書誌事項
- タイトル別名
-
- Development and functional analysis of novel PCSK9/LDLR interaction inhibitors for hypercholesterolemia treatment
抄録
<p>Hypercholesterolemia characterized by excessively elevated levels of plasma low-density lipoprotein-cholesterol (LDLc) increases the risk of atherosclerosis, causing cardiovascular disease and cerebrovascular disease. Proprotein convertase subtilisin/kexin type 9 (PCSK9), which is secreted from liver, interacts with LDL-receptor (LDLR) that uptakes LDLc from plasma into hepatocytes. The PCSK9-LDLR interaction leads degradation of the LDLR on hepatocytes, resulting in elevation of plasma LDLc levels. Although anti-PCSK9 antibodies that inhibit PCSK9-LDLR interaction have been used for the treatment of hypercholesterolemia, the antibody agents are very expensive because they are produced using mammalian cells. To overcome this problem, it is necessary to develop PCSK9/LDLR interaction inhibitors that are produced by chemical synthesis to be low-cost in hypercholesterolemia treatment.</p><p> Here, we report the discovery of novel cyclic peptides that bind to PCSK9 by using the mRNA display evolution based on an Escherichia coli reconstituted cell-free translation system (PURE system) combined with genetic code expansion technique and functional analysis of the cyclic peptides.</p>
収録刊行物
-
- 日本薬理学会年会要旨集
-
日本薬理学会年会要旨集 94 (0), 1-P2-04-, 2021
公益社団法人 日本薬理学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390287441188914176
-
- NII論文ID
- 130008001238
-
- ISSN
- 24354953
-
- 本文言語コード
- ja
-
- データソース種別
-
- JaLC
- Crossref
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可