Mechanism of Action and Structural Requirements of Constrained Peptide Inhibitors of RGS Proteins
dc.contributor.author | Roof, Rebecca A. | en_US |
dc.contributor.author | Jin, Yafei | en_US |
dc.contributor.author | Roman, David L. | en_US |
dc.contributor.author | Sunahara, Roger K. | en_US |
dc.contributor.author | Ishii, Masaru | en_US |
dc.contributor.author | Mosberg, Henry I. | en_US |
dc.contributor.author | Neubig, Richard R. | en_US |
dc.date.accessioned | 2010-04-01T15:42:33Z | |
dc.date.available | 2010-04-01T15:42:33Z | |
dc.date.issued | 2006-04 | en_US |
dc.identifier.citation | Roof, Rebecca A.; Jin, Yafei; Roman, David L.; Sunahara, Roger K.; Ishii, Masaru; Mosberg, Henry I.; Neubig, Richard R. (2006). "Mechanism of Action and Structural Requirements of Constrained Peptide Inhibitors of RGS Proteins." Chemical Biology & Drug Design 67(4): 266-274. <http://hdl.handle.net/2027.42/66199> | en_US |
dc.identifier.issn | 1747-0277 | en_US |
dc.identifier.issn | 1747-0285 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/66199 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=16629824&dopt=citation | en_US |
dc.format.extent | 374224 bytes | |
dc.format.extent | 3110 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.publisher | Blackwell Publishing Ltd | en_US |
dc.rights | 2006 The Authors Journal compilation 2006 Blackwell Munksgaard | en_US |
dc.subject.other | G Protein | en_US |
dc.subject.other | GTPase Activating Protein | en_US |
dc.subject.other | Structure Based Drug Design | en_US |
dc.title | Mechanism of Action and Structural Requirements of Constrained Peptide Inhibitors of RGS Proteins | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Pharmacy and Pharmacology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Department of Pharmacology, 1150 W. Medical Center Dr, University of Michigan, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationum | Department of Medicinal Chemistry, 428 Church Street, University of Michigan, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationother | Department of Pharmacology II, Graduate School of Medicine, Osaka University, 2-2 Yamada-oka, Suita, Osaka 565-0871, Japan | en_US |
dc.identifier.pmid | 16629824 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/66199/1/j.1747-0285.2006.00373.x.pdf | |
dc.identifier.doi | 10.1111/j.1747-0285.2006.00373.x | en_US |
dc.identifier.source | Chemical Biology & Drug Design | en_US |
dc.identifier.citedreference | Hepler J.R. ( 1999 ) Emerging roles for RGS proteins in cell signalling. Trends Pharmacol Sci ; 20 : 376 – 382. | en_US |
dc.identifier.citedreference | Berman D.M., Kozasa T., Gilman A.G. ( 1996 ) The GTPase-activating protein RGS4 stabilizes the transition state for nucleotide hydrolysis. J Biol Chem ; 271 : 27209 – 27212. | en_US |
dc.identifier.citedreference | Traynor J.R., Neubig R.R. ( 2005 ) Regulators of G protein signaling and drugs of abuse. Mol Interv ; 5 : 30 – 41. | en_US |
dc.identifier.citedreference | Wang Q., Liu M., Mullah B., Siderovski D.P., Neubig R.R. ( 2002 ) Receptor-selective effects of endogenous RGS3 and RGS5 to regulate mitogen-activated protein kinase activation in rat vascular smooth muscle cells. J Biol Chem ; 277 : 24949 – 24958. | en_US |
dc.identifier.citedreference | Xu X, Zeng W., Popov S., Berman D.M, Davignon I., Yu K., Yowe D., Offermann S., Muallem S., Wilkie T.M. ( 1999 ) RGS proteins determine signaling specificity of Gq-coupled receptors. J Biol Chem 274 : 3549 – 3556. | en_US |
