Suppr超能文献

从全基因组关联研究到炎性关节炎中合理的药物靶点优先级确定

From genome-wide association studies to rational drug target prioritisation in inflammatory arthritis.

作者信息

Fang Hai, Chen Liye, Knight Julian C

机构信息

Wellcome Centre for Human Genetics, University of Oxford, Oxford, UK.

Botnar Research Centre, University of Oxford, Oxford, UK.

出版信息

Lancet Rheumatol. 2020 Jan;2(1):e50-e62. doi: 10.1016/S2665-9913(19)30134-1. Epub 2019 Dec 10.

Abstract

Early identification of genetically validated drug targets can increase the chances of successful late-stage drug development. 81 high-quality genome-wide association studies (GWAS) in diseases related to inflammatory arthritis have been curated into the GWAS catalogue; however, translation of genetic findings from GWAS into rational drug target discovery has been poor. No human genetic findings have completely driven drug development for inflammatory arthritis; however, genetic associations have partly driven the development of abatacept (CTLA-4-Ig) in rheumatoid arthritis and secukinumab (anti-IL-23R) in ankylosing spondylitis. Roadblocks to progress exist, including little knowledge of the genetic architecture and regulatory mechanisms underlying associations, and the need to identify gene regulatory networks and assess target tractability. New opportunities are arising that could maximise the informativeness of GWAS for drug target validation. Genetic variants can be linked to core genes by using functional genomics and then to peripheral genes interconnected to core genes using network information. Moreover, identification of crosstalk between biological pathways might highlight key points for therapeutic intervention.

摘要

早期识别经过基因验证的药物靶点可以增加后期药物研发成功的几率。与炎性关节炎相关疾病的81项高质量全基因组关联研究(GWAS)已被收录进GWAS目录;然而,将GWAS的基因研究结果转化为合理的药物靶点发现的情况却很不理想。尚无人类基因研究结果能完全推动炎性关节炎的药物研发;不过,基因关联在一定程度上推动了类风湿关节炎中阿巴西普(CTLA-4-Ig)以及强直性脊柱炎中司库奇尤单抗(抗IL-23R)的研发。进展存在障碍,包括对关联背后的遗传结构和调控机制了解甚少,以及需要识别基因调控网络并评估靶点的可操作性。新的机遇正在出现,这可能会使GWAS对药物靶点验证的信息量最大化。通过功能基因组学,基因变异可与核心基因相联系,然后利用网络信息与和核心基因相互连接的外围基因相联系。此外,识别生物途径之间的串扰可能会突出治疗干预的关键点。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验