Evolocumab mechanism to reduce LDL cholesterol (Homo sapiens)

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1LDL-C degradedLDLR is recycled tocell surface to bindand extract more LDL-CPCSK9LDL-CLDLREvolocumabPCSK9LDLRLDL-CPCSK9LDLRLDL-CLDLRLDL-CLDLRLDL-CLDL-C degraded alongwith LDLR and PCSK9


Description

Evolocumab (Repatha) is an injectable monoclonal antibody that reduces LDL cholesterol levels. A limited quantity of LDL cholesterol is extracted from circulative blood when PCSK9-bound LDLR is degraded upon internalization in liver cells. Evolocumab competitively binds PCSK9 away from LDLR complexes, which allows LDLR to be recycled, returning to the surface and clearing additional molecules of LDL cholesterol.

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Bibliography

  1. Dorey, Emma; ''PCSK9 inhibitors: the next cholesterol-lowering blockbusters?''; The Pharmaceutical Journal, 2015 DOI Scholia

History

View all...
CompareRevisionActionTimeUserComment
128627view02:10, 17 February 2024EweitzEvolocumab inhibits PCSK9
128626view02:07, 17 February 2024EweitzRefine receptor placement
128625view02:05, 17 February 2024EweitzUse standard metabolite color
128623view01:58, 17 February 2024EweitzEconomize layout
128056view12:44, 23 January 2024EweitzModified description
128055view12:42, 23 January 2024EweitzStandardize case
125296view17:22, 31 January 2023LarsgwFix references
125034view12:17, 16 January 2023Mkutmonfixed reference title
125033view12:16, 16 January 2023Mkutmonadded doi
118453view14:58, 27 May 2021Marvin M2ref removed double lines
116731view10:30, 11 May 2021EweitzModified title
105111view13:06, 8 July 2019DeSlOntology Term : 'hepatocyte' added !
105110view13:05, 8 July 2019DeSlOntology Term : 'altered cholesterol biosynthetic pathway' added !
105109view13:05, 8 July 2019DeSlOntology Term : 'altered cholesterol transport pathway' added !
105108view12:55, 8 July 2019DeSlConverted DataNode type for Evolocumab from protein to metabolite.
88049view13:44, 25 July 2016SusanOntology Term : 'drug pathway' added !
81714view18:08, 25 August 2015MaintBotfixed typo in lit ref
81680view09:59, 23 August 2015EgonwAdded an xref for Evolocumab (which links to at least a CAS registry number).
81671view22:33, 22 August 2015AlexanderPicofixing multiline label
81670view22:32, 22 August 2015AlexanderPicofixing multiline label
81669view22:24, 22 August 2015AlexanderPicoQuick edit to datanode annotation or property
81668view22:22, 22 August 2015AlexanderPicoAdded lit ref
81667view22:13, 22 August 2015AlexanderPicoModified description
81666view22:05, 22 August 2015AlexanderPicoNew pathway

External references

DataNodes

NameTypeDatabase referenceComment
EvolocumabMetaboliteQ15623825 (Wikidata)
LDL-CMetaboliteCHEBI:47774 (ChEBI)
LDLRGeneProductENSG00000130164 (Ensembl)
PCSK9GeneProductENSG00000169174 (Ensembl)

Annotated Interactions

No annotated interactions

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