Patent classifications
C07K5/117
Growth Hormone Releasing Peptides
Disclosed are peptide and peptidomimetic compounds generally according to formula (I) that are useful as GHRP analogs:
R.sup.1-A.sup.1-A.sup.2-A.sup.3-A.sup.4-A.sup.5-R.sup.2(I)
wherein:
A.sup.1 is Aib, Apc or Inp;
A.sup.2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp;
A.sup.3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1Nal, D-2Nal, D-Ser(Bzl), or D-Trp;
A.sup.4 is 2Fua, Orn, 2Pal, 3Pal, 4Pal, Pff, Phe, Pim, Taz, 2Thi, 3Thi, Thr(Bzl);
A.sup.5 is Apc, Dab, Dap, Lys, Orn, or deleted;
R.sup.1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and
R.sup.2 is OH or NH.sub.2;
and pharmaceutical compositions and methods of use thereof.
MELANOCORTIN 1 RECEPTOR LIGANDS AND METHODS OF USE
The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
Methods and compositions related to inhibition of viral entry
Disclosed are compositions and methods for inhibiting viral entry.
Cyclic compound/peptide comprising an A-beta13-16 peptide and a linker that is covalently coupled to the n-terminus residue and the c-terminus residue of the A-beta13-16 peptide
The disclosure pertains to conformational epitopes in A-beta, antibodies thereto and methods of making and using immunogens and antibodies specific thereto.
Cyclic compound/peptide comprising an A-beta15-18 peptide and a linker that is covalently coupled to the n-terminus residue and the c-terminus residue of the A-BETA15-18 peptide
The disclosure pertains to epitopes identified in A-beta including conformational epitopes, antibodies thereto and methods of making and using immunogens and antibodies specific thereto.
INHIBITORS OF TRANSGLUTAMINASES
The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases.
Water soluble salts of lipidated peptides and methods for preparing and using the same
Provided herein are water soluble salts of Formula I, wherein R.sup.1, A, and M are defined herein. Also provided herein are methods of preparing the salts of Formula I and methods of using the same.
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Peptide analogs of alpha-melanocyte stimulating hormone
Provided herein are stable peptide analogs of the native alpha-melanocyte stimulating hormone (-MSH) having selectivity for the melanocortin 1 receptor (MC1R). Also provided herein are pharmaceutical preparations of the -MSH peptide analogs, as well as methods of using these analogs in the treatment of medical and veterinary conditions involving MC1R.
POLYPEPTIDE COMPOUND AND APPLICATION THEREOF
A polypeptide compound having a structure shown in formula I, or a stereoisomer, mixture or pharmaceutically acceptable salt thereof Experimental results show that the polypeptide compound can effectively exhibit high agonistic activity to GHSR-1a.
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METHODS FOR REDUCING CD36 EXPRESSION
The invention provides a method for treating one or more complications of diabetes in a mammal. The method comprises administering to a mammal in need thereof an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (p.sub.m) and the total number of amino acid residues (r) wherein 3 p.sub.m is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (p.sub.t) wherein 2a is the largest number that is less than or equal to p.sub.t+1, except that when a is 1, p.sub.t may also be 1.