The Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, People's Republic of China.
PLoS One. 2012;7(7):e39782. doi: 10.1371/journal.pone.0039782. Epub 2012 Jul 11.
Due to extensive bioprospecting efforts of the past and technology factors, there have been questions about drug discovery prospect from untapped species. We analyzed recent trends of approved drugs derived from previously untapped species, which show no sign of untapped drug-productive species being near extinction and suggest high probability of deriving new drugs from new species in existing drug-productive species families and clusters. Case histories of recently approved drugs reveal useful strategies for deriving new drugs from the scaffolds and pharmacophores of the natural product leads of these untapped species. New technologies such as cryptic gene-cluster exploration may generate novel natural products with highly anticipated potential impact on drug discovery.
由于过去广泛的生物勘探工作和技术因素,人们对未开发物种的药物发现前景产生了疑问。我们分析了最近从以前未开发物种中获得的批准药物的趋势,这些趋势表明,未开发的具有药物生产潜力的物种尚未接近灭绝,并且很有可能从现有具有药物生产潜力的物种家族和类群中的新物种中提取新药。最近批准的药物的案例研究揭示了从这些未开发物种的天然产物先导物的支架和药效团中提取新药的有用策略。新技术,如隐匿基因簇的探索,可能会产生具有高度预期潜力的新型天然产物,对药物发现产生重大影响。