Structural basis for the inhibitor recognition of human Lyn kinase domain

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 23, 2009, Pages 6557-6560

  Miyano, Nao ^a   Kinoshita, Takayoshi ^a   Nakai, Ryoko ^b   Kirii, Yasuyuki ^b   Yokota, Koichi ^b   Tada, Toshiji ^a  

^a Osaka Prefecture University   (Japan)

^b 1 5 5 Minatojima Minamimachi   (Japan)

Author keywords

Inhibitor; Kinase; Lyn; Src family; Structure

Indexed keywords

ADENOSINE TRIPHOSPHATE; PROTEIN KINASE LYN; STAUROSPORINE;

ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; ENZYME ACTIVITY; HEMATOPOIETIC SYSTEM; HEMATOPOIETIC TISSUE; IMMUNE SYSTEM; INTROSPECTION; MOLECULAR RECOGNITION; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN STRUCTURE; SIGNAL TRANSDUCTION; TUMOR;

BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; SRC-FAMILY KINASES; STAUROSPORINE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 71849110330     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.038     Document Type: Article

References (24)

1. Lowell C.A. Mol. Immunol. 41 (2004) 631
2. Thomas S.M., and Brugge J.S. Annu. Rev. Cell Dev. Biol. 13 (1997) 513
3. Okutani D., Lodyga M., Han B., and Liu M. Am. J. Physiol. Lung Cell Mol. Physiol. 291 (2006) 129
4. Summy J.M., and Gallick G.E. Cancer Metastasis Rev. 22 (2003) 337
5. Chan V.W.F., Meng F., Soriano P., DeFrance A.L., and Lowell C.A. Immunity 7 (1997) 69-81
6. Janas M.L., Hodgkin P., Hibbs M., and Tarlinton D. J. Immunol. 163 (1999) 4192
7. Harder K.W., Parsons L.M., Armes J., Evans N., Kountouri N., Clark R., Quilici C., Grail D., Hodgson G.S., Dunn A.R., and Hibbs M.L. Immunity 15 (2001) 603
8. Hibbs M.L., Harder K.W., Armes J., Kountouri N., Quilici C., Casagranda F., Dunn A.R., and Tarlinton D.M. J. Exp. Med. 196 (2002) 1593
9. Xiao W., Nishimoto H., Hong H., Kitaura J., Nunomura S., Maeda-Yamamoto M., kawakami Y., Lowell C.A., Ra C., and Kawakami T. J. Immunol. 175 (2005) 6885
10. Goldenberg-Furmanov M., Stein I., Pikarsky E., Rubin H., Kasem S., Wygoda M., Weinstein I., Reuveni H., and Ben-Sasson S.A. Cancer Res. 64 (2004) 1058
11. Bates R.C., Edwards N.S., Burns G.F., and Fisher D.E. Cancer Res. 61 (2001) 5275
12. Subramaniam V., Vincent I.R., Gardner H., Chan E., Dhamko H., and Jothy S. Exp. Mol. Path. 83 (2007) 207
13. Roginskaya V., Zuo S., Caudell E., Nambudiri G., Kraker A.J., and Corey S.J. Leukaemia 13 (1999) 855
14. Okamoto M., Hayakawa F., Miyata Y., Watamoto K., Emi N., Abe A., Kiyoi H., Towatari M., and Naoe T. Leukemia 21 (2007) 403
15. Wu J., Meng F., Kong L.-Y., Peng Z., Ying Y., Bornmann W.G., Darnay B.G., Lamothe B., Sun H., Talpaz M., and Donato N.J. J. Nat. Cancer Inst. 100 (2008) 926
16. free = 32.4% Final coordinates were deposited to Protein Data Bank (code: 3A4O).
17. Kinoshita T., Matsubara M., Ishiguro H., Okita K., and Tada T. Biochem. Biophys. Res. Commun. 346 (2006) 840
18. Zhu X., Kim J.L., Newcomb J.R., Rose P.E., Stover D.R., Toledo L.M., Zhao H., and Morgenstern K.A. Structure 7 (1999) 651
19. Breitenlechner C.B., Kairies N.A., Honold K., Scheiblich S., Koll H., Greiter E., Koch S., Schäfer W., Huber R., and Engh R.A. J. Mol. Biol. 353 (2005) 222
20. Kuduva S.S., Craig D.C., Nangia A., and Desiraju G.R. J. Am. Chem. Soc. 121 (1999) 1936
21. There is a report which shows the importance of this groove to the selectivity. See:. Burchat A., Borhani D.W., Calderwood D.J., Hirst G.C., Li B., and Stachlewitz R.F. Bioorg. Med. Chem. Lett. 16 (2005) 118
22. A similar molecule design has been reported with the c-Jun N-terminal kinase-3. See:. Swahn B.-M., Huerta F., Kallin E., Malmström J., Weigelt T., Viklund J., Womack P., Xue Y., and Öhberg L. Bioorg. Med. Chem. Lett. 15 (2005) 5095
23. Liu Y., and Gray N.S. Nat. Chem. Biol. 2 (2006) 358
24. Nagar B., Bornmann W.G., Pellicena P., Schindler T., Veach D.R., Todd Miller W., Clarkson B., and Kuriyan J. Cancer Res. 62 (2002) 4236