Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTJIH8Q)

• DTT Name: CCR5 messenger RNA (CCR5 mRNA)
• Synonyms: HIV-1 fusion coreceptor (mRNA); HIV-1 fusion co-receptor (mRNA); Chemokine receptor CCR5 (mRNA); CMKBR5 (mRNA); CHEMR13 (mRNA); CD195 antigen (mRNA); CD195 (mRNA); CCR-5 (mRNA); CC-CKR-5 (mRNA); C-C chemokine receptor type 5 (mRNA); C-C CKR-5 (mRNA)
• Gene Name: CCR5
• DTT Type: Successful target; [1]
• BioChemical Class: mRNA target
• UniProt ID: CCR5_HUMAN
• TTD ID: T72171
• Sequence:
  MDYQVSSPIYDINYYTSEPCQKINVKQIAARLLPPLYSLVFIFGFVGNMLVILILINCKR
  LKSMTDIYLLNLAISDLFFLLTVPFWAHYAAAQWDFGNTMCQLLTGLYFIGFFSGIFFII
  LLTIDRYLAVVHAVFALKARTVTFGVVTSVITWVVAVFASLPGIIFTRSQKEGLHYTCSS
  HFPYSQYQFWKNFQTLKIVILGLVLPLLVMVICYSGILKTLLRCRNEKKRHRAVRLIFTI
  MIVYFLFWAPYNIVLLLNTFQEFFGLNNCSSSNRLDQAMQVTETLGMTHCCINPIIYAFV
  GEKFRNYLLVFFQKHIAKRFCKCCSIFQQEAPERASSVYTRSTGEQEISVGL
• Function: May play a role in the control of granulocytic lineage proliferation or differentiation. Receptor for a number of inflammatory CC-chemokines including CCL3/MIP-1-alpha, CCL4/MIP-1-beta and RANTES and subsequently transduces a signal by increasing the intracellular calcium ion level.
• KEGG Pathway:
  Cytokine-cytokine receptor interaction (hsa04060)
  Chemokine signaling pathway (hsa04062)
  Endocytosis (hsa04144)
  Toxoplasmosis (hsa05145)
  Viral carcinogenesis (hsa05203)
• Reactome Pathway:
  Chemokine receptors bind chemokines (R-HSA-380108)
  G alpha (i) signalling events (R-HSA-418594)
  Binding and entry of HIV virion (R-HSA-173107)

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Maraviroc	DMTL94F	Human immunodeficiency virus infection	1C62	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DdRNAi therapy rHIV7-shl-TAR-CCR5RZ, stem cells	DM0I5LM	Human immunodeficiency virus infection	1C62	Phase 1/2	[2]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SCH-C	DM8J9SF	Human immunodeficiency virus infection	1C62	Discontinued in Phase 1	[3]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
viral macrophage inflammatory protein-II	DMAXOPS	Discovery agent	N.A.	Investigative	[4]

References

• [1] Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human. Biochem Pharmacol. 2005 Dec 19;71(1-2):163-72.
• [2] Progress on RNAi-based molecular medicines. Int J Nanomedicine. 2012; 7: 3971-3980.
• [3] Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9.
• [4] A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science. 1997 Sep 12;277(5332):1656-9.