University of Arizona

Biousian Biosystems, Inc.

Polt Hill Institute

Robin L Polt

Evan Jones

John Konhilas

Meredith Hay

Lajos Szabo

Edward J Bilsky

Todd Vanderah

Brittany Forte

Tally Milnes

Michael Heien

Jeanne E Pemberton

Raina M Maier

Dillon Hanrahan

Chenxi Liu

Hanoch Senderowitz

Ricardo Palos Pacheco

Bobbi Anglin

John M Streicher

Torsten A E Falk

Clifford S Coss

Methods for quality control and optimizing the formation and characterization of micelles, vesicles or other aggregates are described herein. Pharmaceutically relevant peptides may be modified to form glycopeptide surfactants which form micelles or other aggregates with another surfactant. Glycopeptide and glycolipid surfactants can aggregate to form particles that enhance drug delivery. The glycopeptide surfactants may be drugs or prodrugs which are delivered via the micelles or other aggregated structures.

Micelles and vesicles for the delivery of glycopeptides

The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and pain.

Ang (1-7) derivative oligopeptides for the treatment of pain

The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and/of impairment.

Ang (1-7) derivative oligopeptides and methods for using and producing the same

Methods for quality control and optimizing the formation and characterization of micelles, vesicles or other aggregates are described herein. Pharmaceutically relevant peptides may be modified to form glycopeptide surfactants which form micelles or other aggregates with another surfactant. Glycopeptide and glycolipid surfactants can aggregate to form particles that enhance drug delivery. The glycopeptide surfactants may be drugs or pro-drugs which are delivered via the micelles or other aggregated structures.

The present invention provides carbohydrate-based surfactants and methods for producing the same. Methods for producing carbohydrate-based surfactants include using a glycosylation promoter to link a carbohydrate or its derivative to a hydrophobic compound.

Carbohydrate-based surfactants

Glycosylated peptides with glycosylation at or near the C-terminal domain of the peptide have an enhanced ability to cross the blood brain barrier (BBB) and/or enhanced half-lives. These glycosylated peptides may be used as drugs. For example, a PACAP peptide with a C-terminal glycosylation, e.g., in lieu of the terminal leucine, functions as a PACagonist with enhanced ability to cross the BBB and with enhanced half-life. The peptides can have a pseudoproline residue with glycosylation at or near the C-terminal domain.

Glycosylated peptides with pseudoproline residues and having enhanced half-lives and ability to cross the blood brain barrier

The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and/or impairment, pain, and traumatic brain injury.

Ang-(1-7) derivative oligopeptides for the treatment of pain and other indications

A glycosylated pleiotropic peptide pituitary adenylate cyclase-activating polypeptide (PACAP) which can both agonize PACreceptors, causing neuroprotective effects, and antagonize VPAC receptors, causing anti-inflammation in several models of acute neuronal damage and neurodegenerative diseases, including ALS, PD, migraines, and certain forms of dementia, is described. Also described is a method of relieving symptoms of ALS, PD, migraines, and certain forms of dementia, comprising administering to a subject in need thereof an effective amount of a glycosylated PACAP.

Glycosylated PACAP/VIP analogues with enhanced CNS penetration for treatment of neurodegenerative diseases

Ang-(1-7) derivative oligopeptides and methods for using and producing the same

ANG-(1-7) derivative oligopeptides and methods for using and producing the same

Synthesis of carbohydrate-based surfactants

Methods and materials are provided for the production of glycosylated GLP-1 peptides that exhibit improved properties. The methods and materials of the present invention may be used for treatment of metabolic conditions, such as Syndrome X and diabetes.

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Tucson, AZ, United States of America

Robin L Polt