Recent advances in JAK3 kinase inhibitors

IDrugs

Volumn 2, Issue 10, 1999, Pages 1026-1030

  Sudbeck, Elise A ^a   Uckun, Fatih M ^a  

^a Parker Hughes Cancer Center   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 HYDROXYANILINO) 6,7 DIMETHOXYQUINAZOLINE; ANTILEUKEMIC AGENT; CT 2576; CYCLOSPORIN A; CYTOVARICIN B; IMMUNOSUPPRESSIVE AGENT; ISOENZYME; JANUS KINASE 3 INHIBITOR; LEFLUNOMIDE; N BENZYL 2 CYANO 3 (3,4 DIHYDROXYPHENYL)ACRYLAMIDE; PROTEIN TYROSINE KINASE INHIBITOR; STAUROSPORINE; TACROLIMUS; TERIFLUNOMIDE; UNCLASSIFIED DRUG; WHI P 154; WHI P 97;

ACUTE LYMPHOBLASTIC LEUKEMIA; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; CELL PROLIFERATION; CELL SURVIVAL; DRUG INDICATION; DRUG POTENCY; DRUG RESEARCH; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME INHIBITION; HUMAN; IMMUNOSUPPRESSIVE TREATMENT; NONHUMAN; PROTEIN FAMILY; REVIEW;

EID: 0032853338     PISSN: 13697056     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (61)

