Ligand-receptor engineering and its application towards the complementation of genetic disease and target identification

Current Topics in Medicinal Chemistry

Volumn 5, Issue 4, 2005, Pages 413-420

  Koh, John T ^a   Biggins, John B ^a  

^a UNIVERSITY OF DELAWARE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE A3 RECEPTOR; CALCITRIOL; CALCITRIOL DERIVATIVE; CELL NUCLEUS RECEPTOR; CHAPERONE; DIMETHYL SULFOXIDE; ESTROGEN RECEPTOR; G PROTEIN COUPLED RECEPTOR; GLYCEROL; HORMONE RECEPTOR; LIOTHYRONINE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PROTEIN KINASE; RETINOID X RECEPTOR; STEROID RECEPTOR; THYROID HORMONE; THYROID HORMONE DERIVATIVE; THYROID HORMONE RECEPTOR ALPHA; THYROID HORMONE RECEPTOR BETA; TIRATRICOL; TRIETHYLAMINE; VITAMIN D DERIVATIVE; VITAMIN D RECEPTOR;

BINDING AFFINITY; BIOMEDICAL ENGINEERING; CRYSTAL STRUCTURE; DIABETES INSIPIDUS; DRUG STRUCTURE; DRUG TARGETING; GENE IDENTIFICATION; GENE MUTATION; GENETIC COMPLEMENTATION; GENETIC DISORDER; HEART ARRHYTHMIA; HUMAN; PATHOGENESIS; PROTEIN FOLDING; PROTEIN FUNCTION; PROTEIN STABILITY; REVIEW; TACHYCARDIA; THYROID HORMONE RESISTANCE; VITAMIN D RESISTANT RICKETS;

ANIMALS; GENETIC COMPLEMENTATION TEST; GENETIC DISEASES, INBORN; HUMANS; MOLECULAR CHAPERONES; PROTEIN ENGINEERING; PROTEINS;

EID: 19944399429     PISSN: 15680266     EISSN: None     Source Type: Journal    
DOI: 10.2174/1568026053828420     Document Type: Review

References (91)

1. Bernier, V., Lacace, M., Bichet, D. G. and Bouvier, M. Pharmacological chaperones: Potential treatment for conformational diseases. Trends Endocrinol. Metab., 2004, 15, 222-228.
2. Cohen, F. E. and Kelly, J. W. Therapeutic approaches to protein-misfolding diseases. Nature, 2003, 426, 905-909.
3. Song, J. L. and Chaung, D. T. Natural osmolyte trimethylamine n-oxide corrects assembly defects of mutant branched -chain alpha ketoacid decarboxylases in maple syrup urein disease. J. Biol. Chem., 2001, 276, 40241-40246.
4. Sato, S., Ward, C., Krouse, M., Wine, J. and Kopito, R. Glycerol reverses the misfolding phenotype of the most common cystic fibrosis mutation. J. Biol. Chem., 1996, 271, 635-638.
5. Kim, B. E., Smith, K. and Petris, M. J. A copper treatable menkes disease mutation associated with defective trafficking of a functional menkes copper atpase. J. Med Genet., 2003, 40, 290-295.
6. Tamarappoo, B. K., Yang, B. X. and Verkman, A. S. Misfolding of mutant aquaporin-2 water channels in nephrogenic diabetes insipidus. J. Biol. Chem., 1999, 274, 34825-34831.
7. Loo, T. W. and Clarke, D. M. P-glycoprotein - associations between domains and between domains and molecular chaperones. J. Biol. Chem., 1995, 270, 21839-21844.
8. Morello, J. P., Salahpour, A., Laperriere, A., Bernier, V., Arthus, M. F., Lonergan, M., Petaja-Repo, U., Angers, S., Morin, D., Bichet, D. G. and Bouvier, M. Pharmacological chaperones rescue cell-surface expression and function of misfolded v2 vasopressin receptor mutants. J. Clin. Invest., 2000, 105, 887-895.
9. Bernier, V., Morello, J. P., Salahpour, A., Arthus, M. F., Laperriere, A., Lonergan, M., Bouvier, M. and Bichet, D. G. A pharmacological chaperone acting at the v2-vasopressin receptor offers a treatment for nephrogenic diabetes insipidus. FASEB J., 2002, 16, A142-A143.
