Abstract: Disclosed are methods and compositions for the diagnosis and treatment of diseases associated with aberrant expression of a somatostatin receptor (e.g., cancer) or with increased production of a factor regulatable by somatostatin (e.g., acromegaly). The compounds of the invention are of the general formulae: ##STR1## wherein P is a somatostatin peptide analog which binds to a somatostatin receptor,Y is D-tyrosine, L-tyrosine, or desamino-tyrosine,n is an integer from 1 to 32, inclusive,each q, independently, is an integer from 1 to 32, inclusive, and each s, independently, is an integer from 1 to 32, inclusive, where q and s can be the same or different, andX is of the formulaD--NH.sub.2 --CH(CH.sub.2).sub.m NH.sub.2 --CO.sub.2 H orL--NH.sub.2 --CH(CH.sub.2).sub.m NH.sub.2 --CO.sub.2 H,wherein m is an integer from 1 to 10, inclusive.

Abstract: A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp;A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH;A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6);A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;A.sup.8 is Nal or Trp;m is 1, 2, or 3;n is 1, 2, 3, 4 or 5;each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H;R.sub.4 is C.sub.6 H.sub.4 or absent;R.sub.7 is .dbd.NR.sub.

Abstract: The present invention relates to methods of inhibiting HIV-mediated cell killing which comprises inhibiting the interaction between the CS3 region and viral gp41 and its receptor on the surface of lymphocytes. The invention provides for methods which employ peptides, peptide derivatives, or antibodies to inhibit the CS3/CS3 receptor interaction. In addition, the invention also relates to the CS3 receptor.The present invention is based in part on the discovery that a CS3 specific cellular receptor is widely distributed on human lymphocytes and forms a 108 kd complex with CS3-HSA peptide conjugate. It was further discovered that CS3 peptide effectively blocks HIV mediated cell infection and killing. Therefore, the present invention provides for methods of treatment and prophylaxis of HIV infection as well as a means for better understanding the physiology of acquired immunodeficiency syndrome (AIDS).

Abstract: A compound of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H;each X.sub.1 and X.sub.2, independently, is H, F, Cl, Br, OH, CH.sub.3, or CF.sub.3, provided that at least one of X.sub.1 and X.sub.2 must be H;A.sub.3 is Phe or Tyr; andA.sub.4 is OH, NH.sub.2, or NH-R.sub.3 (wherein R.sub.3 is a saturated aliphatic C.sub.1-8 alkyl);or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.

Abstract: Biologically active peptides are disclosed of the formula: A.sup.1 --A.sup.2 --A.sup.3 --A.sup.4 --Phe--Arg--TrP--A.sup.5, or a pharmaceutically acceptable salt thereof; A.sup.1 is H or acetyl; A.sup.2 is Ala, or D--Ala; A.sup.3 is Glu or Gln; and A.sup.4 is His or Tyr; A.sup.5 is NH.sub.2, Gly--NH.sub.2, or D--Ala--NH.sub.2. Pharmaceutical compositions containing these peptides are capable of promoting nerve regeneration and increasing muscle mass or preventing muscle atrophy following an injury.

Abstract: A method of selectively inhibiting biochemical activity of cells induced by neuromedin B. The method includes the step of contacting cells which contain neuromedin B receptor with a cyclic octapeptide, D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH.sub.2, or an analog thereof.

Abstract: The present invention relates to novel growth hormone-releasing peptides and method for increasing the release of growth hormone levels in mammals, as well as method for increasing milk production in dairy cows and increasing growth rates of animals, such as cattle, sheep, swine, and others. The novel peptides of this invention surprisingly are effective for releasing growth hormone levels in animals by replacing the natural amino acids in positions 1, 2, 3, 8, 9, 10, 12, 21 and 27, as well as derivatizing the N-terminal amino acid residue in human pancreatic islet tumor origin growth hormone-releasing factor.

Abstract: A linear peptide which is an analog of naturally occurring, biologically active substance P having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. The analog has a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue, or a synthetic, a .beta.-amino acid, or a .alpha.-amino acid residue replacing two amino acid residues of the active site.

