQ. ID. NO. 212); X-EQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEK-Z (SEQ. ID. NO. 213); X-QIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKN-Z (SEQ. ID. NO. 214); X-IWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNE-Z (SEQ. ID. NO. 215); X-WNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQ-Z (SEQ. ID. NO. 216); X-NNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQE-Z (SEQ. ID. NO. 217); X-NMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQEL-Z (SEQ. ID. NO. 218); X-MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 219); X-TWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLE-Z (SEQ. ID. NO. 220); X-WMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL-Z (SEQ. ID. NO. 221); X-WMEWDREINNYTSLIHSLIEESQNQQEKNEQELLE-Z SEQ. ID. NO. 222); X-WMEWDREINNYTSLIGSLIEESQNQQEKNEQELLE-Z (SEQ. ID. NO. 159); X-MEWDREINNYTSLIHSLIEESQNQQEKNEQELLELD-Z (SEQ. ID. NO. 223); X-EWDREINNYTSLIHSLIEESQNQQEKNEQELLELDK-Z (SEQ. ID. NO. 224); X-WDREINNYTSLIHSLIEESQNQQEKNEQELLELDKW-Z (SEQ. ID. NO. 225); X-DREINNYTSLIHSLIEESQNQQEKNEQELLELDKWA-Z (SEQ. ID. NO. 226); X-REINNYTSLIHSLIEESQNQQEKNEQELLELDKWAS-Z (SEQ. ID. NO. 227); X-EINNYTSLIHSLIEESQNQQEKNEQELLELDKWASL-Z (SEQ. ID. NO. 228); X-INNYTSLIHSLIEESQNQQEKNEQELLELDKWASLW-Z (SEQ. ID. NO. 229); X-NYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 230); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 185); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWFNITNWLWLIKFI-Z (SEQ. ID. NO. 160); X-TSLIHSLIEESQNQQEKNEQELLELDKWASLWNWFN-Z (SEQ. ID. NO. 231); X-SLIHSLIEESQNQQEKNEQELLELDKWASLWNWFNI-Z (SEQ. ID. NO. 232); X-LIHSLIEESQNQQEKNEQELLELDKWASLWNWFNIT-Z (SEQ. ID. NO. 233); X-TSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 234); X-LIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 235); X-ESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 236); X-NQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 237); X-EKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 238); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNAF-Z (SEQ. ID. NO. 178); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLANWF-Z (SEQ. ID. NO. 179); X-YTSLIHSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 180); X-YTSLIHSLIEESQNQQEKNEQELLQLDKWASLWNWF-Z (SEQ. ID. NO. 181); X-YTSLIHSLIEESQNQQEKNQQELLQLDKWASLWNWF-Z (SEQ. ID. NO. 182); X-YTSLIHSLQEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 183); X-YTSLIHSLIEQSQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 186); X-YTSLIHSLIQESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 187); X-YTSLIHSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 190); X-YTSLIQSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 191); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLFNFF-Z (SEQ. ID. NO. 192); X-YTSLIHSLIEESQNLQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 193); X-YTSLIHSLIEESQNQQEKLEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 194); X-YTSLIHSLIEESQNQQEKNEQELLEFDKWASLWNWF-Z (SEQ. ID. NO. 195); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASPWNWF-Z (SEQ. ID. NO. 197); X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNSF-Z (SEQ. ID. NO. 198); or X-LRAIEAQQHLLQLTVWQIKQLQARILAV-Z (SEQ. ID. NO. 239), in which: amino acid residues are presented by the single-letter code; X comprises an amino group, an acetyl group, a 9-fluorenylmethoxy-carbonyl group, a hydrophobic group, or a macromolecular carrier group; and Z comprises a carboxyl group, an amido group, a hydrophobic group, or a macromolecular carrier group.