10. Sawkar, A. R., Cheng, W. C., Beutler, E., Wong, C. H., Balch, W. E. and Kelly, J. W. Chemical chaperones increase the cellular activity of n370s beta-glucosidase: A therapeutic strategy for gaucher disease. Proc. Natl. Acad. Sci. USA 2002, 99, 15428-15433.
11. Noorwez, S. M., Kuksa, V., Imanishi, Y., Shu, L., Filipek, S., Palczewski, K. and Kauushal, S. Pharmacological chaperone-mediated folding and stabilization of the p23h-opsin mutant associated with autosomal dominant retinitis pigmentosa. J. Biol. Chem., 2003, 278, 14442-14450.
12. Soukup, G. A., Emilsson, G. A. M. and Breaker, R. R. Altering molecular recognition of rna aptamers by allosteric selection. J. Mol. Biol., 2000, 298, 623-632.
13. Vuyisich, M. and Beal, P. A. Controlling protein activity with ligand-regulated rna aptamers. Chemistry & Biology, 2002, 9, 907-913.
14. Buskirk, A. R., Landrigan, A. and Liu, D. R. Engineering a ligand-dependent rna transcriptional activator. Chemistry & Biology, 2004, 11, 1157-1163.
15. Hammarstrom, P., Wiseman, R. L., Powers, E. T. and Kelly, J. W. Prevention of transtyretin amyloid disease by changing protein misfolding energetics. Science, 2003, 299, 713-716.
16. Foster, B. A., Coffey, H. A., Morin, M. J. and Rastinejad, F. Pharmacological rescue of mutant p53 conformation and function. Science, 1999, 286, 2507-10.
17. Bullock, A. N. and Fersht, A. R. Rescueing the function of mutant p53. Nature Rev. Cancer, 2001, 1, 68-76.
18. Latchman, D. S. Transcription-factor mutations and disease. N. Engl. J. Med., 1996, 334, 28-33.
19. Tenbaum, S. and Baniahmad, A. Nuclear receptors: Structure, function and involvement in disease. Int. J. Biochem. Cell Biol., 1997, 290, 1325-41.
20. Ye, H. F., O'Reilly, K. E. and Koh, J. T. A subtype-selective thyromimetic designed to bind a mutant thyroid hormone receptor implicated in resistance to thyroid hormone. J. Am. Chem. Soc., 2001, 123, 1521-1522.
21. Takeda, K., Balzano, S., Sakurai, A., DeGroot, L. J. and Refetoff, S. Screening of nineteen unrelated families with generalized resistance to thyroid hormone for known point mutations in the thyroid hormone receptor beta gene and the detection of a new mutation. J. Clin. Invest., 1991, 87, 496-502.
22. Chatterjee, V. K. K., Nagaya, T., Madison, L. D., Datta, S., Rentoumis, M. and Jameson, J. L. Thyroid hormone resistance syndrome. J. Clin. Invest., 1991, 87, 1977-1984.
23. Refetoff, S., Weiss, R. E. and Usala, S. J. The syndromes of resistance to thyroid hormone. Endocr. Rev., 1993, 14, 348-99.
24. Kopp, P., Kitajima, K. and Jameson, J. L. Syndrome of resistance to thyroid hormone: Insights into thyroid hormone action. Proc. Soc. Exp. Biol. Med., 1996, 211, 49-61.
25. Yen, P. M. Molecular basis of resistance to thyroid hormone. Trends Endocrinol. Metab., 2003, 14, 327-333.
26. Huber, B. R., Desclozeaux, M., West, B. L., Cunha-Lima, S. T., Nguyen, H. T., Baxter, J. D., Ingraham, H. A. and Fletterick, R. J. Thyroid hormone receptor-beta mutations conferring hormone resistance and reduced corepressor release exhibit decreased stability in the n-terminal ligand-binding domain. Mol. Endocrinol., 2003, 17, 107-116.
27. Clifton-Bligh, R. J., de Zegher, F., Wagner, R. L., Collingwood, T. N., Francois, I., Van Helvoirt, M., Fletterick, R. J. and Chatterjee, V. K. A novel TR beta mutation (R383H) in resistance to thyroid hormone syndrome predominantly impairs corepressor release and negative transcriptional regulation. Mol. Endocrinol., 1998, 12, 609-21.
28. Huber, B. R., Sandler, B., West, B. L., Lima, S. T. C., Nguyen, H. T., Apriletti, J. W., Baxter, J. D. and Fletterick, R. J. Two resistance to thyroid hormone mutants with impaired hormone binding. Mol. Endocrinol., 2003, 17, 643-652.
