30 results about "Insulin receptor binding" patented technology

A fibrillation-resistant insulin analogue may be a single-chain insulin analogue or a physiologically acceptable salt thereof, containing an insulin A chain sequence or an analogue thereof and an insulin B chain sequence or an analogue thereof connected by a polypeptide of 4-10 amino acids. The fibrillation-resistant insulin analogue preferably displays less than 1 percent fibrillation with incubation at 37° C. for at least 21 days. A single-chain insulin analogue displays greater in vitro insulin receptor binding than normal insulin while displaying less than or equal binding to IGFR than normal insulin. The fibrillation-resistant insulin may be used to treat a patient using an implantable or external insulin pump, due to its greater fibrillation resistance.

A method treating a mammal by administering a physiologically effective amount of an insulin analogue or a physiologically acceptable salt thereof where the insulin analogue displays more than twofold greater binding affinity to insulin receptor isoform A (IR-A) than insulin receptor isoform B (IR-B). The insulin analogue may be a single-chain insulin analogue or a physiologically acceptable salt thereof, containing an insulin A-chain sequence or an analogue thereof and an insulin B-chain sequence or an analogue thereof connected by a polypeptide of 4-13 amino acids. A single-chain insulin analogue may display greater in vitro insulin receptor binding to IR-A but lower binding to IR-B than normal insulin while displaying less than or equal binding to IGFR than normal insulin.

Provided are an insulin conjugate having improved insulin receptor binding affinity and increased activity, in which a non-peptidyl polymer and an immunoglobulin Fc region are site-specifically linked to an amino acid residue of the insulin beta chain excluding the N-terminus thereof via a covalent bond, a long-acting formulation including the same, and a preparation method thereof. The insulin conjugate of the present invention is used to provide an insulin formulation which exhibits a remarkably increased in vivo activity of the peptide.

A method treating a patient includes administering a physiologically effective amount of a fibrillation-resistant insulin analogue or a physiologically acceptable salt thereof to the patient. The fibrillation-resistant insulin analogue or a physiologically acceptable salt thereof, contains an insulin A-chain sequence modified at position A8 and an insulin B-chain sequence or an analogue thereof. The fibrillation-resistant insulin analogue may exhibit thermodynamic stability similar to or exceeding that of wild-type human insulin and displays a susceptibility to fibrillation similar to or exceeding that of wild-type human insulin. An insulin analogue may display greater in vitro insulin receptor binding than normal insulin while displaying binding to IGFR less than twice that of normal insulin and less than that of fast-acting insulin analogs. The fibrillation-resistant insulin may be used to treat a patient by subcutaneous injection or by using an implantable or external insulin pump, due to its fibrillation resistance.

The present invention relates to the field of biopharmaceuticals, and in particular to a protein, a protein conjugate, a pharmaceutical composition and its use for treating diabetes. The fusion protein of the present invention is obtained by linking two polypeptides, wherein one polypeptide is an interleukin-1 receptor antagonistic protein or an analogue thereof, and another polypeptide is GLP-1 receptor binding polypeptide or an analogue thereof, or an insulin receptor binding polypeptide or an analogue thereof, or a GIP receptor binding polypeptide or an analogue thereof. The fusion proteins of the present invention and conjugates thereof have a significant efficacy in treating diabetes, and can be used in a lower dose, resulting in marked reduction in side effects.

A polypeptide, a nucleic acid molecule encoding the polypeptide and a pharmaceutical composition comprising the polypeptide are provided. The polypeptide is as defined in the description, can bind to insulin receptors, and is effective in reducing blood sugar, reducing glycated hemoglobin, and ameliorating hepato-renal disorders caused by diabetes.

An insulin analog has a reduced insulin titer and a reduced insulin receptor binding affinity compared to the native form for the purpose of increasing the blood half-life of insulin. A conjugate is prepared by linking the insulin analog and a carrier. A long-acting formulation includes the conjugate.

The invention discloses a method for analyzing the binding rate of human insulin and its analogs or conjugates to insulin receptors. First, the insulin receptors are transfected onto HEK-293 cells; antibodies to human insulin receptors are coated on enzyme labels On the plate, the insulin receptor antibody binds to the insulin receptor, human insulin and its analogs or conjugates compete with biotin-labeled insulin for binding to the insulin receptor, avidin binds to biotin, and the receptor binding rate is determined by HRP chromogenicity. The present invention utilizes the principles of antigen-antibody binding, ligand-receptor binding, and biotin binding to avidin to accurately measure the change in insulin receptor binding rate. No pollution, low cost, high accuracy and other requirements.

Disclosed is a recombinant human insulin or analog conjugate thereof. Said conjugate is formed by connecting the µ-amino group of lysine 29 of the B chain to activated polyethylene glycol by means of an amide bond. Further disclosed is a method of preparing said conjugate, a pharmaceutical compound, and a use for said conjugate in preparing medication for treating Type 1 and Type 2 diabetes.