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Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

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Pages 921-947 | Published online: 22 May 2012

Bibliography

  • Luskova P, Draber P. Modulation of the Fc epsilon receptor I signaling bytyrosine kinase inhibitors: search for therapeutic targets of inflammatory and allergy diseases. Curr Pharm Des 2004;10:1727-37
  • Uckun FM, Qazi S. Spleen tyrosine kinase as a molecular target for treatment of leukemias and lymphomas. Expert Rev Anticancer Ther 2010;10:1407-18
  • Genevier HC, Hinshelwood S, Gaspar HB, Expression of Bruton's tyrosine kinase protein within the B cell lineage. Eur J Immunol 1994;24:3100-5
  • Uckun FM, Qazi S. Bruton's tyrosine kinase as a molecular target in treatment of leukemias and lymphomas as well as inflammatory disorders and autoimmunity. Expert Opin Ther Patents 2010;20:1457-70
  • Satterthwaite AB, Witte ON. The role of Bruton's tyrosine kinase in B-cell development and function: a genetic perspective. Immunol Rev 2000;175:120-7
  • Mohamed AJ, Yu L, Backesjo CM, Bruton's tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain. Immunol Rev 2009;228:58-73
  • Satterthwaite AB, Cheroutre H, Khan WN, Btk dosage determines sensitivity to B cell antigen receptor cross-linking. Proc Natl Acad Sci USA 1997;94:13152-7
  • Afar DE, Park H, Howell BW, Regulation of Btk by Src family tyrosine kinases. Mol Cell Biol 1996;16:3465-71
  • Satterthwaite AB, Li Z, Witte ON. Btk function in B cell development and response. Semin Immunol 1998;10:309-16
  • Khan WN, Alt FW, Gerstein RM, Defective B cell development and function in Btk-deficient mice. Immunity 1995;3:283-99
  • Rawlings DJ, Saffran DC, Tsukada S, Mutation of unique region of Bruton's tyrosine kinase in immunodeficient XID mice. Science 1993;261:358-61
  • Satterthwaite AB, Li Z, Witte ON. Btk function in B cell development and response. Semin Immunol 1998;10:309-16
  • Conley ME, Dobbs AK, Farmer DM, Primary B cell immunodeficiencies: comparisons and contrasts. Annu Rev Immunol 2009;27:199-27
  • Herman SE, Gordon AL, Hertlein E, Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood 2011;117:6287-96
  • Honigberg LA, Smith AM, Sirisawad M, The bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA 2010;107:13075-80
  • Pan Z. Bruton's tyrosine kinase as a drug discovery target. Drug News Perspect 2008;2:357-62
  • Hata D, Kawakami Y, Inagaki N, Involvement of Bruton's tyrosine kinase in FcepsilonRI-dependent mast cell degranulation and cytokine production. J Exp Med 1998;187:1235-47
  • Jongstra-Bilen J, Puig Cano A, Hasija M, Dual functions of Bruton's tyrosine kinase and Tec kinase during Fcgamma receptor-induced signaling and phagocytosis. J Immunol 2008;181:288-98
  • Pan Z, Scheerens H, Li S, Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase. Chem Med Chem 2007;2:58-61
  • Davis RE, Ngo VN, Lenz G, Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 2010;463:88-92
  • Herman SE, Honigberg LA, Smith AM, The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA 2010;107:13075-80
  • Ponader S, Chen S-S, Buggy JJ, Bruton's tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood 2012;119:1182-9
  • Chang BY, Huang MM, Francesco M, The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther 2011;13:R115
  • Burger JA, O'Brien S, Fowler N, The Bruton's tyrosine kinase inhibitor, PCI-32765, is well tolerated and demonstrates promising clinical activity in chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL): an update on ongoing Phase 1 studies. Blood 2010;116:32a
  • Advani R, Sharman JP, Smith SM, Effect of Btk inhibitor PCI-32765 monotherapy on responses in patients with relapsed aggressive NHL: evidence of antitumor activity from a phase I study [abstract 8012]. J Clin Oncol 2010;28:15s
  • Advani R, Sharman J, Smith ST, The Btk inhibitor PCI-32765 is highly active and well tolerated in patients with relapsed/refractory B cell malignancies: final results from a phase I study. Ann Oncol 2011;22(Suppl 4):iv135-7
