Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) including but not limited to conjugates comprising FK-506 and ascomycin. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating. Further embodiments include methods for making the inventive compound. Additional embodiments of the invention are also discussed herein.

Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) including but not limited to conjugates comprising FK-506 and ascomycin. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating. Further embodiments include methods for making the inventive compound. Additional embodiments of the invention are also discussed herein.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: Multicomponent compositions and methods of use thereof are disclosed herein. Some embodiments of the present invention include multicomponent compositions comprising a first component and a second component, where the first component comprises a notch influencing molecule and the second component comprises a GPCR targeted molecule. Kits comprising the multicomponent composition are also disclosed. Methods for providing the multicomponent composition to one or more cells are additionally provided. Further embodiments include methods of using the multicomponent composition such as, for example, methods of administering the multicomponent composition and method of treating organisms (such as mammals) using the multicomponent composition.

Abstract: Featured are methods and compositions for treating, managing, preventing, or reducing injury to the kidney of a mammal (e.g., a human) caused by one or more iodinated radiocontrast media. The methods include administering an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds, which includes native human PACAP38, native human PACAP27, native human vasoactive intestinal peptide (VIP), their agonists, analogs, fragments, and derivatives, with activities toward one or more of the PACAP/VIP receptors, including all of their various isoforms. Also provided are pharmaceutical compositions of one or more PACAP-like compounds, either alone or in combination with one or more other prophylactic/therapeutic agents useful for treating, managing, or preventing injury to the kidney of a mammal (e.g., a human) undergoing treatment with one or more iodinated radiocontrast media.

Abstract: This invention relates to analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders. These PACAP analogs coupled to suitable radionuclides can be used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, and coupled to small molecule therapeutics can be used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP analogs of the invention either alone or in combination with one or more other prophylactic/therapeutic agent.

Abstract: The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperpro-liferative disorders.

Abstract: The present invention is directed to a method of decreasing the rate of proliferation of medullary thyroid carcinoma cells which comprises contacting medullary thyroid carcinoma cells with one or more SSTR2 agonist. A somatostatin receptor antagonist having the formula Cpa-cyclo(D-Cys-4-Pal-D-Trp-Lys-Thr-Cys)-Nal-NH2 is also disclosed.

Abstract: The invention features somatostatin antagonists having a D-amino acid at the second residue.

Abstract: This invention relates to novel analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders, including (but not limited to) cancer and autoimmune disease. These PACAP analogs can be coupled to suitable radionuclides and used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, or coupled to small molecule therapeutics and used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP-like compounds of the invention either alone or in combination with one or more other prophylactic/therapeutic agents.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: This invention relates to novel analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders, including (but not limited to) cancer and autoimmune disease. These PACAP analogs can be coupled to suitable radionuclides and used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, or coupled to small molecule therapeutics and used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP-like compounds of the invention either alone or in combination with one or more other prophylactic/therapeutic agents.

Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18 (SEQ ID NO: 93), wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

Abstract: Featured are methods and compositions for treating, managing, preventing, or reducing injury to the kidney of a mammal (e.g., a human) caused by one or more iodinated radiocontrast media. The methods include administering an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds, which includes native human PACAP38, native human PACAP27, native human vasoactive intestinal peptide (VIP), their agonists, analogs, fragments, and derivatives, with activities toward one or more of the PACAP/VIP receptors, including all of their various isoforms. Also provided are pharmaceutical compositions of one or more PACAP-like compounds, either alone or in combination with one or more other prophylactic/therapeutic agents useful for treating, managing, or preventing injury to the kidney of a mammal (e.g., a human) undergoing treatment with one or more iodinated radiocontrast media.

Abstract: Multicomponent compositions and methods of use thereof are disclosed herein. Some embodiments of the present invention include multicomponent compositions comprising a first component and a second component, where the first component comprises a notch influencing molecule and the second component comprises a GPCR targeted molecule. Kits comprising the multicomponent composition are also disclosed. Methods for providing the multicomponent composition to one or more cells are additionally provided. Further embodiments include methods of using the multicomponent composition such as, for example, methods of administering the multicomponent composition and method of treating organisms (such as mammals) using the multicomponent composition.

Abstract: The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

Abstract: The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.

Abstract: This invention relates to novel analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders, including (but not limited to) cancer and autoimmune disease. These PACAP analogs can be coupled to suitable radionuclides and used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, or coupled to small molecule therapeutics and used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP-like compounds of the invention either alone or in combination with one or more other prophylactic/therapeutic agents.

Abstract: This invention relates to methods and compositions for the treatment, management, reduction, or prevention of injuries to one or more major organs of the body, e.g., the brain, heart, lung, kidneys, liver, and gastrointestinal tract, of a mammal (e.g., a human) caused by one or more calcineurin or mammalian target of rapamycin (mTOR) complex inhibitors. The methods include administering an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds to the mammal.