Increased plasma membrane expression of human follicle-stimulating hormone receptor by a small molecule thienopyr(im)idine

Molecular and Cellular Endocrinology

Volumn 298, Issue 1-2, 2009, Pages 84-88

  Janovick, Jo Ann ^a   Maya Núñez, Guadalupe ^b   Ulloa Aguirre, Alfredo ^a,b   Huhtaniemi, Ilpo T ^c   Dias, James A ^d   Verbost, Pieter ^e   Conn, P Michael ^a,b,f  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^b Hospital Luis Castelazo Ayala   (Mexico)

^c IMPERIAL COLLEGE LONDON   (United Kingdom)

^d WADSWORTH CENTER   (United States)

^e MERCK RESEARCH LABORATORIES   (United States)

^f OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

FSH receptor; GPCR; Peptidomimetic; Pharmacoperone; Receptor; Small molecule; Therapeutics

Indexed keywords

FOLLITROPIN RECEPTOR; LUTEINIZING HORMONE; ORG 41841; PYRIMIDINE DERIVATIVE; THIENOPYR(IM)IDINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING SITE; CELL MEMBRANE; CONTROLLED STUDY; DRUG EFFECT; DRUG STRUCTURE; ENDOPLASMIC RETICULUM; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION;

ANIMALS; CELL MEMBRANE; CERCOPITHECUS AETHIOPS; COS CELLS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MODELS, BIOLOGICAL; PROTEIN BINDING; PROTEIN TRANSPORT; PYRIDINES; PYRIMIDINES; RECEPTORS, FSH; RECEPTORS, LH; THIOPHENES; TRANSFECTION;

EID: 57749204782     PISSN: 03037207     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.mce.2008.09.015     Document Type: Article

References (30)

