Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTH0DUS)

• DTT Name: Low-density lipoprotein receptor (LDL-R)
• Synonyms: LDL receptor
• Gene Name: LDLR
• DTT Type: Successful target; [1]
• BioChemical Class: Low density lipoprotein receptor
• UniProt ID: LDLR_HUMAN
• TTD ID: T94692
• Sequence:
  MGPWGWKLRWTVALLLAAAGTAVGDRCERNEFQCQDGKCISYKWVCDGSAECQDGSDESQ
  ETCLSVTCKSGDFSCGGRVNRCIPQFWRCDGQVDCDNGSDEQGCPPKTCSQDEFRCHDGK
  CISRQFVCDSDRDCLDGSDEASCPVLTCGPASFQCNSSTCIPQLWACDNDPDCEDGSDEW
  PQRCRGLYVFQGDSSPCSAFEFHCLSGECIHSSWRCDGGPDCKDKSDEENCAVATCRPDE
  FQCSDGNCIHGSRQCDREYDCKDMSDEVGCVNVTLCEGPNKFKCHSGECITLDKVCNMAR
  DCRDWSDEPIKECGTNECLDNNGGCSHVCNDLKIGYECLCPDGFQLVAQRRCEDIDECQD
  PDTCSQLCVNLEGGYKCQCEEGFQLDPHTKACKAVGSIAYLFFTNRHEVRKMTLDRSEYT
  SLIPNLRNVVALDTEVASNRIYWSDLSQRMICSTQLDRAHGVSSYDTVISRDIQAPDGLA
  VDWIHSNIYWTDSVLGTVSVADTKGVKRKTLFRENGSKPRAIVVDPVHGFMYWTDWGTPA
  KIKKGGLNGVDIYSLVTENIQWPNGITLDLLSGRLYWVDSKLHSISSIDVNGGNRKTILE
  DEKRLAHPFSLAVFEDKVFWTDIINEAIFSANRLTGSDVNLLAENLLSPEDMVLFHNLTQ
  PRGVNWCERTTLSNGGCQYLCLPAPQINPHSPKFTCACPDGMLLARDMRSCLTEAEAAVA
  TQETSTVRLKVSSTAVRTQHTTTRPVPDTSRLPGATPGLTTVEIVTMSHQALGDVAGRGN
  EKKPSSVRALSIVLPIVLLVFLCLGVFLLWKNWRLKNINSINFDNPVYQKTTEDEVHICH
  NQDGYSYPSRQMVSLEDDVA
• Function: In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis.
• KEGG Pathway:
  Endocytosis (hsa04144)
  Ovarian steroidogenesis (hsa04913)
  Bile secretion (hsa04976)
  Toxoplasmosis (hsa05145)
  Hepatitis C (hsa05160)
• Reactome Pathway:
  Chylomicron-mediated lipid transport (R-HSA-174800)
  Retinoid metabolism and transport (R-HSA-975634)
  LDL-mediated lipid transport (R-HSA-171052)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Porfimer Sodium	DM7ZWNY	Non-small-cell lung cancer	2C25.Y	Approved	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alpha-D-Mannose	DMF5DLW	Discovery agent	N.A.	Investigative	[2]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Lung cancer	2C82	Lung tissue	2.34E-41	-1.56	-1.5

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [2] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.