De novo designed membrane-traversing and orally bioavailable macrocycles
AssigneeUniversity of Washington
InventorsDavid BAKER, Gaurav BHARDWAJ, Jacob O'CONNOR, Sephen RETTIE, Lance Joseph STEWART, Gizem GOKCE, Jonathan PALMER, Vikram MULLIGAN
Life of this patent
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Abstract
Cyclic peptides are disclosed that comprise an amino acid sequence having no more than 3 amino acid substitutions compared to the amino acid sequence selected from the group consisting of SEQ ID NO: 1-123 and 125-131 or mirror images thereof.
Claims34
A cyclic peptide comprising or consisting of an amino acid sequence having no more than 3 amino acid substitutions compared to the amino acid sequence selected from the group consisting of SEQ ID NO:
- 1-123 and 125-131 or mirror images thereof, wherein residues in uppercase are L amino acids, and residues in lower case are D amino acids, wherein an asterisk identifies the amino acid residue following the asterisk as being an N-methylated amino acid.
- SEQ ID NO
- 6-mers
- 1
- iPfiPf
- 2
- pfaPPl
- 3
- p*faPPl
- 4
- PPVfPf
- 5
- PP*VfPf
- 6
- *faP*vFP
- 7
- vf*LpFP
- 8
- *Vf*LpFP
- 9
- iP*fiP*f
- 10
- faPvFP
- 7-mers
- 11
- P*lvLPpI
- 12
- lp*LIP*lL
- 13
- LP*llPpl
- 14
- lp*ALpPL
- 15
- VIpFIpa
- 16
- Pplf*Lvf
- 17
- VIp*FIpa
- 8-mers
- 18
- lLplLaPL
- 19
- lvP*lliP*l
- 20
- FLPplVpl
- 21
- LPpLv*a*al
- 22
- P*lliP*liv
- 23
- pp*AfA*L*ll
- 24
- lVpPlVpP
- 25
- Plf*FP*llp
- 26
- Plf*FP*ll*G
- 27
- plVpp*LvI
- 28
- P*llFpp*aI
- 29
- v*l*A*avPpI
- 30
- PpA*L*lIvP
- 31
- pp*LlpP*ll
- 129
- pP*llpP*ll
- 32
- PBliPBli
- 33
- ia*A*lPv*lP
- 34
- f*a*Lpllpv
- 35
- Pa*l*f*Lvap
- 36
- V*LpLV*LpL
- 37
- APpVA*L*lV
- 38
- lV*l*llVpP
- 39
- lp*la*lplA
- 40
- Fpp*LIPpl
- 41
- MpPll*avP
- 42
- ap*LLP*lv*a
- 43
- ap*lvap*lv
- 44
- fiPpivP*f
- 47
- FpPL*l*I*IL
- 56
- pP*lIpP*Il
- 9 mers
- 45
- pPBLBVP*lI
- 46
- Lip*LlP*fVl
- 48
- Pv*avPlv*Lf
- 49
- Pav*L*FIAPl
- 50
- *LvL*L*fvpvp
- 51
- PlLLP*a*aIp
- 52
- pA*F*la*lv*VP
- 53
- A*l*lPlpp*lf
- 54
- P*aV*l*llL*aP
- 55
- v*A*A*l*lfppP
- 57
- Vf*a*L*lIpPa
- 58
- piIF*FPp*LI
- 59
- PlI*avpPlP
- 60
- PpPaI*l*lfa
- 61
- P*aaV*lllpL
- 62
- APpVMPv*l*a
- 63
- p*aV*l*apPLP
- 64
- i*aiPAvpPl
- 65
- piPP*lvI*la
- 66
- lLp*LlP*aMa
- 67
- vpPa*l*laVp
- 68
- plAP*aLi*lV
- 69
- lVI*I*FVPGP
- 70
- pAllp*FLvP
- 71
- pPGIlVP*aI
- 72
- pMlP*lLF*lV
- 73
- PpAP*laFif
- 74
- pIl*lp*FvVP
- 92
- vV*LPVL*Lpl
- 94
- Pv*L*f*fp*LiA
- 130
- pv*M*alpPLP
- 10-mers
- 75
- Ip*zFap*Lv*lPv
- 76
- PpAv*LA*lp*VV
- 77
- lL*LLP*LA*AlP
- 78
- *L*FLp*LiPpAv
- 79
- aLVp*LVP*lV*I
- 80
- P*lAP*lfLV*L*L
- 81
- fA*l*A*LPpViP
- 82
- Pi*A*LLPpA*Lf
- 83
- l*ApppPv*L*lA
- 84
- FpPvV*l*a*Vpa
- 85
- P*lFiPLlp*av
- 86
- F*alIPpVP*al
- 87
- P*af*LlpPa*LV
- 88
- fip*A*lLLpPl
- 89
- l*aLfipaPpL
- 90
- M*a*L*alpapPL
- 91
- vlpvpPp*Lf*L
- 92
- *G*FLp*LiPpAv
- 93
- vafI*l*aPpPM
- 94
- *L*fLp*LiPpAv
- 95
- aP*fpFpPALL
- 96
- aGpf*F*FfafP
- 97
- PvpVVPvpFF
- 98
- Llp*ApP*lA*lV
- 99
- P*a*lAlPpi*li
- 100
- p*lvIp*ApL*ll
- 101
- apPvl*l*lAlP
- 102
- PviP*a*Lplli
- 103
- aPVP*faAV*fL
- 104
- LVf*Ip*FlPLp
- 105
- *L*GP*la*LP*ILF
- 106
- *f*LPAV*I*FI*A*A
- 107
- lILp*FVP*GF*L
- 108
- LfPla*LL*AfP
- 11-mers
- 109
- VPpL*iip*LIip
- 110
- VPpL*iip*FIip
- 111
- AP*lVliP*l*Ap*L
- 112
- V*L*lAipPf*a*lP
- 113
- V*l*LplapPAfl
- 114
- pI*AipPlI*Av*L
- 115
- Ppp*lf*L*lIAPv
- 116
- PpVv*llpPI*AI
- 118
- Lpp*LL*alp*la*l
- 119
- Lf*L*app*lvPpa
- 120
- P*aLPp*a*lF*lVI
- 121
- PI*V*apPlV*lfp
- 122
- vp*vl*IIP*liIP
- 123
- ipLlp*LfL*aiP
- 125
- lp*fapPpaall
- 126
- ipLlp*LfL*giP
- 12-mers
- 127
- p*FIpLlLpPa*aI
- 128
- p*VIpLfLpPa*lI
- 131
- VP*liPVAP*VlP*a
- 117
- VP*liPVAP*vlP*a
A cyclic peptide comprising or consisting of a bin string as listed in Table 3, wherein, wherein:
- A is a right-handed helical region;
- B is a right-handed strand region;
- X is a mirror image of A;
- Y is a mirror image of B;
- O are amino acids with phi <0 and cis peptide bond between the residue i and i+1;
- and
- Z are amino acids with phi >0 and cis peptide bond between the residue i and i+1.
Use of the cyclic peptide, conjugate, or cyclic peptide library of any preceding claim to, for example, to carry a linked moiety across a cell membrane, or as a scaffold for target-based drug design, or to screen molecules of interest for binding to one or more of the cyclic peptides.
Dependencies are inferred from the claim text.