1. Bernier V., Lagace M., Bichet D.G., and Bouvier M. Pharmacological chaperones: potential treatment for conformational diseases. Trends Endocrinol. Metab. 15 (2004) 222-228
2. Castro-Fernandez C., Maya-Nunez G., and Conn P.M. Beyond the signal sequence: protein routing in health and disease. Endocr. Rev. 26 (2005) 479-503
3. Cohen B.D., Bariteau J.T., Magenis L.M., and Dias J.A. Regulation of follitropin receptor cell surface residency by the ubiquitin-proteasome pathway. Endocrinology 144 (2003) 4393-4402
4. Conn P.M., Ulloa-Aguirre A., Ito J., and Janovick J.A. G protein-coupled receptor trafficking in health and disease: lessons learned to prepare for mutant rescue in vivo. Pharmacol. Rev. 59 (2007) 225-250
5. Conn P.M., Knollman P.E., Brothers S.P., and Janovick J.A. Protein folding as post-translational regulation: evolution of a mechanism for controlled plasma membrane expression of a GPCR. Mol. Endocrinol. 20 (2006) 3035-3041
6. Conn P.M., Janovick J.A., Brothers S.P., and Knollman P.E. 'Effective inefficiency': cellular control of protein trafficking as a mechanism of post-translational regulation. J. Endocrinol. 190 (2006) 13-16
7. Conn P.M., Leaños-Miranda A., and Janovick J.A. Protein origami: therapeutic rescue of misfolded gene products. Mol. Interv. 2 (2002) 308-316
8. Fishburn C.S., Elazar Z., and Fuchs S. Differential glycosylation and intracellular trafficking for the long and short isoforms of the D2 dopamine receptor. J. Biol. Chem. 270 (1995) 29819-29824
9. Gluzman Y. SV40-transformed simian cells support the replication of early SV40 mutants. Cell 23 (1981) 175-182
10. Harper J.F., and Brooker G. Femtomole sensitive radioimmunoassay of cyclic AMP and cyclic GMP after 2′0 acetylation by acetic anhydride in aqueous solution. J. Cyclic Nucleotide Res. 1 (1975) 207-218
11. Hong S., Phand T., Ji I., and Hi T.H. The amino-terminal region of the luteinizing hormone/choriogonadotropin receptor contacts both subunits of human choriogonadotropin. J. Biol. Chem. 273 (1998) 13835-13840
12. Jäschke H., Neumann S., Moore S., Thomas C.J., Colson A.-O., Costanzi S., Kleinau G., Jiang J.-K., Paschke R., Raaka B.M., Krause G., and Gershengorn M.C. 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 (2006) 9841-9844
13. Janovick J.A., Knollman P.E., Brothers S.P., Ayala-Yanez R., Aziz A.S., and Conn P.M. Regulation of G protein-coupled receptor trafficking by inefficient plasma membrane expression: molecular basis of an evolved strategy. J. Biol. Chem. 281 (2006) 8417-8425
14. Janovick J.A., Maya-Nuñez G., and Conn P.M. Rescue of hypogonadotropic hypogonadism-causing and manufactured GnRH receptor mutants by a specific protein-folding template: misrouted proteins as a novel diseased etiology and therapeutic target. J. Clin. Endocrinol. Metab. 87 (2002) 3255-3262
15. Lu M., Staszewski L., Echeverri F., Xu H., and Moyer B.D. Endoplasmic reticulum degradation impedes olfactory G-protein coupled receptor functional expression. BMC Cell. Biol. 5 (2004) 34
16. Lu M., Echeverri F., and Moyer B.D. Endoplasmic reticulum retention, degradation, and aggregation of olfactory G-protein coupled receptors. Traffic 4 (2003) 416-433
17. Nechamen C.A., and Dias J.A. Point mutations in follitropin receptor result in ER retention. Mol. Cell. Endocrinol. 201 (2003) 123-131
18. Nechamen C.A., and Dias J.A. Human follicle stimulating hormone receptor trafficking and hormone binding sites in the amino terminus. Mol. Cell. Endocrinol. 166 (2000) 101-110
19. Petäjä-Repo U.E., Hogue M., Bhalla S., Laperrière A., Morello J.-P., and Bouvier M. Ligands act as pharmacological chaperones and increase the efficiency of δ opioid receptor maturation. EMBO J. 21 (2002) 1628-1637
20. Petäjä-Repo U.E., Hogue M., Laperriere A., Walker P., and Bouvier M. Export from the endoplasmic reticulum represents the limiting step in the maturation and cell surface expression of the human delta opioid receptor. J. Biol. Chem. 275 (2000) 13727-13736
21. Pietilä E.M., Tuusa J.T., Apaja P.M., Aatsinki J.T., Hakalahti A.E., Rajaniemi H.J., and Petäjä-Repo U.E. Inefficient maturation of the rat luteinizing hormone receptor. A putative way to regulate receptor numbers at the cell surface. J. Biol. Chem. 280 (2005) 26622-26629
22. Rannikko A., Pakarinen P., Manna R.R., Beau I., Misrahi M., Aittomaki K., and Huhtaniemi I. Functional characterization of the human FSH receptor with an inactivating Ala189Val mutation. Mol. Hum. Reprod. 8 (2002) 311-317
23. 3 cells stably transfected with gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid. Endocrinology 135 (1994) 2220-2227
24. Steiner A.L., Parker C.W., and Kipnis D.M. Radioimmunoassay for cyclic nucleotides. J. Biol. Chem. 247 (1972) 1106-1113
25. Timossi C., Ortiz-Elizondo C., Pineda D.B., Dias J.A., Conn P.M., and Ulloa-Aguirre A. Functional significance of the BBXXB motif reversed present in the cytoplasmic domains of the human follicle-stimulating hormone receptor. Mol. Cell. Endocrinol. 223 (2004) 17-26
26. Ulloa-Aguirre A., Janovick J.A., Leaños-Miranda A., and Conn P.M. G protein-coupled receptor trafficking: understanding the chemical basis of health and disease. AC Chem. Biol. 1 (2006) 631-638
27. Ulloa-Aguirre A., Janovick J.A., Brothers S.P., and Conn P.M. Pharmacological rescue of conformationally-defective proteins: implications for the treatment of human disease. Traffic 5 (2004) 821-837
28. Uribe A., Zariñán T., Pérez-Solís M., Gutiérrez-Sagal R., Jardón-Valadez E., Piñeiro A., Dias J.A., and Ulloa-Aguirre A. Functional and structural roles of conserved cysteine residues in the carboxyl-terminal domain of the follicle-stimulting hormone receptor in human embryonic kidney 293 cells. Biol. Reprod. 78 (2008) 869-882
29. van Straten N.C., Schoonus-Gerritsma G.G., van Someren R.G., Draaijer J., Adang A.E.P., Timmers C.M., Hanssen R.G.J.M., and van Boeckel C.A.A. The first orally active low molecular weight agonists for the LH receptor: thienopyr(im)idines with therapeutic potential for ovulation induction. Chem. Biochem. 10 (2002) 1023-1026
30. Wuller S., Wiesner B., Loffler A., Furkert J., Krause G., Hermosilla R., Schaefer M., Schulein R., Rosenthal W., and Oksche A. Pharmacochaperones post-translationally enhance cell surface expression by increasing conformational stability of wild-type and mutant vasopressin V2 receptors. J. Biol. Chem. 279 (2004) 47254-47263