1. Tortolani PJ, Lai BK, Riva A, Johnston JA, Chen YQ, Reaman GH, Beckwith M, Longo D, Ortaldo JR, Bhatia K et al: Regulation of JAK3 expression and activation in human B cells and B cell malignancies. J Immunol (1995) 155:52205226.
2. Meydan N, Grunbèrger T, Dadi H, Shahar M, Arpaia E, Lapidot Z, Leeder JS, Freedman M, Cohen A, Gazit A, Levitzki A, Roifman CM: Inhibition of acute lymphoblastic leukaemia by a JAK2 inhibitor. Nature (1996) 379:645-648.
3. Zhang Q, Nowak I, Vonderheid EC, Rook AH, Kadin ME, Nowell PC, Shaw LM, Wasik MA: Activation of JAK/STAT proteins involved in signal transduction pathway mediated by receptor for interleukin 2 in malignant T-lymphocytes derived from cutaneous anaplastic large T-cell lymphoma and Sezary syndrome. Proc Natl Acad Sei USA (1996) 93:9148-9153.
4. Nielsen M, Kaltoft K, Nordahl M, Ropke C, Geisler C, Mustelin T, Dobson P, Svejgaard A, Odum N: Constitutive activation of a slowly migrating isoform of STAT3 In mycosis fungoides: tyrphostin AG490 inhibits STAT3 activation and growth of mycosis fungoides tumor cell lines. Proc Natl Acad Sei USA (1997) 94:6764-6769.
5. Takemoto S, Mulloy JC, Cereseto A, Migone TS, Patel BK, Matsuoka M, Yamaguchi K, Takatsuki K, Kamihira S, White JD, Leonard WJ, Waldmann T, Franchini G: Proliferation of adult T-cell leukemia/lymphoma cells is associated with the constitutive activation of JAK/STAT proteins. Proc Natl Acad Sei USA (1997) 94:13897-13902.
6. Liu KD, Gaffen SL, Goldsmith MA: JAK/STAT signaling by cytokine receptors. CurrOpin Immunol (1998) 10:271-278.
7. Wasik MA, Nowak I, Zhang Q, Shaw LM: Suppression of proliferation and phosphorylation of Jak3 and STATS in malignant T-cell lymphoma cells by derivatives of octytamino-undecyl-dimethylxanthlne. Leuk Lymphoma (1998)28:551-560.
8. Witthuhn BA, Williams MD, Kerawalla H, Uckun FM: Differential substrate recognition capabilities of Janus family protein tyrosine kinases within the interleukin 2 receptor (II-2R) system: JAK3 as a potential molecular target for treatment of leukemias with a hyperactive JAK-STAT signaling machinery. Leuk Lymphoma (1999) 32:289-297.
9. Horvath CM, Damell JE: The state of the STATs: recent developments in the study of signal transduction to the nucleus. CurrOpin Ce//B/o/(1997) 9(2):233-239.
10. Levy DE: The house that JAK/STAT built Cytokine Growth Factor Rev (1997) 8(1):81-90.
11. Russell SM, Johnston JA, Noguchi M, Kawamura M, Bacon CM, Friedmann M, Berg M, McVicar DW, Witthuhn BA, Silvennoinen O et al: Interaction of IL-2R βand YC chains with JAK1 and JAK3: implications for XSCID and XCID. Science (1994) 266:1042-1045.
12. Noguchi M, Yi H, Rosenblatt HM, Filipovich AH, Adelstein S, Modi WS, McBride OW, Leonard WJ: lnterleukin-2 receptor y chain mutation results in X-linked severe combined immunodeficiency in humans. Cell (1993) 73:147-157.
13. Leonard WJ, O'Shea JJ: JAKS and STATS: Biological implications. Annu Rev Immunol (1998) 16:293-322.
14. Leonard WJ: The molecular basis of X-linked severe combined immunodeficiency: defective cytokine receptor signaling. Annu Rev Med (1996) 47:229-239.
15. Demoulin JB, Uyttenhove C, Van Roost E, DeLestre B, Donckers D, Van Snick J, Renauld JC: A single tyrosine of the interleukin-9 (IL-9) receptor Is required for STAT activation, antiapoptotic activity, and growth regulation by IL-9. Mol Ce//B/O/O996) 16:4710-4716.
16. Jurlander J, Lai CF, Tan J, Chou CC, Geisler CH, Schriber J, Blumenson LE, Narula SK, Baumann H, Caligiuri MA: Characterization of interleukin-10 receptor expression on B-cell chronic lymphocytic leukemia cells. Blood (1997) 89:4146-4152.
17. Kaneko S, Suzuki N, Koizumi H, Yamamoto SS, Sakane T: Rescue by cytokines of apoptotic cell death Induced by IL2 deprivation of human antigen-specific T-cell clones. Clin Exp Immun (1997) 109:185-193.
18. Nakamura N, Chin H, Miyasaka N, Miura O: An epidermal growth factor receptor/JAK2 tyrosine kinase domain chimera induces tyrosine phosphorylation of STATS and transduces a growth signal in hematopoietic cells. J Biol Chem (1996) 271:19483-19488.
19. Bunjes D, Hardt C, Rollinghoff M, Wagner H: Cyclosporin A mediates immunosuppression of primary cytotoxic T-cell responses by impairing the release of interleukin 1 and interleukin 2. Eur J Immunol (1981) 11:657-661.
