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LDL R信息

英文名称:LDL receptor
中文名称:低密度脂蛋白受体
靶点别称:FHCL1,Low-density lipoprotein receptor,LDLR,LDL receptor,Low Density Lipoprotein Receptor,Low-Density Lipoprotein Receptor Class A Domain-Containing Protein 3,Familial Hypercholesterolemia,LDLCQ2,FHC,FH,Receptors, LDL
上市药物数量:0
临床药物数量:6
最高研发阶段:临床二期

LDL R 分子别名

LDLR,FH,FHC,LDLCQ2

LDL R 分子背景

Low-Density Lipoprotein (LDL) Receptor is also known as LDLR, FH, FHC, LDLCQ2, and is a mosaic protein of ~840 amino acids (after removal of signal peptide) that mediates the endocytosis of cholesterol-rich LDL. It is a cell-surface receptor that recognizes the apoprotein B100 which is embedded in the phospholipid outer layer of LDL particles. The receptor also recognizes the apoE protein found in chylomicron remnants and VLDL remnants (IDL). It belongs to the Low density lipoprotein receptor gene family. LDL receptor complexes are present in clathrin-coated pits (or buds) on the cell surface, which when bound to LDL-cholesterol via adaptin, are pinched off to form clathrin-coated vesicles inside the cell. This allows LDL-cholesterol to be bound and internalized in a process known as endocytosis and prevents the LDL just diffusing around the membrane surface. This occurs in all nucleated cells (not erythrocytes), but mainly in the liver which removes ~70% of LDL from the circulation. Synthesis of receptors in the cell is regulated by the level of free intracellular cholesterol; if it is in excess for the needs of the cell then the transcription of the receptor gene will be inhibited. LDL receptors are translated by ribosomes on the endoplasmic reticulum and are modified by the Golgi apparatus before travelling in vesicles to the cell surface. LDL is directly involved in the development of atherosclerosis, due to accumulation of LDL-cholesterol in the blood. Atherosclerosis is the process responsible for the majority of cardiovascular diseases.

LDL R 前沿进展

LDL R临床药物信息

英文名称 研发代码 研发阶段 公司 适应症 临床试验
LLG-783 (Novartis) LLG-783 临床二期 诺华制药 详情
BI-905681 BI-905681 Boehringer Ingelheim Ltd 详情
Serpin Peptide 16 SP-16 Serpin Pharma 详情
Phosphorylcholine monoclonal antibody PC-mAb 临床二期 Dyax Pharma ST段抬高型心肌梗死, 心脏和血管疾病, 动脉炎 详情

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