29. Polikar, R., Feld, G. K., Dittrich, H. C., Smith, J. and Nicod, P. Effect of thyroid replacement therapy on the frequency of benign atrial and ventricular arrhythmias. J. Am. Coll. Cardiol., 1989, 14, 999-1002.
30. Kahaly, G. J., Matthews, C, H., Mohr-Kahaly, S., Richards, C. A. and Chatterjee, V. K. K. Cardiac involvement in thyroid hormone resistance. J. Clin. Endocrinol. Metab., 2002, 87, 204-212.
31. Radetti, G., Persani, L., Molinaro, G., Mannavola, D., Cortelazzi, D., Chatterjee, V. K. K. and BeckPeccoz, P. Clinical and hormonal outcome after two years of triiodothyroacetic acid treatment in a child with thyroid hormone resistance. Thyroid, 1997, 7, 775-778.
32. Grover, G. J., Egan, D. M., Sleph, P. G., Beehler, B. C., Chiellini, G., Nguyen, N. H., Baxter, J. D. and Scanlan, T. S. Effects of the thyroid hormone receptor agonist gc-1 on metabolic rate and cholesterol in rats and primates: Selective actions relative to 3,5,3′-triiodo-l-thyronine. Endocrinology, 2004, 145, 1656-1661.
33. Yen, P. M. and Cheng, S. Y. Germline and somatic thyroid hormone receptor mutations in man. J. Endocrinol. Investig., 2003, 26, 780-787.
34. Takeda, T., Suzuki, S., Liu, R. T. and DeGroot, L. J. Triiodothyroacetic acid has unique potential for therapy of resistance to thyroid hormone. J. Clin. Endocrinol. Metab. 1995, 80, 2033-40.
35. Asteria, C., Rajanayagam, O., Collingwood, T. N., Persani, L., Romoli, R., Mannavola, D., Zamperini, P., Buzi, F., Ciralli, F., Chatterjee, V. K. K. and Beck-Peccoz, P. Prenatal diagnosis of thyroid hormone resistance. J. Clin. Endocrinol. Metab., 1999, 84, 405-410.
36. Messier, N., Laflamme, L., Hamann, G. and Langlois, M. F. effect of triac on resistance to thyroid hormone receptor mutants: Potential basis for therapy. Mol. Cell. Endocrinol., 2001, 174, 59-69.
37. Messier, N. and Langlois, M. F. Triac regulation of transcription is T-3 receptor isoform- and response element-specific. Mol. Cell. Endocrinol., 2000, 165, 57-66.
38. Shi, Y., Ye, H., Link, K. H., Putnam, M. C., Hubner, I., Dowdel, S. and Koh, J. T. Mutant-selective thyromimetics for the chemical rescue of thyroid hormone mutants associated with resistance to thyroid hormone (RTH). Biochemistry, 2005, 44, 4612-4626.
39. Chiellini, G., Apriletti, J. W., al Yoshihara, H., Baxter, J. D., Ribeiro, R. C. and Scanlan, T. S. A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor. Chem. Biol., 1998, 5, 299-306.
40. Malloy, P. J. and Feldman, D. Vitamin d resistance. Am. J. Med., 1999, 106, 355-70.
41. Malloy, P. J., Pike, J. W. and Feldman, D. The vitamin d receptor and the syndrome of hereditary 1,25- dihydroxyvitamin d-resistant rickets. Endocr. Rev., 1999, 20, 156-88.
42. Bouillon, R., Okamura, W. H. and Norman, A. W. Structure-function relationships in the vitamin d endocrine system. Endocr. Rev., 1995, 16 200-57.
43. Whitfield, G. K., Selznick, S. H., Haussler, C. A., Hsieh, J. C., Galligan, M. A., Jurutka, P. W., Thompson, P. D., Lee, S. M., Zerwekh, J. E. and Haussler, M. R. Vitamin d receptors from patients with resistance to 1,25-dihydroxyvitamin d-3: Point mutations confer reduced transactivation in response to ligand and impaired interaction with the retinoid x receptor heterodimeric partner. Mol. Endocrinol., 1996, 10, 1617-1631.
44. Kristjansson, K., Rut, A. R., Hewison, M., O'Riordan, J. L. and Hughes, M. R. Two mutations in the hormone binding domain of the vitamin d receptor cause tissue resistance to 1,25 dihydroxyvitamin d3. J. Clin. Invest. 1993, 92, 12-6.
