IMMUNOSUPPRESSANT ANALOGS THROUGH TARGETED GENETICS

环孢素将移植科学领域带入了 医学的主流。不幸的是，长期的生存和质量 移植受者的寿命仍然严重减少。 最近，天然产物FK-506和雷帕霉素在 研究表明比环孢素更安全、更有效、更有效。 此外，这些药物似乎具有协同作用，可能是因为 它们干扰免疫反应的不同途径。小说 化学合成的FK-506和雷帕霉素类似物有助于 阐明这些药物的作用机制。其他新类比 可能导致毒性较低的药物或联合治疗的新选择。 费马逻辑的科学家，在基因操作方面拥有公认的技能 放线菌，建议开发基因技术作为替代方案 到化学合成以生产新的类似物。在第一阶段， 基因系统将在生产微生物中得到发展。在……里面 第二阶段，基因工具将被用来操纵生物合成 通过靶向基因失活或替换的途径。类似于 量身定做的结构修改可以通过以下方式实现 发酵。新的结构将获得专利，进行生物测试， 并对临床测试或进一步的化学物质开放许可 由感兴趣的合作伙伴进行开发。

Cyclosporin brought the field of transplantation science into the mainstream of medicine. Unfortunately, long-term survival and quality of life for transplant recipients are still severely diminished. Recently, the natural products, FK-506 and rapamycin, have proven in studies to be safe, more potent, and more effective than cyclosporin. Furthermore, these drugs appear to act synergistically, possibly because they interfere with different pathways of the immune response. Novel chemically-synthesized analogs of FK-506 and rapamycin have helped elucidate the mechanism of action of these drugs. Other new analogs could lead to less toxic drugs or new choices for combination therapy. FermaLogic scientists, with proven skills in the genetic manipulation of Actinomycetes, propose to develop genetic technology as an alternative to chemical synthesis for producing novel analogs. In Phase One, a genetic system would be developed in the producing micro-organism. In Phase Two, the genetic tools would be used to manipulate the biosynthetic pathway by targeted gene inactivation or replacement. Analogs with tailored structural modifications could be produced inexpensively through fermentation. Novel structures would be patented, biologically tested, and open to licensing for clinical testing or further chemical development by interested partners.