STTR Phase I: Selection of Unnatural Cyclic Peptide Libraries by Messenger Ribonucleic Acid (mRNA) Display

这项小型企业技术转移（STTR）一期项目将探索利用mRNA展示技术分离与抗癌靶点血管内皮生长因子（VEGF）相互作用的非核糖体肽合成酶（NRPS）样肽的可行性。这些肽是重要的药物治疗，表现出抗生素和免疫抑制活性。这项STTR研究将开发肽鉴定的方法，可选择在体外使用遗传技术。这些肽具有非常高的亲和力，具有高特异性的结合，但具有类似药物的特性，如蛋白酶抗性和较长的血清半衰期。该项目将验证和优化技术，以创建nrpps样肽，并将产生抑制VEGF的先导化合物。在商业上，该项目将产生抑制VEGF的nrpps样肽。这些方法将比目前的抗vegf疗法更便宜、更容易地提供潜在的先导化合物。此外，STTR的研究验证了合成环状非自然肽库的新技术，这些肽库类似于nrpps样肽。这项技术将作为一个药物发现平台，用于分离其他治疗方法。

This Small Business Technology Transfer (STTR) Phase I project will explore the feasibility of using mRNA display to isolate non-ribosomal peptide synthetase (NRPS)-like peptides that interact with the anti-cancer target, vascular endothelial growth factor (VEGF). These peptides are important pharmaceutical therapeutics that exhibit antibiotic and immunosuppressive activities. This STTR research will develop methods for peptide identification that are selectable in vitro using genetic techniques. These peptides exhibit very high affinities, show high specificities of binding, but have drug-like properties such as protease resistance and long serum half-lives. This project will validate and optimize the technology to create NRPS-like peptides and will result in a lead compound for VEGF inhibition.Commercially, this project will result in NRPS-like peptides that inhibit VEGF. These methods will provide potential lead compounds more cheaply and easily than current anti-VEGF therapeutics. Additionally, the STTR research validates new technology to synthesize cyclic, unnatural peptide libraries that resemble NRPS-like peptides. This technology will serve as a drug discover platform for the isolation of other therapeutics.