Abstract: A bradykinin analog which contains nine or ten amino acid residues and at least one [CH.sub.2 NH] pseudopeptide bond, the analog being useful as an antagonist or agonist of the naturally occuring bradykinin.

Abstract: This invention provides novel growth hormone-releasing peptides and a method for increasing the release and raising the levels of growth hormone in mammals. The invention also provides a method for increasing the growth rate of meat producing animals, treating the symptoms of growth hormone deficiencies in mammals and improving the efficiency of feed utilization by meat producing and dairy animals.

Abstract: A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

Abstract: A decapeptide of the formula: N-AC-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A-.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.

Abstract: A method of treating a mammal suffering from cancer by administering to the mammal somatostatin or an analog thereof, the analog being a hexapeptide analog or higher, in a dosage of at least 25 .mu.g/kg/day.

Abstract: This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides ae synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3.This invention also features somatostatin analogs with non-peptide bonds.This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

Abstract: A decapeptide of the formula:N-Ac-A.sup.1 -A.sup.2 -A.sup.3 -SER.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9 -A.sup.10,wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl); A.sup.5 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl); A.sup.6 is D-Lys, D-Arg, .beta.-Nal, D-.beta.-Nal, D-Trp, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl) or D-lys-.epsilon.-NH-R (where R is H, a branched or straight chain or cyclo C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sup.7 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, or C.sub.1-3 alkyl), cyclohexyala, or Trp; A.sup.8 is Arg, Lys, or Lys-.epsilon.-NH-R (where R is H, a branched or straight chain or cyclo C.sub.1 -C.sub.10 alkyl group, or an aryl croup); A.sup.9 is Pro; and A.sup.10 is D-Ala-NH.sub.2, Gly-NH.sub.2, D-Ser, or D-Ser-NH.sub.2 ; provided that at least one of A.

Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.

Abstract: This invention features a method for the solid phase synthesis of non-peptide bonds (CH.sub.2 --NH) in polypeptide chains. These polypeptides are synthesized by standard procedures and the non-peptide bond synthesized by reacting an amino aldehyde and an amino acid in the presence of NaCNBH.sub.3.This invention also features somatostatin analogs with non-peptide bonds.This invention further features a solid phase method of chemically modifying a peptide. The method involves synthesizing .alpha.-N-R and side group N-R analogs of peptides, where R is a an alkyl or aryl group, by reacting a carbonyl-containing compound and an amino acid in the presence of NaCNBH.sub.3.

Abstract: Heptapeptide analogs of somatastatin which inhibit secretion of growth hormone.

Abstract: A decapeptide of the formula:N-Ac-A.sup.1 -A.sup.2 -A.sup.3 -Ser-A.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 -A.sup.8 -A.sup.9, wherein each A.sup.1, A.sup.2, and A.sup.3, independently, is D-.beta.-Nal, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, or C.sub.1-3 alkyl), D-Trp, D-benzothienyl (2)-Ala, or D-benzothienyl (1)-Ala; A.sup.4 is p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), Tyr, Lys, Arg, Leu, Trp, or Nal; A.sup.5 is D-Lys, D-Tyr, D-Arg, D-Phe, D-.beta.-Nal, D-Trp, D-homo-Arg, D-diethyl-homo-Arg, D-p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, or C.sub.1-3 alkyl), or D-Lys-.epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.10 alkyl group, or an aryl group); A.sub.6 is Leu, .beta.-Nal, p-X-Phe (where X is halogen, H, NH.sub.2, NO.sub.2, OH, C.sub.2 F.sub.5, C.sub.1-3 alkyl), or Trp; A.sup.7 is Arg, Lys, or Lys .epsilon.-NH-R (where R is H, a branched or straight chain C.sub.1 -C.sub.6 alkyl group, or an aryl group); A.sub.8 is Pro; and A.sup.

Abstract: An octapeptide of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl, R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 -A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o- m- or p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .alpha.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.