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Beta-Peptide Inhibitors of Protein-Protein Interactions

蛋白质-蛋白质相互作用的β肽抑制剂

基本信息

批准号：
7465484
负责人：
WILLIAM SETH HORNE
金额：
$ 4.48万
依托单位：
UNIVERSITY OF WISCONSIN-MADISON
依托单位国家：
美国
项目类别：
财政年份：
2006
资助国家：
美国
起止时间：
2006-08-01 至 2009-06-26
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7465484
关键词：
Amino Acid Sequence Amino Acids Antineoplastic Agents Area Binding Biological Biological Assay Biopolymers Carbohydrates Catalysis Cell Surface Receptors Cell physiology Cellular Structures Characteristics Class Clinical Development Dimerization Drug Design Epidermal Growth Factor Epidermal Growth Factor Receptor ErbB Receptor Family Protein Family Fellowship Goals HIV Fusion Inhibitors Home environment Human Individual Lead Libraries Life Ligands Light Link Malignant Neoplasms Membrane Membrane Proteins Molecular Names Nature Nucleic Acids Numbers Organism Peptide Library Peptides Pharmaceutical Chemistry Pharmaceutical Preparations Pharmacologic Substance Physical condensation Polymers Preparation Proteins Randomized Reaction Receptor Activation Receptor Protein-Tyrosine Kinases Reporting Signal Transduction Structural Models Structure T-20 Therapeutic Work anti-cancer therapeutic base combinatorial design inhibitor/antagonist interest member protein protein interaction protein structure function receptor receptor function scaffold small molecule success

项目摘要

DESCRIPTION (provided by applicant): Protein-protein interactions are of great importance in cell function and, consequently, as targets for medicinal chemistry. Where traditional small-molecule based drug design has proven ineffective in the development of antagonists of certain interactions, macromolecular approaches are finding increasing utility. Human epidermal growth factor receptor (EGFR) is a membrane bound cell surface receptor the malfunction of which is linked to a number of cancers. We propose to identify beta-peptide foldamers capable of modulating EGFR function by mimicking protein surfaces involved in receptor dimerization. This project will allow us to explore the scope and limitations of beta-peptide scaffolds as mimics of natural protein surfaces and could lead to the development of new anticancer therapeutics.

描述（由申请人提供）：蛋白质-蛋白质相互作用在细胞功能中非常重要，因此是药物化学的靶标。传统的基于小分子的药物设计在开发某些相互作用的拮抗剂方面被证明是无效的，大分子方法正在发现越来越多的效用。人表皮生长因子受体（EGFR）是一种膜结合细胞表面受体，其功能障碍与许多癌症有关。我们建议通过模拟参与受体二聚化的蛋白质表面来鉴定能够调节EGFR功能的β肽折叠蛋白。这个项目将使我们能够探索β肽支架作为天然蛋白质表面模拟物的范围和局限性，并可能导致新的抗癌疗法的发展。