When will thyrotropin receptor antagonists and inverse thyrotropin receptor agonists become available for clinical use?

Thyroid

Volumn 21, Issue 8, 2011, Pages 817-819

  Emerson, Charles H ^a  

^a UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; ANTITHYROID AGENT; CHORIONIC GONADOTROPIN; HORMONE RECEPTOR BLOCKING AGENT; HORMONE RECEPTOR STIMULATING AGENT; LEVOTHYROXINE; LIOTHYRONINE; RADIOACTIVE IODINE; THYROID HORMONE; THYROTROPIN; THYROTROPIN RECEPTOR; THYROTROPIN RECEPTOR AGONIST; THYROTROPIN RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

CHORIOCARCINOMA; DIFFERENTIATED THYROID CANCER; DRUG EFFICACY; EDITORIAL; GOITER; GRAVES DISEASE; HUMAN; HYPERTHYROIDISM; HYPOPHYSIS TUMOR; HYPOTHYROIDISM; MULTINODULAR GOITER; MUTATIONAL ANALYSIS; NODULAR GOITER; PREGNANCY; PRIORITY JOURNAL; REMISSION; SIGNAL TRANSDUCTION; SOMATIC MUTATION; THYROID CANCER; THYROID FUNCTION; THYROID NODULE; THYROIDECTOMY; THYROTOXICOSIS; THYROTROPIN BLOOD LEVEL; THYROTROPIN RELEASE;

HUMANS; MUTATION; RECEPTORS, THYROTROPIN; THYROTROPIN;

EID: 79961200833     PISSN: 10507256     EISSN: 15579077     Source Type: Journal    
DOI: 10.1089/thy.2011.2108.ed     Document Type: Editorial

References (28)

