STRUCTURAL BIOLOGY & TARGETED DRUG DESIGN FOR AIDS

我们这个项目的目标是设计、合成和测试小说 针对HIV-1的抗病毒化疗药物 逆转录酶和HIV-1核糖核酸酶H和HIV蛋白酶，其中 是HIV-1生命周期中至关重要的酶。我们设计并制作了 合成了多种化合物，包括： 核苷酸和脱氧核苷酸类似物，焦磷酸类似物 抑制剂，杂芳烃抑制剂，非天然氨基酸， 基于多肽和仿多肽的抑制剂。质谱学已经 与~1H、~(13)C、~(19)F核磁共振联用 和~(31)P核磁共振表征不同化学结构的先导化合物 自然和背景。质谱学仍将是不可或缺的一部分 我们在分析下一代抑制剂方面的研究成果。

Our goal for this project is to design, synthesize and test novel antiviral chemotherapeutic agents, specifically targeted against HIV-1 reverse transcriptase and HIV-1 ribonuclease H and HIV protease, which are vital enzymes to the life cycle of HIV-1. We have designed and synthesized a wide variety of chemical compounds which include: nucleotide and deoxynucleotide analog inhibitors, pyrophosphate analog inhibitors, heteroaromatic inhibitors, unnatural amino acids, peptide-based and petidomimetic inhibitors. Massspectrometry has played an important role in association with 1H NMR, 13C NMR, 19F NMR and 31P NMR in characterizing these lead compounds of diverse chemical nature and background. Mass spectrometry will remain an integral part of our research in analyzing the next generation of inhibitors.