20. Imami N, Brookes PA, Lombardi G, Hakooz B, Johns M, Goldman JM, Batchelor JR, Lechler Rl, Ritter MA: Association between interleukin-4-producing T lymphocyte frequencies and reduced risk of graft-versus-host disease. Transplantation (1998) 65:979-988.
21. Li XC, Roy-Chaudhury P, Hancock WW, Manfro R, Zand MS, Li Y, Zheng XX, Nickerson PW, Steiger J, Malek TR, Strom TB: IL-2 and IL-4 double knockout mice reject islet allografts: a role for novel T-cell growth factors in allograft rejection. J Immunol (1998) 161:890-896.
22. Harris DT, Sakiestewa D, Lyons C, Kreitman RJ, Pastan I: Prevention of graft-versus-host disease (GvHD) by elimination of recipient-reactive donor T-cells with recombinant toxins that target the interleukin 2 (IL-2) receptor. Bone Marrow Transplant (1999) 23:137-144.
23. Sugamura K, Asao H, Kondo M, Tanaka N, Ishii N, Ohbo K, Nakamura M, Takeshita T: The interleukin-2 receptor y chain: Its role in the multiple cytokine receptor complexes and T-cell development in XSCID. Annu Rev Immunol (1996) 14:179-205.
24. Miyazaki T, Kawahara A, Fujii H, Nakagawa Y, Minami Y, Liu ZJ, Oishi I, Silvennoinen O, Witthuhn BA, Ihle JN: Functional activation of JAK1 and JAK3 by selective association with IL-2 receptor subunits. Science (1994) 266:1045-1047.
25. Boussiotis VA, Barber DA, Nakarai T, Freeman GJ, Gribben JG, Bernstein GM, D'Andréa AD, Ritz J, Nadler LM: Prevention of T-cell anergy by signaling through the y c chain of the IL-2 receptor. Science (1994) 266:1039-4102.
26. Galli SJ: New concepts about the mast cells. New Engl J Med (1993) 328:257-265.
27. Gordon JR, Galli SJ: Mast cells as a source of both preformed and immunologically-inducible TNFα/cachectin. Nature (1990) 346:274-276.
28. Hamawy MJ, Mergenhagen SE, Siraganian RP: Protein tyrosine phosphorylatio'i as a mechanism of signalling in mast cells and basophüs. Ce//S/gna/(1995) 7:535-544.
29. Malaviya R, Malaviya R, Jakschik BA: Reversible translocation of 5-lipoxygenase In mast cells upon IgE/antigen stimulation. J Biol Chem (1993) 268:4939-4944.
30. Malaviya R, Uckun FM: Targeting Janus kinase (JAKJ-3 in mast cells prevents immediate hypersensitivity reactions and anaphylaxis. JBiol Chem (1999) in press.
31. Malaviya R, Uckun FM: Genetic and biochemical evidence for a critical role of Janus kinase (JAK)-3 in mast cellmediated Type I hypersensitivity reactions. Biochem Biophys Res Commun (1999) 257:807-813.
32. Krolewski JJ, Lee R, Eddy R, Shows TB, Dalla-Favera R: Identification and chromosomal mapping of new human tyrosine kinase genes. Oncogene (1990) 5(3):277-282.
33. Wilks AF, Harpur AG, Kurban RR, Ralph SJ, Zürcher G, Ziemiecki A: Two novel protein-tyrosine kinases, each with a second phosphotransferase-related catalytic domain, define a new class of protein kinase. Mol Cell Biol (1991) 11(4):2057-2065.
34. Harpur AG, Andres AC, Ziemiecki A, Aston RR, Wilks AF: JAK2, a third member of the JAK family of protein tyrosine kinases. Oncogene (1992) 7(7): 1347-1353.
35. (a) Takahashi T, Shirasawa T: Molecular cloning of rat JAK3, a novel member of the JAK family of protein tyrosine kinases. F£BS Lett (1994) 342(2):124-128.
36. (b) Johnston JA, Kamura M, Kirken RA, Chen YQ, Blake TB, Shibuya K, Ortalso JR, McVicar DW, O'Shea JJ: Phosphorylation and activation of the Jak-3 Janus kinase in response to interleukin-2. Nature (1994) 370:151-153.
37. Witthun BA, Silvennoinen O, Miura O, Lai KS, Cwik C, Liu ET, Ihle JN: Involvement of the Jak-3 Janus kinase in signalling by interleukins 2 and 4 in lymphoid and myeloid cells. Nature (1994) 370:153-157.
38. Frank SJ, Gilliland G, Kraft AS, Arnold CS: Interaction of the growth hormone receptor cytoplasmic domain with the JAK2 tyrosine kinase. Endocrinology (1994) 270:776-785.
39. Frank SJ, Yi W, Zhao Y, Goldsmith JF, Gilliland G, Jiang J, Sakai I, Kraft AS: Regions of the JAK2 tyrosine kinase required for coupling to the growth hormone receptor. J Biol Chem (1995) 270:776-785.
40. Zhao Y, Wagner F, Frank SJ, Kraft AS: The amino-terminal portion of the JAK2 protein kinase Is necessary for binding and phosphorylation of the granulocytemacrophage colony-stimulating factor receptor βc chain. J Biol Chem (1995) 270:814-818.
