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Artwork for Biotech Bar

以轻松愉快的方式聊聊AI制药

PublishesTwice monthlyEpisodes7Founded3 years ago
Language
ZH-CN
Categories
Natural SciencesTechnologyScience

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Artwork for Biotech Bar

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哈喽大家好,我是钰沐菡,欢迎回来。我们的播客在段更了一段时间之后, 终于要重新跟大家见面了。接下来的几期,我们会聚焦小分子药物领域,跟大家聊一下最近很火的减肥药,靶向GLP1受体的小分子激动剂,靶向降解药物,分子胶和PROTAC等小分子药物领域的进展。

本期节目,我们来聊一聊最近很火的药物靶点GLP1R (glucagon-like peptide-1 receptor),具体来聊一聊GLP1R激动剂开发的历史,小分子激动剂最近的进展,结构生物学以及近些年冷冻电镜技术得快速发展对于GLP1受体以... more

小核酸药物在当前医药行业中非常火热,但在递送技术的创新层面依然存在困境,已上市的小核酸药物仅能针对肝脏靶点。小核酸抗体偶联药物(Antibody-oligonucleotide conjugates,AOC)和小核酸多肽偶联药物(Peptide-oligonucleotide conjugates,POC)利用抗体或多肽将治疗性寡核苷酸递送至特定细胞或组织,将抗体/多肽的组织特异性优势,与小核酸的靶点特异性优势相结合,可一定程度上用于解决目前小核酸药物仅能通过脂质纳米颗粒(LNP)、N-乙酰半乳... more

"靶向分子+偶联药物”模式(XDC)由靶向分子、连接体 (linker)、效应分子(payload)组成,识别肿瘤细胞后内吞进入溶酶体后释放药物,通过诱导微管抑制、DNA损伤引起细胞凋亡,同时也通过旁观者效应杀死周围肿瘤细胞。

抗体偶连药物 (ADC)中使用的payload一般是细胞毒性化合物。目前最常用的payload主要针对DNA或微管蛋白,针对DNA的有:卡利霉素、双卡霉素、PBD、SN-38和DXd,针对微管蛋白的有 Auristatins(MMAE、MMAF) 和美登素衍生物(DM2,... more

"靶向分子+偶联药物”模式(XDC)对于肿瘤的靶向治疗意义重大,与传统化疗的大面积杀伤特性不同,XDC能够精准识别、攻击肿瘤细胞,可使用更少的药物达到更好治疗效果和更低的毒性。XDC由靶向分子、连接体、细胞毒性药物组成,识别肿瘤细胞后内吞进入溶酶体后释放药物,通过诱导微管抑制、DNA损伤引起细胞凋亡,同时也通过旁观者效应杀死周围肿瘤细胞。XDC的优点主要体现在靶向分子上,它不但帮助药物定位,并且所具备的多种特征也用来维持药物稳定和后续释放,比如和受体结合的亲和性和特异性,稳定性,以及是否可以透膜... more

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