›15.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-NKSLEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKASLWNWF-Z (SEQ. ID. NO:210).d2

›16.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-SLEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQ-Z (SEQ. ID. NO. 211).d2

›17.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-LEQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQE-Z (SEQ. ID. NO. 212).d2

›18.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-EQIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEK-Z (SEQ. ID. NO. 213).d2

›19.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-QIWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKN-Z (SEQ. ID. NO. 214).d2

›20.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-IWNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNE-Z (SEQ. ID. NO. 215).d2

›21.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-WNNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQ-Z (SEQ. ID. NO. 216).d2

›22.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-NNMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQE-Z (SEQ. ID. NO. 217).d2

›23.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-NMTWMEWDREINNYTSLIHSLIEESQNQQEKNEQEL-Z (SEQ. ID. NO. 218).d2

›24.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 219).d2

›25.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-TWMEWDREINNYTSLIHSLIEESQNQQEKNEQELLE-Z (SEQ. ID. NO. 220).d2

›26.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-WMEWDREINNYTSLIHSLIEESQNQQEKNEQELLEL-Z (SEQ. ID. NO. 221).d2

›27.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-WMEWDREINNYTSLIHSLIEESQNQQEKNEQELLE-Z (SEQ. ID. NO. 222).d2

›28.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-WMEWDREINNYTSLIGSLIEESQNQQEKNEQELLE-Z (SEQ. ID. NO. 159).d2

›29.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-MEWDREINNYTSLIHSLIEESQNQQEKNEQELLELD-Z (SEQ. ID. NO. 223).d2

›30.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-EWDREINNYTSLIHSLIEESQNQQEKNEQELLELDK-Z (SEQ. ID. NO. 224).d2

›31.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-WDREINNYTSLIHSLIEESQNQQEKNEQELLELDKW-Z (SEQ. ID. NO. 225).d2

›32.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-DREINNYTSLIHSLIEESQNQQEKNEQELLELDKWA-Z (SEQ. ID. NO. 226).d2

›33.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-REINNYTSLIHSLIEESQNQQEKNEQELLELDKWAS-Z (SEQ. ID. NO. 227).d2

›34.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-EINNYTSLIHSLIEESQNQQEKNEQELLELDKWASL-Z (SEQ. ID. NO. 228).d2

›35.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-INNYTSLIHSLIEESQNQQEKNEQELLELDKWASLW-Z (SEQ. ID. NO. 229).d2

›36.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-NYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 230).d2

›37.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNW-Z (SEQ. ID. NO. 185).d2

›38.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWFNITNWLWLIKFI-Z (SEQ. ID. NO. 160).d2

›39.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-TSLIHSLIEESQNQQEKNEQELLELDKWASLWNWFN-Z (SEQ. ID. NO. 231).d2

›40.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-SLIHSLIEESQNQQEKNEQELLELDKWASLWNWFNI-Z (SEQ. ID. NO. 232).d2

›41.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-LIHSLIEESQNQQEKNEQELLELDKWASLWNWFNIT-Z (SEQ. ID. NO. 233).d2

›42.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-TSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 234).d2

›43.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-LIHSLIEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 235).d2

›44.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-ESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 236).d2

›45.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-NQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 237).d2

›46.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-EKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 238).d2

›47.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNAF-Z (SEQ. ID. NO. 178).d2

›48.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLANWF-Z (SEQ. ID. NO. 179).d2

›49.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 180).d2

›50.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLQLDKWASLWNWF-Z (SEQ. ID. NO. 181).d2

›51.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNQQELLQLDKWASLWNWF-Z (SEQ. ID. NO. 182).d2

›52.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLQEESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 183).d2

›53.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEQSQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 186).d2

›54.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIQESQNQQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 187).d2

›55.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 190).d2

›56.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIQSLIEESQNQQEKNEQQLLELDKWASLWNWF-Z (SEQ. ID. NO. 191).d2

›57.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLFNFF-Z (SEQ. ID. NO. 192).d2

›58.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNLQEKNEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 193).d2

›59.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKLEQELLELDKWASLWNWF-Z (SEQ. ID. NO. 194).d2

›60.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLEFDKWASLWNWF-Z (SEQ. ID. NO. 195).d2

›61.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASPWNWF-Z (SEQ. ID. NO. 197).d2

›62.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNSF-Z (SEQ. ID. NO. 198).d2

›63.↳ 2The peptide of claim 2, wherein the peptide has the formula: X-LRAIEAQQHLLQLTVWQIKQLQARILAV-Z (SEQ. ID. NO. 239).d2

›64.independentmultiple · 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63The peptide of any one of claims 15 through 63, wherein X is an acetyl group, and Z is an amido group.

Classifications

6 codes

USPC · US Patent Classification

530/300424/188.1530/326530/325530/350530/324

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