title: Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies.
abstract: BACKGROUND
  The thyroid-stimulating hormone receptor (TSHR) is the essential molecule for thyroid growth and thyroid hormone production. Since it is also a key autoantigen in Graves' disease and is involved in thyroid cancer pathophysiology, the targeting of the TSHR offers a logical model for disease control.
  
  
  METHODS
  We review the structure and function of the TSHR and the progress in both small molecule ligands and TSHR antibodies for their therapeutic potential.
  
  
  CONCLUSIONS
  Stabilization of a preferential conformation for the TSHR by allosteric ligands and TSHR antibodies with selective modulation of the signaling pathways is now possible. These tools may be the next generation of therapeutics for controlling the pathophysiological consequences mediated by the effects of the TSHR in the thyroid and other extrathyroidal tissues.
authors.affiliation: Icahn School of Medicine at Mount Sinai and the James J. Peters VA Medical Center, Thyroid Research Unit , 1 Gustave L Levy Place, New York, NY 10029 , USA +1 212 241 7975 ; +1 212 428 6748 ; terry.davies@mssm.edu.
authors.forename: Terry F
authors.initials: TF
authors.lastname: Davies
authors.forename: Rauf
authors.initials: R
authors.lastname: Latif
mesh_terms: D000818:Animals; D000906:Antibodies / Q000276:immunology; D001324:Autoantigens / Q000276:immunology; D015195:Drug Design; D006111:Graves Disease / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D011989:Receptors, Thyrotropin / Q000276:immunology / Q000378:metabolism*; D015398:Signal Transduction / Q000502:physiology; D013964:Thyroid Neoplasms / Q000188:drug therapy* / Q000473:pathology
chemical_list: D000906:Antibodies; D001324:Autoantigens; D008024:Ligands; D011989:Receptors, Thyrotropin
keywords: Graves’ disease; autoantibodies; glycoprotein-hormone receptor; small molecule ligands; thyroid cancer; thyroid-stimulating hormone receptor