  • O'Brien S, Burger JA, Coutre SE, The Btk Inhibitor PCI-32765 is highly active and tolerable in patients with poor-risk CLL: interim results from a phase Ib/II study. Ann Oncol 2011;22(Suppl 4):iv123-4
  • O'Brien S, Burger JA. BlumKA, et al. The Bruton's tyrosine kinase (BTK) inhibitor PCI-32765 induces durable responses in relapsed or refractory (R/R) chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL): follow-up of a phase Ib/II study [abstract 983]. Blood 2011;118:449
  • Liu L, Di Paolo J, Barbosa J, Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-Induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. J Pharmacol Exp Ther 2011;338:154-63
  • Liu L, Halladay JS, Shin Y, Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor. Drug Metab Dispos 2011;39:1840-9
  • Mahajan S, Ghosh S, Sudbeck EA, Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl)propenamide]. J Biol Chem 1999;274:9587-99
  • Heinonen JE, Smith CI, Nore BF. Silencing of Bruton's tyrosine kinase (Btk) using short interfering RNA duplexes (siRNA). FEBS Lett 2002;527:274-8
  • Uckun FM, Dibirdik I, Qazi S, Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). Bioorg Med Chem 2007;15:800-14
  • Uckun FM. Chemosensitizing anti-cancer activity of LFM-A13, a leflunomide metabolite analog targeting polo-like kinases. Cell Cycle 2007;6:3021-6
  • Uckun F, Dibirdik I, Sarkissian A, Qazi S. In vitro and in vivo chemosensitizing activity of LFM-A13, a dual-function inhibitor of Bruton's tyrosine kinase and polo-like kinases, against human leukemic B-cell precursors. Arzneimittelforschung 2011;61:252-9
  • Bam R, Lin W, Khan S, Cell surface CXCR4 and BTK expression are associated in myeloma cells and osteoclast precursors and mediate myeloma cell homing and clonogenicity, and osteoclastogenesis [abstract 884]. Blood 2011;118:404
  • Evans E, Sheets M, Bernar H, Prolonged inhibition of BCR signaling and suppression of B cell lymphoma through Irreversible Inhibition of Bruton's tyrosine kinase [abstract 2608]. Blood 2008;112:904
  • Evans E, Teste R, Aslanian S, Clinical development of AVL-292; a potent, selective covalent Btk inhibitor for the treatment of B cell malignancies [abstract 3485]. Blood 2011;118:1487
  • Evans E, Ponader S, Karp R, Covalent inhibition of Btk with clinical development compound AVL-292 disrupts signaling that maintains the microenvironment necessary for chronic lymphocytic leukemia growth [abstract 2.23]. Clin Lymphoma Myeloma Leukoc 2011;11(Suppl 2):s173
  • Eda H, Santo L, Cirstea DD, Targeting Bruton's tyrosine kinase as a novel approach to inhibit osteoclast function in multiple myeloma [abstract 2882]. Blood 2011;118:1243
  • Evans E, Tester R, Sharon A, Translational medicine of a selective inhibitor of Btk in rheumatic diseases: pharmacology and early clinical development [abstract]. Arthritis Rheum 2011;63(Suppl 10):1757
  • Mocsai A, Ruland J, Tybulewicz VL. The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 2010;10:387-402
  • Rogers NC, Slack EC, Edwards AD, Syk-dependent cytokine induction by Dectin-1 reveals a novel pattern recognition pathway for C type lectins. Immunity 2005;22:507-17
  • Trner M, Schweighoffer E, Colucci F, Tyrosine kinase SYK: essential functions for immunoreceptor signalling. Immunol Today 2000;21:148-54
  • Zarbock A, Abram CL, Hundt M, PSGL-1 engagement by E-selectin signals through Src kinase Fgr and ITAM adapters DAP12 and FcR gamma to induce slow leukocyte rolling. J Exp Med 2008;205:2339-47
  • Geahlen RL. Syk and pTyr'd: signaling through the B cell antigen receptor. Biochim Biophys Acta 2009;1793:1115-27
  • Irish JM, Czerwinski DK, Nolan GP, Levy R. Altered B-cell receptor signaling kinetics distinguish human follicular lymphoma B cells from tumor infiltrating nonmalignant B cells. Blood 2006;108:3135-42
  • Baudot AD, Jeandel PY, Mouska X, The tyrosine kinase Syk regulates the survival of chronic lymphocytic leukemia B cells through PKCdelta and proteasome-dependent regulation of Mcl-1 expression. Oncogene 2009;28:3261-73
