Glycoprotein hormone receptors

Overview

Glycoprotein hormone receptors are activated by a non-covalent heterodimeric glycoprotein made up of a common α chain (glycoprotein hormone common alpha subunit CGA, P01215), with a unique β chain that confers the biological specificity to FSH, LH, hCG or TSH. There is binding cross-reactivity across the endogenous agonists for each of the glycoprotein hormone receptors. The deglycosylated hormones appear to exhibit reduced efficacy at these receptors [1,2].

References

  1. Sairam MR. Role of carbohydrates in glycoprotein hormone signal transduction. FASEB J 1989;3:1915-26.
  2. Davidson JS, Assefa D, Pawson A, et al. Irreversible activation of the gonadotropin-releasing hormone receptor by photoaffinity cross-linking: localization of attachment site to Cys residue in N-terminal segment. Biochemistry 1997;36:12881-9.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Family
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Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
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Reference agonist:
FSH
EC50:
8.6 ng/ml
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
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Dermatology
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à la carte
Reference agonist:
rLHα/β
EC50:
26 ng/ml
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
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Musculoskeletal
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Reference agonist:
TSH
EC50:
18 ng/ml
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
FSH
EC50:
10 ng/mL
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
rLHα/β
EC50:
7.7 ng/mL