45. Malloy, P. J., Eccleshall, T. R., Gross, C., VanMaldergem, L., Bouillon, R. and Feldman, D. Hereditary vitamin d resistant rickets caused by a novel mutation in the vitamin d receptor that results in decreased affinity for hormone and cellular hyporesponsiveness. J. Clin. Investig., 1997, 99, 297-304.
46. Farach-Carson, M. C. and Ridall, A. L. Dual 1,25-dihydroxy-vitamin d3 signal response pathways in osteoblasts: Cross-talk between genomic and membrane-initiated pathways. Am. J. Kidney Dis., 1998, 31, 729-42.
47. Gardezi, S. A., Nguyen, C., Malloy, P. J., Posner, G. H., Feldman, D. and Peleg, S. A rationale for treatment of hereditary vitamin d-resistant rickets with analogs of 1 alpha,25-dihydroxyvitamin d-3. J. Biol. Chem., 2001, 276, 29148-29156.
48. Peleg, S., Nguyen, C., Woodard, B. T., Lee, J. K. and Posner, G. H. Differential use of transcription activation function 2 domain of the vitamin d receptor by 1,25-dihydroxyvitamin d-3 and its a ring-modified analogs. Mol. Endocrinol., 1998, 12, 525-535.
49. Swann, S. L., Bergh, J., Mary C. Farach-Carson, Ocasio, C. A. and Koh, J. T. Structure based design of selective agonists for a rickets-associated mutant of the vitamin d receptor. J. Am. Chem. Soc., 2002, 124, 13795-13805.
50. Swann, S. L., Bergh, J. J., Farach-Carson, M. C. and Koh, J. T. (2002) Rational design of vitamin d3 analogs which selectively restore activity to a vitamin d receptor mutant associated with rickets. Org. Lett., 2002, 4, 3863-3866.
51. Barroso, I., Gurnell, M., Crowley, V. E., Agostini, M., Schwabe, J. W., Soos, M. A., Maslen, G. L., Williams, T. D., Lewis, H., Schafer, A. J., Chatterjee, V. K. and O'Rahilly, S. Dominant negative mutations in human PPAR gamma associated with severe insulin resistance, diabetes mellitus and hypertension [see comments]. J. Am. Chem. Soc., 1999, 402, 880-3.
52. Agostini, M., Gurnell, M., Savage, D. B., Wood, E. M., Smith, A. G., Rajanayagam, O., Garnes, K. T., Levinson, S. H., Xu, H. E., Schwabe, J. W. R., Willson, T. M., O'Rahilly, S. and Chatterjee, V. K. Tyrosine agonists reverse the molecular defects associated with dominant-negative mutations in human peroxisome proliferator-activated receptor gamma. Endocrinology, 2004, 145, 1527-1538.
53. Koh, J. T. Engineering selectivity and discrimination into ligand-receptor interfaces. Chemistry & Biology, 2002, 9, 17-23.
54. Bishop, A. C. and Shokat, K. M. Acquisition of inhibitor-sensitive protein kinases through protein design. Pharmacol. Ther., 1999, 82, 337-46.
55. Bishop, A. C., Kung, C. Y., Shah, K., Witucki, L., Shokat, K. M. and Liu, Y. Generation of monospecific nanomolar tyrosine kinase inhibitors via a chemical genetic approach. J. Am. Chem. Soc., 1999, 121, 627-631.
56. Bishop, A., Buzko, O., Heyeck-Dumas, S., Jung, I., Kraybill, B., Liu, Y., Shah, K., Ulrich, S., Witucki, L., Yang, F., Zhang, C. and Shokat, K. M. Unnatural ligands for engineered proteins: New tools for chemical genetics. Annu. Rev. Biophys. Biomol. Struct., 2000, 29, 577-606.
57. Bishop, A. C., Ubersax, J. A., Petsch, D. T., Matheos, D. P., Gray, N. S., Blethrow, J., Shimizu, E., Tsien, J. Z., Schultz, P. G., Rose, M. D., Wood, J. L., Morgan, D. O. and Shokat, K. M. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature, 2000, 407, 395-401.
58. Ulrich, S. M., Buzko, O., Shah, K. and Shokat, K. M. Towards the engineering of an orthogonal protein kinase/nucleotide triphosphate pair. Tetrahedron, 2000, 56, 9495-9502.
59. Maly, D.J.; Allen, J. A.; Shokat, K. M. A mechanism-based cross-linker for the identification of kinase-substrate pairs. J. Am. Chem. Soc., 2004, 126, 9160-9161.