1. Sherman SI 2011 Targeted therapies for thyroid tumors. Mod Pathol 24(Suppl 2):S44-52.
2. Ladenson PW 2011 Thyroid hormone analogues: Ready for prime time. Thyroid 21:101-102.
3. Allen MD, Neumann S, Gershengorn S 2011 Small molecule thyrotropin receptor agonist activates naturally-occurring TSH-insensitive mutants and reveals their distinct cAMP signal persistence. Thyroid 21:907-912.
4. Titus S, Neumann S, Zheng W, Southall N, Michael S, Klumpp C, Yasgar A, Shinn P, Thomas CJ, Inglese J, Gershengorn MC, Austin CP 2008 Quantitative high- throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor. J Biomol Screen 13:120-127. (Pubitemid 351248693)
5. Neumann S, Raaka BM, Gershengorn MC 2010 Constitutively active thyrotropin and thyrotropin-releasing hormone receptors and their inverse agonists. Methods Enzymol 485:147-160.
6. Neumann S, Raaka BM, Gershengorn MC 2009 Human TSH receptor ligands as pharmacological probes with potential clinical application. Expert Rev Endocrinol Metab 4:669.
7. Neumann S, Kleinau G, Costanzi S, Moore S, Jiang JK, Raaka BM, Thomas CJ, Krause G, Gershengorn MC 2008 A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism. Endocrinology 149:5945-5950.
8. Neumann S, Huang W, Titus S, Krause G, Kleinau G, Alberobello AT, Zheng W, Southall NT, Inglese J, Austin CP, Celi FS, Gavrilova O, Thomas CJ, Raaka BM, Gershengorn MC 2009 Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A 106:12471-12476.
9. Neumann S, Huang W, Eliseeva E, Titus S, Thomas CJ, Gershengorn MC 2010 A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology 151:3454-3459.
10. Neumann S, Gershengorn MC 2011 Small molecule TSHR agonists and antagonists. Ann Endocrinol (Paris) 72:74-76.
11. Neumann S, Eliseeva E, McCoy JG, Napolitano G, Giuliani C, Monaco F, Huang W, Gershengorn MC 2011 A new small-molecule antagonist inhibits Graves' disease antibody activation of the TSH receptor. J Clin Endocrinol Metab 96:548-554.
12. Moore S, Jaeschke H, Kleinau G, Neumann S, Costanzi S, Jiang JK, Childress J, Raaka BM, Colson A, Paschke R, Krause G, Thomas CJ, Gershengorn MC 2006 Evaluation of small-molecule modulators of the luteinizing hormone/ choriogonadotropin and thyroid stimulating hormone receptors: Structure-activity relationships and selective binding patterns. J Med Chem 49:3888-3896. (Pubitemid 43967885)
13. Kleinau G, Haas AK, Neumann S, Worth CL, Hoyer I, Furkert J, Rutz C, Gershengorn MC, Schulein R, Krause G 2010 Signaling-sensitive amino acids surround the allosteric ligand binding site of the thyrotropin receptor. FASEB J 24:2347-2354.
14. Jaschke H, Neumann S, Moore S, Thomas CJ, Colson AO, Costanzi S, Kleinau G, Jiang JK, Paschke R, Raaka BM, Krause G, Gershengorn MC 2006 A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR). J Biol Chem 281:9841-9844. (Pubitemid 43864515)
15. Haas AK, Kleinau G, Hoyer I, Neumann S, Furkert J, Rutz C, Schulein R, Gershengorn MC, Krause G 2011 Mutations that silence constitutive signaling activity in the allosteric ligandbinding site of the thyrotropin receptor. Cell Mol Life Sci 68:159-167.
16. Boutin A, Allen MD, Geras-Raaka E, Huang W, Neumann S, Gershengorn M 2011 Thyrotropin receptor stimulates internalization- independent persistent phosphoinositide signaling. Mol Pharmacol. In press.
17. Reinfelder J, Maschauer S, Foss CA, Nimmagadda S, Fremont V, Wolf V, Weintraub BD, Pomper MG, Szkudlinski MW, Kuwert T, Prante O 2011 Effects of recombinant human thyroid-stimulating hormone superagonists on thyroidal uptake of (18)F-fluorodeoxyglucose and radioiodide. Thyroid 21:783-792.
18. Sanders J, Allen F, Jeffreys J, Bolton J, Richards T, Depraetere H, Nakatake N, Evans M, Kiddie A, Premawardhana LD, Chirgadze DY, Miguel RN, Blundell TL, Furmaniak J, Smith BR 2005 Characteristics of a monoclonal antibody to the thyrotropin receptor that acts as a powerful thyroid-stimulating autoantibody antagonist. Thyroid 15:672-682. (Pubitemid 41117519)
19. Sanders J, Evans M, Betterle C, Sanders P, Bhardwaja A, Young S, Roberts E, Wilmot J, Richards T, Kiddie A, Small K, Platt H, Summerhayes S, Harris R, Reeve M, Coco G, Zanchetta R, Chen S, Furmaniak J, Smith BR 2008 A human monoclonal autoantibody to the thyrotropin receptor with thyroid-stimulating blocking activity. Thyroid 18:735-746. (Pubitemid 352009924)
20. Rees Smith B, Sanders J, Evans M, Tagami T, Furmaniak J 2009 TSH receptor-autoantibody interactions. Horm Metab Res 41:448-455.
21. Haugen BR, Cooper DS, Emerson CH, Luster M, Maciel RM, Biscolla RP, Mazzaferri EL, Medeiros-Neto G, Reiners C, Robbins RJ, Robinson BG, Schlumberger M, Yamashita S, Pacini F 2008 Expanding indications for recombinant human TSH in thyroid cancer. Thyroid 18:687-694. (Pubitemid 352009942)
22. Cooper DS, Doherty GM, Haugen BR, Kloos RT, Lee SL, Mandel SJ, Mazzaferri EL, McIver B, Pacini F, Schlumberger M, Sherman SI, Steward DL, Tuttle RM 2009 Revised American Thyroid Association management guidelines for patients with thyroid nodules and differentiated thyroid cancer. Thyroid 19:1167-1214.
23. Barbesino G 2010 Drugs affecting thyroid function. Thyroid 20:763-770.
24. Yip J, Lang BH, Lo CY 2011 Changing trend in surgical indication and management for Graves' disease. Am J Surg.
25. Emerson CH, Anderson AJ, Howard WJ, Utiger RD 1975 Serum thyroxine and triiodothyronine concentrations during iodide treatment of hyperthyroidism. J Clin Endocrinol Metab 40:33-36.
26. Hershman JM 2004 Physiological and pathological aspects of the effect of human chorionic gonadotropin on the thyroid. Best Pract Res Clin Endocrinol Metab 18:249-265. (Pubitemid 38801668)
27. Emerson CH, Utiger RD 1972 Hyperthyroidism and excessive thyrotropin secretion. N Engl J Med 287:328-333.
28. Gesundheit N, Petrick PA, Nissim M, Dahlberg PA, Doppman JL, Emerson CH, Braverman LE, Oldfield EH, Weintraub BD 1989 Thyrotropin-secreting pituitary adenomas: Clinical and biochemical heterogeneity. Case reports and follow-up of nine patients. Ann Intern Med 111:827-835. (Pubitemid 19283919)