dc.identifier.citedreference | Ghavami A., Hunt R.A., Olsen M.A., Zhang J., Smith D.L., Kalgaonkar S., Rahman Z., Young K.H. ( 2004 ) Differential effects of regulator of G protein signaling (RGS) proteins on serotonin 5-HT1A, 5-HT2A, and dopamine D2 receptor-mediated signaling and adenylyl cyclase activity. Cell Signal 16 : 711 – 721. | en_US |
dc.identifier.citedreference | Hague C., Bernstein L.S., Ramineni S., Chen Z., Minneman K.P., Hepler J.R. ( 2005 ) Selective inhibition of alpha1A-adrenergic receptor signaling by RGS2 association with the receptor third intracellular loop. J Biol Chem ; 280 : 27289 – 27295. | en_US |
dc.identifier.citedreference | Krumins A.M., Barker S.A., Huang C., Sunahara R.K., Yu K., Wilkie T.M., Gold S.J., Mumby S.M. ( 2004 ) Differentially regulated expression of endogenous RGS4 and RGS7. J Biol Chem 279 : 2593 – 2599. | en_US |
dc.identifier.citedreference | Wieland T., Mittmann C. ( 2003 ) Regulators of G-protein signalling: multifunctional proteins with impact on signalling in the cardiovascular system. Pharmacol Ther ; 97 : 95 – 115. | en_US |
dc.identifier.citedreference | Gold S.J., Ni Y.G., Dohlman H.G., Nestler E.J. ( 1997 ) Regulators of G-protein signaling (RGS) proteins: region-specific expression of nine subtypes in rat brain. J Neurosci ; 17 : 8024 – 8037. | en_US |
dc.identifier.citedreference | Neubig R.R., Siderovski D.P. ( 2002 ) Regulators of G-protein signalling as new central nervous system drug targets. Nat Rev Drug Discov ; 1 : 187 – 197. | en_US |
dc.identifier.citedreference | Zhong H., Neubig R.R. ( 2001 ) Regulator of G protein signaling proteins: novel multifunctional drug targets. J Pharmacol Exp Ther ; 297 : 837 – 845. | en_US |
dc.identifier.citedreference | Standaert D.G., Young A.B. ( 2001 ) Treatment of central nervous system degenerative disorders. In: Hardman J.G., Limbird L.E., editors. Goodman and Gilman's The Pharmacological Basis of Therapeutics. New York, USA : McGraw Hill ; p. 549 – 568. | en_US |
dc.identifier.citedreference | Usui I., Imamura T., Satoh H., Huang J., Babendure J.L., Hupfeld C.J., Olefsky J.M. ( 2004 ) GRK2 is an endogenous protein inhibitor of the insulin signaling pathway for glucose transtport stimulation. EMBO J 23 : 2821 – 2829. | en_US |
dc.identifier.citedreference | Riddle E.L., Schwartzman R.A., Bond M., Insel P.A. ( 2005 ) Multi-tasking RGS proteins in the heart: the next therapeutic target ? Circ Res ; 96 : 401 – 411. | en_US |
dc.identifier.citedreference | Druey K.M. ( 2003 ) Regulators of G protein signalling: potential targets for treatment of allergic inflammatory diseases such as asthma. Expert Opin Ther Targets ; 7 : 475 – 484. | en_US |
dc.identifier.citedreference | Berman D.M., Wang Y., Liu Z., Dong Q., Burke L.A., Liotta L.A., Fiser R., Wu X. ( 2004 ) A functional polymorphism in RGS6 modulates the risk of bladder cancer. Cancer Res 64 : 6820 – 6826. | en_US |
dc.identifier.citedreference | Hiol A., Davey P.C., Osterhout J.L., Waheed A.A., Fischer E.R., Chen C.K., Millgan G., Druey K.M., Jones T.L. ( 2003 ) Palmitoylation regulates regulators of G-protein signaling (RGS) 16 function. I. Mutation of amino-terminal cysteine residues on RGS16 prevents its targeting to lipid rafts and palmitoylation of an internal cysteine residue. J Biol Chem 278 : 19301 – 19308. | en_US |
