"CLICK CHEMISTRY" ASSEMBLY OF HIV PROTEASE INHIBITORS

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 艾滋病毒蛋白水解酶靶标的性质和重要性是众所周知的。耐药性演变的问题是 现在被认为是有效的长期治疗的主要障碍。指导下的新型合成方法 通过计算机对接，有望产生更有效的艾滋病毒蛋白酶抑制剂，这些抑制剂在脸上是强健的 抵抗的力量。在蛋白酶突变体的背景下利用“点击化学”原位合成抑制剂的可能性 指出了解决这个问题的一种新的灵活方法。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. The nature and importance of the HIV protease target is well known. The problem of the evolution of drug resistance is now recognized as a major impediment to effective long-term therapeutic treatment. Novel synthetic approaches, guided by computational docking hold the promise of generating more effective HIV protease inhibitors, that are robust in the face of resistance. The possibilities of in situ synthesis of inhibitors utilizing "click chemistry" in the context of protease mutants points to a new flexible approach to this problem.