대구경북첨단의료산업진흥재단 / Tara Man Kadayat, 조성진*, 진정욱*
Abstract
One of the three subtypes of the peroxisome proliferator-activated receptor (PPAR) functioning as a transcription factor is the PPARor PPARδ. PPARδ is crucial to pathophysiological processes, including metabolic disorders, liver diseases, and cardiovascular diseases. In the past, the clinical development of PPARδ-selective agonist drugs has been stalled due to potential safety-related issues. Despite the elusiveness of such a drug, efforts continue in developing drugs that target PPARδ due to advances in the knowledge of the PPARδ receptor's structure and functions. While several preclinical and clinical studies are reported on PPARδ agonists, there is limited data with no clinical evidence available for PPARδ-selective antagonists. In this review, we mainly focus on the challenges of PPARδ selectivity and the medicinal chemistry of most active agonists discovered by different pharmaceutical companies and institutes. With this in mind, we also provide an update on the development status of PPARδ agonists that are undergoing clinical trials and their therapeutic promise for the treatment of various diseases.
Tara Man Kadayat, Aarajana Shrestha, Yong Hyun Jeon, Hongchan An, Jina Kim, Sung Jin Cho, Jungwook Chin
편집위원
핵수용체중에 하나인 PPARdelta에 대해서 최근 다양한 대사성 질환과 관련해서 리뷰가 되어 있음. 대구경북첨단의료산업진흥재단에서 개발하고 있는 이와 관련된 다양한 리간드들을 방사선동위원소 표지하여 임상에서 활용할 수 있는 핵의학영상조영제를 개발하면 좋을 것 같음.
2020-07-31 16:28:13