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Home > Curated Information Page > PubMed Id: 32234959
Gillis A, et al. (2020) Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Sci Signal 13 32234959
This page summarizes selected information from the record referenced above and curated into PhosphoSitePlus®, a comprehensive online resource for the study of protein post-translational modifications (NAR, 2015, 43:D512-20). To learn more about the scope of PhosphoSitePlus®, click here.
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T370-p - MOR-1 (mouse)
Modsite: sARIRQNtREHPstA SwissProt Entrez-Gene
Orthologous residues
MOR‑1 (human): T372‑p, MOR‑1 iso5 (human): T372‑p, MOR‑1 (mouse): T370‑p, MOR‑1 (rat): T370‑p
Characterization
Methods used to characterize site in vivo phospho-antibody, western blotting
Relevant cell lines - cell types - tissues:  293 (epithelial)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Potential in vivo enzymes for site: 
Type Enzyme Evidence Notes
KINASE GRK2 (mouse) transfection of wild-type enzyme, pharmacological inhibitor of upstream enzyme
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
DAMGO increase
fentanyl increase
naloxone DAMGO inhibit treatment-induced increase
Cmpd101 DAMGO inhibit treatment-induced increase
morphine no change compared to control
Downstream Regulation
Effect of modification (function):  molecular association, regulation, receptor internalization, induced
Effect of modification (process):  signaling pathway regulation
Modification regulates interactions with: 
Interacting molecule Interacting domains Effect Consequences (function) Consequences (process) Detection assays
ARRB2 (human) Induces FRET
Comments:  regulates B-arrestin signaling

S375-p - MOR-1 (mouse)
Modsite: QNtREHPstANtVDR SwissProt Entrez-Gene
Orthologous residues
MOR‑1 (human): S377‑p, MOR‑1 iso5 (human): S377‑p, MOR‑1 (mouse): S375‑p, MOR‑1 (rat): S375‑p
Characterization
Methods used to characterize site in vivo phospho-antibody, western blotting
Relevant cell lines - cell types - tissues:  293 (epithelial)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Potential in vivo enzymes for site: 
Type Enzyme Evidence Notes
KINASE GRK2 (mouse) transfection of wild-type enzyme, pharmacological inhibitor of upstream enzyme
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
DAMGO increase
fentanyl increase
naloxone DAMGO inhibit treatment-induced increase
Cmpd101 DAMGO inhibit treatment-induced increase
morphine increase
oxycodone increase
oliceridine increase
PZM21 increase
methadone increase
SR-17018 increase
Downstream Regulation
Effect of modification (function):  molecular association, regulation, receptor internalization, induced
Effect of modification (process):  signaling pathway regulation
Modification regulates interactions with: 
Interacting molecule Interacting domains Effect Consequences (function) Consequences (process) Detection assays
ARRB2 (human) Induces FRET
Comments:  regulates B-arrestin signaling

T376-p - MOR-1 (mouse)
Modsite: NtREHPstANtVDRT SwissProt Entrez-Gene
Orthologous residues
MOR‑1 (human): T378‑p, MOR‑1 iso5 (human): T378‑p, MOR‑1 (mouse): T376‑p, MOR‑1 (rat): T376‑p
Characterization
Methods used to characterize site in vivo phospho-antibody, western blotting
Relevant cell lines - cell types - tissues:  293 (epithelial)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Potential in vivo enzymes for site: 
Type Enzyme Evidence Notes
KINASE GRK2 (mouse) transfection of wild-type enzyme, pharmacological inhibitor of upstream enzyme
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
DAMGO increase
fentanyl increase
naloxone DAMGO inhibit treatment-induced increase
Cmpd101 DAMGO inhibit treatment-induced increase
morphine no change compared to control
Downstream Regulation
Effect of modification (function):  molecular association, regulation, receptor internalization, induced
Effect of modification (process):  signaling pathway regulation
Modification regulates interactions with: 
Interacting molecule Interacting domains Effect Consequences (function) Consequences (process) Detection assays
ARRB2 (human) Induces FRET
Comments:  regulates B-arrestin signaling

T379-p - MOR-1 (mouse)
Modsite: EHPstANtVDRTNHQ SwissProt Entrez-Gene
Orthologous residues
MOR‑1 (human): T381‑p, MOR‑1 iso5 (human): T381‑p, MOR‑1 (mouse): T379‑p, MOR‑1 (rat): T379‑p
Characterization
Methods used to characterize site in vivo phospho-antibody, western blotting
Relevant cell lines - cell types - tissues:  293 (epithelial)
Cellular systems studied:  cell lines
Species studied:  human
Upstream Regulation
Potential in vivo enzymes for site: 
Type Enzyme Evidence Notes
KINASE GRK2 (mouse) transfection of wild-type enzyme, pharmacological inhibitor of upstream enzyme
Treatments, proteins and their effect on site modification: 
Treatments Referenced Treatments Manipulated Protein Referenced Protein Effect Notes
DAMGO increase
fentanyl increase
naloxone DAMGO inhibit treatment-induced increase
Cmpd101 DAMGO inhibit treatment-induced increase
morphine no change compared to control
Downstream Regulation
Effect of modification (function):  molecular association, regulation, receptor internalization, induced
Effect of modification (process):  signaling pathway regulation
Modification regulates interactions with: 
Interacting molecule Interacting domains Effect Consequences (function) Consequences (process) Detection assays
ARRB2 (human) Induces FRET
Comments:  regulates B-arrestin signaling