dc.identifier.citedreference | Bernstein L.S., Grillo A.A., Loranger S.S., Linder M.E. ( 2000 ) RGS4 binds to membranes through an amphipathic alpha-helix. J Biol Chem ; 275 : 18520 – 18526. | en_US |
dc.identifier.citedreference | Bernstein L.S., Ramineni S., Hague C., Cladman W., Chidiac P., Levey A.I., Hepler J.R. ( 2004 ) RGS2 binds directly and selectively to the M1 muscarinic acetylcholine receptor third intracellular loop to modulate Gq/11alpha signaling. J Biol Chem 279 : 21248 – 56. | en_US |
dc.identifier.citedreference | Tesmer J.J., Berman D.M., Gilman A.G., Sprang S.R. ( 1997 ) Structure of RGS4 bound to AlF4-activated G(i alpha1): stabilization of the transition state for GTP hydrolysis. Cell ; 89 : 251 – 261. | en_US |
dc.identifier.citedreference | Jin Y., Zhong H., Omnaas J.R., Neubig R.R., Mosberg H.I. ( 2004 ) Structure-based design, synthesis, and pharmacologic evaluation of peptide RGS4 inhibitors. J Pept Res ; 63 : 141 – 146. | en_US |
dc.identifier.citedreference | Jameson E.E., Roof R.A., Whorton M.R., Mosberg H.I., Sunahara R.K., Neubig R.R., Kennedy R.T. ( 2005 ) Real-time detection of basal and stimulated G protein GTPase activity using fluorescent GTP analogues. J Biol Chem 280 : 7712 – 7719. | en_US |
dc.identifier.citedreference | Lan K.L., Zhong H., Nanamori M., Neubig R.R. ( 2000 ) Rapid kinetics of regulator of G-protein signaling (RGS)-mediated Galphai and Galphao deactivation. Galpha specificity of RGS4 AND RGS7. J Biol Chem ; 275 : 33497 – 33503. | en_US |
dc.identifier.citedreference | Lan K.L., Sarvazyan N.A., Taussig R., Mackenzie R.G., DiBello P.R., Dohlman H.G., Neubig R.R. ( 1998 ) Point mutation in Galphao and Galphail blocks interaction with regulator of G protein signaling proteins. J Biol Chem 273 : 12794 – 12797. | en_US |
dc.identifier.citedreference | Lee E., Linder M.E., Gilman A.G. ( 1994 ) Expression of G-protein alpha subunits in Escherichia coli. Methods Enzymol ; 237 : 146 – 164. | en_US |
dc.identifier.citedreference | Ishii M., Inanobe A., Fujita S., Makino Y., Hosoya Y., Kurachi Y. ( 2001 ) Ca(2+) elevation evoked by membrane depolarization regulates G protein cycle via RGS proteins in the heart. Circ Res ; 89 : 1045 – 1050. | en_US |
dc.identifier.citedreference | Doupnik C.A., Xu T., Shinaman J.M. ( 2001 ) Profile of RGS expression in single rat atrial myocytes. Biochim Biophys Acta ; 1522 : 97 – 107. | en_US |
dc.identifier.citedreference | Kardestuncer T., Wu H., Lim A.L., Neer E.J. ( 1998 ) Cardiac myocytes express mRNA for ten RGS proteins: changes in RGS mRNA expression in ventricular myocytes and cultured atria. FEBS Lett ; 438 : 285 – 288. | en_US |
dc.identifier.citedreference | Sowell M.O., Ye C., Ricupero D.A., Hansen S., Quinn S.J., Vassilev P.M., Mortensen R.M. ( 1997 ) Targeted inactivation of alphai2 or alphai3 disrupts activation of the cardiac muscarinic K+ channel, IK+Ach, in intact cells. Proc Natl Acad Sci U S A 94 : 7921 – 7926. | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
Files in this item
Remediation of Harmful Language
The University of Michigan Library aims to describe library materials in a way that respects the people and communities who create, use, and are represented in our collections. Report harmful or offensive language in catalog records, finding aids, or elsewhere in our collections anonymously through our metadata feedback form. More information at Remediation of Harmful Language.
Accessibility
If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.