60. Liu, Y., Shah, K., Yang, F., Witucki, L. and Shokat, K. M. Engineering src family protein kinases with unnatural nucleotide specificity. Chem. Biol., 1998, 5, 91-101.
61. Liu, Y., Shah, K., Yang, F., Witucki, L. and Shokat, K. M. A molecular gate which controls unnatural atp analogue recognition by the tyrosine kinase v-src. Bioorg. Med. Chem., 1998, 6, 1219-1226.
62. Gillespie, P. G., Gillespie, S. K., Mercer, J. A,, Shah, K. and Shokat, K. M. Engineering of the myosin-ibeta nucleotide-binding pocket to create selective sensitivity to N(6)-modified ADP analogs. J. Biol. Chem., 1999, 274, 31373-81.
63. Liu, Y., Witucki, L. A., Shah, K., Bishop, A. C. and Shokat, K. M. Src-abl tyrosine kinase chimeras: Replacement of the adenine binding pocket of c-abl with v-src to swap nucleotide and inhibitor specificities. Biochemistry, 2000, 39, 14400-14408.
64. Weiss, E. L., Bishop, A., Shokat, K. and Drubin, D. G. Chemical genetic analysis of the budding yeast p21-activated kinase cla4p. Mol. Biol. Cell, 2000, 11, 350a-350a.
65. Carroll, A. S., Bishop, A. C., DeRisi, J. L., Shokat, K. M. and O'Shea, E. K. Chemical inhibition of the pho85 cyclin-dependent kinase reveals a role in the environmental stress response. Proc. Nat. Acad. Sci. USA, 2001, 98, 12578-12583.
66. Alaimo, P. J., Knight, Z. A. and Shokat, K. M. Using chemical genetics to obtain allele-specific inhibitors of phosphatidylinositol 3-kinase (pi 3-k). Mol. Biol. Cell, 2002, 13, 152a-152a.
67. Paulson, J. L., Morgan, D. O. and Shokat, K. M. Signaling by the mitotic exit network kinase cdc15. Mol. Biol. Cell, 2002, 13, 156a-156a.
68. Weiss, E. L., Kurischko, C., Zhang, C., Shokat, K., Drubin, D. G. and Luca, F. C. The saccharomyces cerevisiae mob2p-cbk1p kinase complex promotes polarized growth and acts with the mitotic exit network to facilitate daughter cell-specific localization of ace2p transcription factor. J. Cell Biol., 2002, 158, 885-900.
69. Benjamin, K. R., Zhang, C., Shokat, K. M. and Herskowitz, I. Control of landmark events in meiosis by the cdk cdc28 and the meiosis-specific kinase ime2. Genes & Development, 2003, 17, 1524-1539.
70. Eblen, S. T., Kumar. N. V., Shah, K., Henderson, M. J., Watts, C. K. W., Shokat, K. M. and Weber, M. J. Identification of novel erk2 substrates through use of an engineered kinase and ATP analogs. J. Biol. Chemistry, 2003, 278, 14926-14935.
71. Ubersax, J. A., Woodbury, E. L., Quang, P. N., Paraz, M., Blethrow, J. D., Shah, K., Shokat, K. M. and Morgan, D. O. Targets of the cyclin-dependent kinase cdk1. Nature, 2003, 425, 859-864.
72. Sreenivasan, A., Bishop, A. C., Shokat, K. M. and Kellogg, D. R. Specific inhibition of elm1 kinase activity reveals functions required for early G(1) events. Mol. Cell. Biol., 2003, 23, 6327-6337.
73. Hindley, A. D., Park, S., Wang, L. L., Shah, K., Wang, Y. L., Hu, X. C., Shokat, K. M., Kolch, W., Sedivy, J. M. and Yeung, K. C. Engineering the serine/threonine protein kinase raf-1 to utilise an orthogonal analogue of atp substituted at the N-6 position. FEBS Lett., 2004, 556, 26-34.
74. Wan, L. H., de los Santos, T., Zhang, C., Shokat, K. and Hollingsworth, N. M. Mek1 kinase activity functions downstream of red1 in the regulation of meiotic double strand break repair in budding yeast. Mol. Biol. Cell, 2004, 15, 11-23.
75. Bishop, A. C., Shah, K., Liu, Y., Witucki, L., Kung, C. Y. and Shokat, K. M. Design of allele-specific inhibitors to probe protein kinase signaling. Curr. Biol., 1998, 8, 257-266.
