PMID- 7890708
OWN - NLM
STAT- MEDLINE
DCOM- 19950418
LR  - 20210210
IS  - 0021-9258 (Print)
IS  - 0021-9258 (Linking)
VI  - 270
IP  - 11
DP  - 1995 Mar 17
TI  - Signal transduction and ligand specificity of the human monocyte chemoattractant 
      protein-1 receptor in transfected embryonic kidney cells.
PG  - 5786-92
AB  - We have examined the ligand specificity and signal transduction pathways of a 
      recently cloned receptor for monocyte chemoattractant protein-1 (MCP-1). In human 
      293 cells stably transfected with the MCP-1 receptor, MCP-1 bound specifically 
      with high affinity (Kd = 260 pM) and induced a rapid mobilization of calcium from 
      intracellular stores. The closely related chemokines MIP-1 alpha, MIP-1 beta, 
      RANTES, interleukin 8 (IL-8), and Gro-alpha were inactive at concentrations as 
      high as 300 nM. Activation of the MCP-1 receptor potently inhibited adenylyl 
      cyclase with an IC50 = 90 pM. Activation of the MIP-1 alpha/RANTES receptor also 
      mediated inhibition of adenylyl cyclase activity but with a different 
      pharmacological profile: MIP-1 alpha (110 pM, IC50), RANTES (140 pM), MIP-1 beta 
      (10 nM), and MCP-1 (820 nM). Mobilization of intracellular calcium and inhibition 
      of adenylyl cyclase were blocked by pertussis toxin, suggesting that the MCP-1 
      receptor coupled to G alpha i. These results demonstrate that the MCP-1 receptor 
      binds and signals in response to picomolar concentrations of MCP-1 in a highly 
      specific manner. Signaling was manifested as mobilization of intracellular 
      calcium and inhibition of adenylyl cyclase and was mediated by a pertussis 
      toxin-sensitive G-protein(s).
FAU - Myers, S J
AU  - Myers SJ
AD  - Gladstone Institute of Cardiovascular Disease, San Francisco, California 
      94141-9100.
FAU - Wong, L M
AU  - Wong LM
FAU - Charo, I F
AU  - Charo IF
LA  - eng
GR  - HL52773/HL/NHLBI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - J Biol Chem
JT  - The Journal of biological chemistry
JID - 2985121R
RN  - 0 (Adenylyl Cyclase Inhibitors)
RN  - 0 (CCR2 protein, human)
RN  - 0 (Chemokine CCL2)
RN  - 0 (Chemotactic Factors)
RN  - 0 (Cytokines)
RN  - 0 (Iodine Radioisotopes)
RN  - 0 (Ligands)
RN  - 0 (Lymphokines)
RN  - 0 (Receptors, CCR2)
RN  - 0 (Receptors, Chemokine)
RN  - 0 (Receptors, Cytokine)
RN  - 0 (Recombinant Proteins)
RN  - EC 3.1.4.- (Type C Phospholipases)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Adenylyl Cyclase Inhibitors
MH  - Binding, Competitive
MH  - Calcium/metabolism
MH  - Cell Line
MH  - Chemokine CCL2
MH  - Chemotactic Factors/*metabolism
MH  - Cytokines/*pharmacology
MH  - Embryo, Mammalian
MH  - Humans
MH  - Iodine Radioisotopes
MH  - Kidney
MH  - Kinetics
MH  - Ligands
MH  - Lymphokines/pharmacology
MH  - Receptors, CCR2
MH  - *Receptors, Chemokine
MH  - Receptors, Cytokine/*metabolism
MH  - Recombinant Proteins/metabolism
MH  - *Signal Transduction
MH  - Substrate Specificity
MH  - Transfection
MH  - Type C Phospholipases/metabolism
EDAT- 1995/03/17 00:00
MHDA- 1995/03/17 00:01
CRDT- 1995/03/17 00:00
PHST- 1995/03/17 00:00 [pubmed]
PHST- 1995/03/17 00:01 [medline]
PHST- 1995/03/17 00:00 [entrez]
AID - S0021-9258(18)81426-0 [pii]
AID - 10.1074/jbc.270.11.5786 [doi]
PST - ppublish
SO  - J Biol Chem. 1995 Mar 17;270(11):5786-92. doi: 10.1074/jbc.270.11.5786.