Spanning binding sites on allosteric proteins with polymer-linked ligand dimers

Nature

Volumn 395, Issue 6703, 1998, Pages 710-713

  Kramer, Richard H ^a   Karpen, Jeffrey W ^b  

^a UNIVERSITY OF MIAMI MILLER SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF COLORADO SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC GMP; CYCLIC GMP DEPENDENT PROTEIN KINASE; DIMER; LIGAND; POLYMER;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; BINDING SITE; DIMERIZATION; DRUG DESIGN; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN STRUCTURE;

ALLOSTERIC SITE; ANIMALS; CATTLE; CYCLIC GMP; CYCLIC GMP-DEPENDENT PROTEIN KINASES; DIMERIZATION; DRUG DESIGN; ION CHANNELS; LIGANDS; NEURONS; POLYETHYLENE GLYCOLS; POLYMERS; RATS; RECOMBINANT PROTEINS; RODS (RETINA); XENOPUS;

EID: 0032531947     PISSN: 00280836     EISSN: None     Source Type: Journal    
DOI: 10.1038/27227     Document Type: Article

References (28)

1. Gallop, M. A., Barrett, R. W., Dower, W. J., Fodor, S. P. & Gordon, E. M. Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries. J. Med. Chem. 37, 1233-1251 (1994).
2. Finn, J. T., Grunwald, M. E. & Yau, K.-W. Cyclic nucleotide-gated ion channels: an extended family with diverse functions. Annu. Rev. Physiol. 58, 395-426 (1996).
3. Zagotta, W. N. & Siegelbaum, S. A. Structure and function of cyclic nucleotide-gated channels. Annu. Rev. Neurosci. 19, 235-263 (1996).
4. Francis, S. H. & Corbin, J. D. Progress in understanding the mechanism and function of cyclic GMP-dependent protein kinase. Adv. Pharm. 26, 115-170 (1994).
5. Taylor, S.S., Buechler, J. A. & Yonemoto, W. cAMP-dependent protein kinase: framework for a diverse family of regulatory enzymes. Annu. Rev. Biochem. 59, 971-1005 (1990).
6. Liu, D. T., Tibbs, G. R. & Siegelbaum, S. A. Subunit stoichiometry of cyclic nucleotide-gated channels and effects of subunit order on channel function. Neuron 16, 983-990 (1996).
7. Shabb, J. B. & Corbin, J. D. Cyclic nucleotide-binding domains in proteins having diverse functions. J. Biol. Chem. 267, 5723-5726 (1992).
8. Botelho, L. H., Rothermael, J. D., Coombs, R. V. & Jastorff, B. cAMP analog antagonists of cAMP action. Meth. Enzymol. 159, 159-172 (1988).
9. Butt, E., Van Bemmelen, M., Fischer, L., Walter, U. & Jastorff, B. Inhibition of cGMP-dependent protein kinase by (Rp)-guanosine 3′,5′-monophosphorothioates. FEBS Lett. 263, 47-50 (1990).
10. Butt, E., Eigenthaler, M. & Genieser, H. G. (Rp)-8-pCPT-cGMPS, a novel cGMP-dependent protein kinase inhibitor. Eur. J. Pharmacol. 269, 265-268 (1994).
11. Kramer, R. H. & Tibbs, G. R. Antagonists of cyclic nucleotide-gated channels and molecular mapping of their site of action. J. Neurosci. 16, 1285-1293 (1996).
12. Wei, J.-Y., Cohen, E. D., Yan, Y.-Y., Genieser, H.-G. & Barnstable, C. J. Identification of competitive antagonists of the rod photoreceptor cGMP-gated cation channel: beta-phenyl-1,N2-etheno-substituted cGMP analogues as probes of the cGMP-binding site. Biochemistry 35, 16815-16823 (1996).
13. Brown, R. L., Bert, R. J., Evans, F. E. & Karpen, J. W. Activation of retinal rod cGMP-gated channels: what makes for an effective 8-substituted derivative of cGMP? Biochemistry 32, 10089-10095 (1993).
14. Zimmerman, A. L., Yamanaka, G., Eckstein, F., Baylor, D. A. & Stryer, L. Interaction of hydrolysis-resistant analogs of cyclic GMP with the phosphodiesterase and light-sensitive channel of retinal rod outer segments. Proc. Natl Acad. Sci. USA 82, 8813-8817 (1985).
15. Cartetta, A., Cavaggioni, A. & Sorbi, R. T. Binding stoichiometry of a fluorescent cGMP analogue to membranes of retinal rod outer segments. Eur. J. Biochem. 153, 49-53 (1985).
16. Koch, K.-W. & Kaupp, U. B. Cyclic GMP directly regulates a cation conductance in membranes of bovine rods by a cooperative mechanism. J. Biol. Chem. 260, 6788-6800 (1985).
17. Tanaka, J. C., Eccleston, J. F. & Furman, R. E. Photoreceptor channel activation by nucleotide derivatives. Biochemistry 28, 2776-2784 (1989).
18. Knoll, D. & Hermans, J. Polymer-protein interactions. Comparison of experiment and excluded volume theory. J. Biol. Chem. 258, 5710-5715 (1983).
19. Florey, P. J. Principles of Polymer Chemistry (Cornell Univ. Press, Ithaca, New York, 1953).
20. Dhallan, R. S., Yau, K.-W., Schrader, K. A. & Reed, R. R. Primary structure and functional expression of a cyclic-nucleotide-activated channel from olfactory neurons. Nature 347, 184-187 (1990).
21. Kaupp, U. B. et al. Primary structure and functional expression from complementary DNA of the rod photoreceptor cyclic GMP-gated channel. Nature 342, 762-766 (1989).
22. Goulding, E. H., Tibbs, G. R., Liu, D. & Siegelbaum, S. A. Role of H5 domain in determining pore diameter and ion permeation through cyclic nucleotide-gated channels. Nature 364, 61-64 (1993).
23. Su, Y. et al. Regulatory subunit of protein kinase A: structure of deletion mutant with cAMP binding domains. Science 269, 807-813 (1995).
24. Chen, T.-Y. et al. A new subunit of the cyclic nucleotide-gated cation channel in retinal rods. Nature 362, 764-767 (1993).
25. Liman, E. R. & Buck, L. B. A second subunit of the olfactory cyclic nucleotide-gated channel confers high sensitivity to cAMP. Neuron 13, 611-621 (1994).
26. Bradley, J., Li, J., Davidson, N., Lester, H. A. & Zinn, K. Heteromeric olfactory cyclic nucleotide-gated channels: a subunit that confers increased sensitivity to cAMP. Proc. Natl Acad. Sci. USA 91, 8890-8894 (1994).
27. Körschen, H. G. et al. A 240 kDa protein represents the complete beta subunit of the cyclic nucleotide-gated channel from rod photoreceptor. Neuron 15, 627-636 (1995).
28. Sekhar, K. R. et al. Relaxation of pig coronary arteries by new and potent cGMP analogs that selectively activate type I alpha, compared with type I beta, cGMP-dependent protein kinase. Mol. Pharmacol. 42, 103-108 (1992).