76. Lin, Q., Jiang, F. Y., Schultz, P. G. and Gray, N. S. Design of allele-specific protein methyltransferase inhibitors. J. Am. Chem. Soc., 2001, 123, 11608-11613.
77. Jacobson, K. A., Gao, Z. G., Chen, A. S., Barak, D., Kim, S. A., Lee, K., Link, A., Van Rompaey, P., van Calenbergh, S. and Liang, B. T. Neoceptor concept based on molecular complementarity in gpcrs: A mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides. J. Med. Chem., 2001, 44, 4125-4136.
78. Kim, S. K.; Gao, Z. G.; Van Rompaey, P.; Gross, A. S.; Chen, A.; Van Calenbergh, S.; Jacobson, K. A. Modeling the adenosine receptors: Comparison of the binding domains of A(2A) agonists and antagonists. J. Med. Chem., 2003, 46, 4847-4859.
79. Muthyala, R. S., Sheng, S. B., Carlson, K. E., Katzenellenbogen, B. S. and Katzenellenbogen, J. A. Bridged bicyclic cores containing a 1,1-diarylethylene motif are high-affinity subtype-selective ligands for the estrogen receptor. J. Med. Chem., 2003, 46, 1589-1602.
80. Sun, J.; Baudry, J.; Katzenellenbogen, J. A.; Katzenellenbogen, B. S. Molecular basis for the subtype discrimination of the estrogen receptor-beta-selective ligand diarylpropionitrile. Mol. Endocrinol., 2003, 17, 247-258.
81. Milburn, M. V. and Wisely, G. B. Activation and function of an orphan nuclear receptor - crystal structure of the ppar-gamma ligand binding domain. FASEB J., 1997, 11, P29.
82. Falkenstein, E., Tillmann, H. C., Christ, M., Feuring, M. and Wehling, M. Multiple actions of steroid hormones - a focus on rapid, nongenomic effects. Pharmacol. Rev., 2000, 52, 513-555.
83. Pawlikowski, M., Winczyk, K. and Jaranowska, M. Immunohistochemical demonstration of nitric oxide synthase (nos) in the normal rat pituitary gland, estrogen-induced rat pituitary tumor and human pituitary adenomas. Folia Histochemica Et Cytobiologica, 2003, 41, 87-90.
84. Geary, G. G., Krause, D. N. and Duckles, S. P. Estrogen reduces mouse cerebral artery tone through endothelial nos- and cyclooxygenase-dependent mechanisms. Am. J. Physiol.-Heart and Circul. Physiol., 2000, 279, H511-H519.
85. Qiu, J., Bosch, M. A., Tobias, S. C., Grandy, D. K., Scanlan, T. S., Ronnekleiv, O. K. and Kelly, M. J. Rapid signaling of estrogen in hypothalamic neurons involves a novel g-protein-coupled estrogen receptor that activates protein kinase c. J. Neurosci., 2003, 23, 9529-9540.
86. Losel, R. and Wehling, M. Nongenomic actions of steroid hormones. Nat. Rev. Mol. Cell Biol., 2003, 4, 46-56.
87. Tedesco, R., Thomas, J. A., Katzenellenbogen, B. S. and Katzenellenbogen, J. A. The estrogen receptor: A structure-based approach to the design of new specific hormone-receptor combinations. Chem. Biol., 2001, 8, 277-87.
88. Shi, Y. and Koh, J. T. Selective regulation of gene expression by an orthogonal estrogen receptor-ligand pair created by polar-group exchange. Chem. Biol., 2001, 8, 501-10.
89. Shi, Y. H. and Koh, J. T. Functionally orthogonal ligand-receptor pairs for the selective regulation of gene expression generated by manipulation of charged residues at the ligand-receptor interface of er alpha and er beta. J. Am. Chem. Soc., 2002, 124, 6921-6928.
90. Koh, J. T., Putnam, M., Tomic-Canic, M. and McDaniel, C. M. Selective regulation of gene expression using rationally-modified retinoic acid receptors. J. Am. Chem. Soc., 1999, 121, 1984-1985.
91. Doyle, D. F., Braasch, D. A., Jackson, L. K., Weiss, H. E., Boelim, M. F., Mangelsdorf, D. J. and Corey, D. R. Engineering orthogonal ligand-receptor pairs from "near drugs". J. Am. Chem. Soc., 2001, 123, 11367-11371.