LDL R

LDL R

LDL R Overview

Molecule Name
LDL receptor
Synonyms
LDLR,FH,FHC,LDLCQ2
Drug Development Progress
Drugs in Clinical Trials4
Approved Drugs0
Highest Development StagePhase 2 Clinical
Target Synonym
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
Background
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 Product List

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Clinical Drug Information

English NameResearch CodeHighest Development StageCompanyIndicationClinical Trial
Phosphorylcholine monoclonal antibodyPC-mAbPhase 2 ClinicalDyax Pharma
Arteritis; Cardiovascular Diseases; ST Elevation Myocardial Infarction
Details
LLG-783 (Novartis)LLG-783Phase 2 ClinicalNovartis Pharma Ag
Details
NGGT-006NGGT-006; NGGT006Phase 1 ClinicalSuzhou Nuojiebei Biotechnology Co Ltd
Homozygous familial hypercholesterolemia
Details
68-Ga-RMX-VH68-Ga-RMX-VHClinicalRadiomedix Inc
Carcinoma, Pancreatic Ductal; Glioblastoma; Pancreatic Neoplasms
Details