During the last years the low-molecular non-peptidic regulators of the polypeptide hormones receptors containing LGR-repeats were identified. In the review the data on the structure and the molecular mechanisms of action of these regulators as agonists and antagonists of the luteinizing, follicle-stimulating and thyrotropin hormones are analyzed and systematized. The regulators interact with the serpentine domain of LGR-receptor and trigger the signaling cascades coupled with the receptor. Low-molecular agonists and antagonists of the LGR-receptors are considered as a new generation of the drugs that regulates the functional activity of sensitive to pituitary glycoprotein hormones signaling systems with high efficiency and selectivity. These regulators are more accessible compared to the hormones and can be use orally.
Shpakov A.O. et al. Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats // Biomeditsinskaya Khimiya. - 2010. - V. 56. -N 3. - P. 303-318.
Shpakov A.O. et al., "Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats." Biomeditsinskaya Khimiya 56.3 (2010): 303-318.
Shpakov, A. O., Shpakova, E. A. (2010). Low-molecular regulators of polypeptide hormones receptors containing LGR-repeats. Biomeditsinskaya Khimiya, 56(3), 303-318.
Puett D., Li Y., DeMars G., Angelova K., Fanelli F. (2007) Mol. Cell. Endocrinol., 260, 126-136. CrossRef Scholar google search
Van Koppen C.J., Zaman G.J.R., Timmers C.M., Kelder J., Mosselman S., Van de Lagemaat R., Smit M.J., Hanssen R.G.J.M. (2008) Naunyn-Schmiedeberg`s Arch. Pharmacol., DOI 10.1007/s00210-008-0318-3. CrossRef Scholar google search
Nishi S., Hsu S.Y., Zell K., Hsueh A.J. (2000) Endocrinology, 141, 4081-4090. Scholar google search
Karges B., Gidenne S., Aumas C., Haddad F., Kelly P.A., Milgrom E., De Roux N. (2005) Mol. Endocrinol., 19, 2086-2098. CrossRef Scholar google search
Jiang M., Lamminen T., Pakarinen P., Hellman J., Manna P., Herrera R.J., Huhtaniemi I. (2002) Mol. Hum. Reprod., 8, 201-212. CrossRef Scholar google search
Jaschke 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., Gershengorn M.C. (2006) J. Biol. Chem., 281, 9841-9844. CrossRef Scholar google search
Neumann S., Kleinau G., Costanzi S., Moore S., Jiang J.K., Raaka B.M., Thomas C.J., Krause G., Gershengorn M.C. (2008) Endocrinology, DOI: 10.1210/en.2008-0836. CrossRef Scholar google search
Moore S., Jaeschke H., Kleinau G., Neumann S., Costanzi S., Jiang J.K., Childress J., Raaka B.M., Colson A., Paschke R., Krause G., Thomas C.J., Gershengorn M.C. (2006) J. Med. Chem., 49, 3888-3896. CrossRef Scholar google search
Jorand-Lebrun C., Brondyk B., Lin J., Magar S., Murray R., Reddy A., Schroff H., Wands G., Weiser W., Xu Q., McKenna S., Brugger N. (2007) Bioorg. Med. Chem. Lett., 17, 2080-2085. CrossRef Scholar google search
Bouloux P.M., Handelsman D.J., Jockenhovel F., Nieschlag E., Rabinovich J., Frasa W.L., de Bie J.J., Woortman G., Itskovitz-Eldor J. (2001) Hum. Reprod., 16, 1592-1597. CrossRef Scholar google search
Maclean D., Holden F., Davis A.M., Scheuerman R.A., Yanofsky S., Holmes C.P., Fitch W.L., Tsutsui K., Barrett R.W., Gallop M.A. (2004) J. Comb. Chem., 6, 196-206. CrossRef Scholar google search
Yanofsky S.D., Shen E.S., Holden F., Whitehorn E., Aguilar B., Tate E., Holmes C.P., Scheuerman R., MacLean D., Wu M.M., Frail D.E., Lopez F.J., Winneker R., Arey B.J., Barrett R.W. (2006) J. Biol. Chem., 281, 13226-13233. CrossRef Scholar google search
Wrobel J., Jetter J., Kao W., Rogers J., Di L., Chi J., Perez M.C., Chen G.C., Shen E.S. (2006) Bioorg. Med. Chem., 14, 5729-5741. CrossRef Scholar google search
Van Straten N.C., van Berkel T.H., Demont D.R., Karstens W.J., Merkx R., Oosterom J., Schulz J., van Someren R.G., Timmers C.M., van Zandvoort P.M. (2005) J. Med. Chem., 48, 1697-1700. CrossRef Scholar google search
Smits G., Olatunbosun O., Delbaere A., Pierson R., Vassart G., Costagliola S. (2003) New Engl. J. Med., 349, 760-766. CrossRef Scholar google search
Vasseur C., Rodien P., Beau I., Desroches A., Gerard C., de Poncheville L., Chaplot S., Savagner F., Croue A., Mathieu E., Lahlou N., Descamps P., Misrahi M. (2003) New Engl. J. Med., 349, 753-759. CrossRef Scholar google search
Montanelli L., Delbaere A., Di Carlo C., Nappi C., Smits G., Vassart G., Costagliola S. (2004) J. Clin. Endocrinol. Metab., 89, 1255-1258. CrossRef Scholar google search
Montanelli L., Van Durme J.J., Smits G., Bonomi M., Rodien P., Devor E.J., Moffat-Wilson K., Pardo L., Vassart G., Costagliola S. (2004) Mol. Endocrinol., 18, 2061-2073. CrossRef Scholar google search
Parma J., Duprez L., Van Sande J., Cochaux P., Gervy C., Mockel J., Dumont J.E., Vassart G. (1993) Nature, 365, 649-651. CrossRef Scholar google search
Duprez L., Parma J., Van Sande J., Allegeier A., Leclere J., Schvartz C., Delisle M.J., Decoulx M., Orgiazzi J., Dumont J.E., Vassart G. (1994) Nature, 377, 396-401. Scholar google search
Shpakov A.O., Pertseva M.N. (2007) in: Signal Transduction Research Trends (N.O. Grachevsky ed.) Nova Science Publishers, Inc., NY, pp. 45-93. Scholar google search