Fragment-based drug discovery: Concept and aim

Yakugaku Zasshi

Volumn 130, Issue 3, 2010, Pages 315-323

  Tanaka, Daisuke ^a  

^a DAINIPPON SUMITOMO PHARMA CO LTD   (Japan)

Author keywords

Chemical space; Fragment screening; Fragment based drug discovery; Lead likeness; Ligand efficiency; Rule of three

Indexed keywords

LEAD; MITOGEN ACTIVATED PROTEIN KINASE P38; UROKINASE;

BIOAVAILABILITY; BIOLOGICAL ACTIVITY; DRUG SCREENING; FRAGMENT BASED DRUG DISCOVERY; HIGH THROUGHPUT SCREENING; INTERMETHOD COMPARISON; PRACTICE GUIDELINE; REVIEW;

DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL;

EID: 77649260308     PISSN: 00316903     EISSN: 13475231     Source Type: Journal    
DOI: 10.1248/yakushi.130.315     Document Type: Review

References (19)

1. "Fragment-based Approaches in Drug Discovery," ed. by Jahnke W., Erlanson D. A., Wiley-VCH, Weinheim, 2006.
2. de Kloe G. E., Bailey D., Leurs R., de Esch I. J. P., Drug Discov. Today, 14, 630-646 (2009).
3. Bohacek R. S., McMartin C., Guida W. C., Med. Res. Rev., 16, 3-50 (1996).
4. Hann M. M., Oprea T. I., Curr. Opin. Chem. Biol., 8, 255-263 (2004).
5. Hann M. M., Leach A. R., Harper G., J. Chem. Inf. Comput. Sci., 41, 856-864 (2001).
6. Lipinski C. A., Lombardo F., Dominy B. W., Feeny P. J., Adv. Drug Deliv. Rev., 46, 3-26 (2001).
7. Leeson P. D., Springthorpe B., Nature Rev. Drug Discov., 6, 881-890 (2007).
8. Congreve M., Carr R., Murry C., Jhoti H., Drug Discov. Today, 8, 876-877 (2003).
9. Reynolds C. H., Tounge B. A., Bembenek S. D., J. Med. Chem., 51, 2432-2438 (2008).
10. Coan K. E. D., Shoichet B. K., J. Am. Chem. Soc., 130, 9606-9612 (2008).
11. Wyatt P. G., Woodhead A. J., Berdini V., Boulstridge J. A., Carr M. G., Cross D. M., Davis D. J., Devine L. A., Early T. R., Feltell R. E., Lewis E. J., McMenamin R. L., Navarro E. F., O'Brien M. A., O'Reilly M., Reule M., Saxty G., Seavers L. C. A., Smith D.-M., Squires M. S., Trewartha G., Walker M. T., Woolford A. J.-A., J. Med. Chem., 51, 4986-4999 (2008).
12. Hopkins A. L., Groom C. R., Alex A., Drug Discov. Today, 9, 430-431 (2004).
13. Abad-Zapatero C., Metz J. T., Drug Discov. Today, 10, 464-469 (2005).
14. Orita M., Ohno K., Niimi T., Drug Discov. Today, 14, 321-328 (2009).
15. Hajduk P. J., Sheppard G., Nettesheim D. G., Olejniczak E. T., Shuker S. B., Meadows R. P., Steinman D. H., Carrera Jr. G. M., Marcotte P. A., Severin J., Walter K., Smith H., Gubbins E., Simmer R., Holzman T. F., Mor gan D. W., Davidsen S. K., Summers J. B., Fesik S. W., J. Am. Chem. Soc., 119, 5818-5827 (1997).
16. unpublished data.
17. Nienaber V. L., Richardson P. L., Klighofer V., Bouska J. J., Giranda V. L., Greer J., Nat. Biotechnol., 18, 1105-1108 (2000).
18. Fejzo J., Lepre C. A., Peng J. W., Bemis G. W., Ajay, Murcko M. A., Moore J. M., Chem. Biol., 6, 755-769 (1999).
19. Howard N., Abell C., Blakemore W., Chessari G., Congreve M., Howard S., Jhoti H., Murray C. W., Seavers L. C. A., van Montfort R. L. M., J. Med. Chem., 49, 1346-1355 (2006).