Page last updated: 2024-10-24

PCSK9-AnxA2 complex

Definition

Target type: cellularcomponent

A protein complex consisting of the serine protease PCSK9 (proprotein convertase subtilisin/kexin-9) and annexin A2 (AnxA2). [GOC:BHF, GOC:nc, PMID:22848640]

The PCSK9-AnxA2 complex is a protein complex that plays a role in regulating cholesterol levels. The cellular component of this complex can be described as follows:

- **Localization:** The PCSK9-AnxA2 complex is primarily located in the **trans-Golgi network (TGN)**, a cellular compartment involved in protein sorting and trafficking.
- **Membrane Association:** Both PCSK9 and AnxA2 are **membrane-associated proteins**. PCSK9 interacts with the **luminal domain of the low-density lipoprotein receptor (LDLR)**, a transmembrane protein responsible for cholesterol uptake. AnxA2 is known to associate with **lipid rafts**, specialized membrane microdomains enriched in cholesterol and sphingolipids.
- **Interaction with Other Components:** The interaction between PCSK9 and AnxA2 likely involves the **interaction of their respective transmembrane domains**. The complex may also interact with other proteins involved in **vesicle trafficking and protein sorting**, such as **adaptins and clathrin**.
- **Dynamic Nature:** The cellular localization and composition of the PCSK9-AnxA2 complex may vary depending on factors such as **cell type, cellular state, and the presence of specific ligands or inhibitors**.

Overall, the cellular component of the PCSK9-AnxA2 complex represents a dynamic and multifaceted entity within the TGN, playing a critical role in cholesterol metabolism and lipoprotein trafficking.'
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Proteins (2)

ProteinDefinitionTaxonomy
Proprotein convertase subtilisin/kexin type 9A proprotein convertase subtilisin/kexin type 9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8NBP7]Homo sapiens (human)
Annexin A2An annexin A2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07355]Homo sapiens (human)

Compounds (3)

CompoundDefinitionClassesRoles
s 1033(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide
anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
N-(3,4-dimethylphenyl)-2-[[5-[[(4,6-dimethyl-2-pyrimidinyl)thio]methyl]-4-(2-furanylmethyl)-1,2,4-triazol-3-yl]thio]acetamideanilide
PF-06446846PF-06446846 : A triazolopyridine that is 3H-[1,2,3]triazolo[4,5-b]pyridine substituted by a 4-{(3-chloropyridin-2-yl)[(3R)-piperidin-3-yl]carbamoyl}phenyl group at position 3. It is a potent inhibitor of PCSK9.

PF-06446846: inhibits translation of PCSK9 ;structure in first source
benzamides;
monochloropyridine;
piperidines;
tertiary carboxamide;
triazolopyridine
antilipemic drug;
EC 3.4.21.61 (kexin) inhibitor