41. Kohlhuber F, Rogers NC, Watling D, Feng J, Guschin D, Briscoe J, Witthuhn BA, Kotenko SV, Pestka S, Stark OR, Ihle JN, Kerr IM: A JAK1/JAK2 chimera can sustain a and y Interferon responses. Mol Cell Biol (1997) 17:695-706.
42. Chen M, Cheng A, Chen YQ, Hymel A, Hanson EP, Kimmel L, Minami Y, Taniguchi T, Changelian P, O'Shea J: The amino terminus of JAK3 is necessary and sufficient for binding to the common Y chain and confers the ability to transmit interleukin 2-mediated signals. Proc Natl Acad Sei USA (1997)94:6910-6915.
43. Yamashita N, Kazuo SY, Kitamura M, Wakao H, Furihata K, Furihata K, Hayakawa Y, Miyajima A, Seto H: Cytovaricin B, a new inhibitor of JAK-STAT signal transduction produced by Streptomyces torulosus. JAntibiot (Tokyo) (1997) 50:440-442.
44. Sudbeck EA, Liu XP, Narta RK, Mahajan S, Ghosh S, Mao C, Uckun FM: Structure-based design of specific inhibitors of Janus kinase 3 as apopiosis-inducing antileukemic agents. Clin Cancer Res (1999) 5:1569-1582.
45. Manna SK, Aggarwal BB: Immunosuppressive leflunomide metabolite (A-771726) blocks TNF-dependent nuclear factor-K B activation and gene expression. J tmmunol (1999)162:2095-2102.
46. Matter T, Kochhar K, Bartlett R, Bremer EG, Finnegan A: Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide. FEBS Lett (1993) 334:161 -164.
47. Ghosh S, Zheng Y, Jun X, Narta R, Mahajan S, Navara C, Mao C, Sudbeck EA, Uckun FM: α-Cyano-β-hydroxy-β-methyl-A44-(trrfluoromethoxy)phenyl] propenamide: an inhibitor of the EG F receptor tyrosine kinase with potent cytotoxic activity against breast cancer cells. Clin Cancer Res (1998) 4:2657-2668.
48. Siemasko K, Chong AS, Jack HM, Gong H, Williams JW, Finnegan A: Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in lgG1 production. J Immunol (1998)160:1581-1588.
49. Fiorucci G, Percario ZA, Marcelin C, Coccia EM, Affabris, Romeo G: Inhibition of protein phosphorylation modulates expression of the JAK family protein tyrosine kinases. J Virol (1995) 69:5833-5837.
50. Nakano H, Kobayashi E, Takahashi I, Tamaoki T, Kuzuu Y, Iba H: Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60. J Antiblot (1987) 40:706-708.
51. Meggio F, Donella DA, Ruzzene M, Brunati AM, Cesaro Guerra LB, Meyer T, Mett H, Fabbro D, Füret P, et al: Different susceptibility of protein kinases to Staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2. EurJBiochem (1995) 234:317-322.
52. Lamers MB, Antson AA, Hubbard RE, Scott RK, Williams DH: Structure of the protein tyrosine kinase domain of Cterminal Src kinase (CSK) in complex with Staurosporine. J Mol Biol (1999) 285:713-725.
53. Fujita-Yamaguchi Y, Kathuria S: Characterization of receptor tyrosine-specific protein kinases by the use of inhibitors. Staurosporine is 100-times more potent inhibitor of insulin receptor than IGF-1 receptor. Biochem Biophys Res Commun (1988) 157:955-962.
54. Caravatti G, Meyer T, Fredenhagen A, Trinks U, Mett H, Fabbro D: Inhibitory activity and selectivity of Staurosporine derivatives towards protein kinase C. Bioorg Med Chem Lett (1994) 4:399-404.
55. Prade L, Engh RA, Girod A, Kinzel V, Huber R, Bossemeyer D: Staurosporine-induced conformational changes of cAMPdependent protein kinase catalytic subunit explain inhibitory potential. Structure (1997) 5:1627-1637.
56. Wang LH, Kirken RA, Erwin RA, Yu CR, Farrar WL: JAK3, STAT and MARK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T-cell response. J Immunol (1999) 162(7):3897-3904.
57. Sicheri F, Moarefi I, Kuriyan J: Crystal structure of the SRC family tyrosine kinase HCK. Nature (1997) 385:602-9.
58. Hubbard, SR: Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog. EMBO J(1997) 16:5572-5581.
59. Mahajan S, Ghosh S, Sudbeck EA, Zheng Y, Downs S, Hupke M, Uckun FM: Rational design and synthesis of a novel anti- . leukemic agent targeting Bruton's tyrosine kinase (BTK): LFMA13 [a-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyi) propenamide]. J Bid Chem (1999) 274:9587-9599.
60. Malaviya R, Uckun FM: Janus kinase (JAK)-3 In mast cells as a mediator of immediate hypersensitive reactions and anaphylaxis. J Allergy Clin Immunol (1999) 103:S58-S59.
61. Cetkovic-Cvrlje M, Uckun FM: Janus kinase (JAK) 3 inhibitor WHI-P131 prolongs mouse islet allograft survival without impairment of Islet cell function. Transplantation (1999) submitted.