  • Buchner M, Fuchs S, Prinz G, Spleen tyrosine kinase is overexpressed and represents a potential therapeutic target in chronic lymphocytic leukemia. Cancer Res 2009;69:5424-32
  • Quiroga MP, Balakrishnan K, Kurtova AV, B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406. Blood 2009;114:1029-37
  • Cheng S, Coffey G, Zhang XH, SYK inhibition and response prediction in diffuse large B-cell lymphoma. Blood 2011;118:6342-52
  • Mocsai A, Ruland J, Tybulewicz VL. The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 2010;10:387-402
  • Braselmann S, Taylor V, Zhao H, R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 2006;319:998-1008
  • Chen L, Monti S, Juszczynski P, SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 2008;111:2230-7
  • Sweeny DJ, Li W, Grossbard E, Lau DT. Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey. Xenobiotica 2010;40:415-23
  • Zhu Y, Herlaar E, Masuda ES, Immunotoxicity assessment for the novel Spleen tyrosine kinase inhibitor R406. Toxicol Appl Pharmacol 2007;221:268-77
  • Pine PR, Chang B, Schoettler N, Inflammation and bone erosion are suppressed in models of rheumatoid arthritis following treatment with a novel Syk inhibitor. Clin Immunol 2007;124:244-57
  • Suljagic M, Longo PG, Bennardo S, The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the E{micro}- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood 2010;116:4894-905
  • Bahjat FR, Pine PR, Reitsma A, An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus. Arthritis Rheum 2008;58:1433-44
  • Smith J, McDaid JP, Bhangal G, A spleen tyrosine kinase inhibitor reduces the severity of established glomerulonephritis. J Am Soc Nephrol 2010;21:231-6
  • Podolanczuk A, Lazarus AH, Crow AR, Of mice and men: an open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of Syk. Blood 2009;113:3154-60
  • Sweeny DJ, Li W, Clough J, Metabolism of fostamatinib, the oral methylene phosphate prodrug of the spleen tyrosine kinase inhibitor R406 in humans: contribution of hepatic and gut bacterial processes to the overall biotransformation. Drug Metab Dispos 2010;38:1166-76
  • Genovese MC, Kavanaugh A, Weinblatt ME, An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis: a three-month randomized, placebo-controlled, phase ii study in patients with active rheumatoid arthritis that did not respond to biologic agents. Arthritis Rheum 2011;63:337-45
  • Weinblatt ME, Kavanaugh A, Burgos-Vargas R, Treatment of rheumatoid arthritis with a Syk kinase inhibitor: a twelve-week, randomized, placebo-controlled trial. Arthritis Rheum 2008;58:3309-18
  • Weinblatt ME, Kavanaugh A, Genovese MC, An oral spleen tyrosine kinase (Syk) inhibitor for rheumatoid arthritis. N Engl J Med 2010;363:1303-12
  • Friedberg JW, Sharman J, Sweetenham J, Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia. Blood 2010;115:2578-85
  • Niimi T, Orita M, Okazawa-Igarashi M, Design and synthesis of non-peptidic inhibitors for the Syk C-terminal SH2 domain based on structure-based in-silico screening. J Med Chem 2001;44:4737-40
  • Rossi AB, Herlaar E, Braselmann S, Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol 2006;118:749-55
  • Guyer BJ, Shimamoto SR, Bradhurst AL, Mast cell inhibitor R112 is well tolerated and affects prostaglandin D2 but not other mediators, symptoms, or nasal volumes in a nasal challenge model of allergic rhinitis. Allergy Asthma Proc 2006;27:208-13
  • Meltzer EO, Berkowitz RB, Grossbard EB. An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. J Allergy Clin Immunol 2005;115:791-6
  • Norman P. A novel Syk kinase inhibitor suitable for inhalation:R-343(?)–WO-2009031011. Expert Opin Ther Patents 2009;19:1469-72
  • Yamamoto N, Takeshita K, Shichijo M, The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]-nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther 2003;306:1174-81
  • Wolter F, Clausnitzer A, Akoglu B, Piceatannol, a natural analog of resveratrol, inhibits progression through the S phase of the cell cycle in colorectal cancer cell lines. J Nutr 2002;132:298-302
  • Wang BH, Lu ZX, Polya GM. Inhibition of eukaryote serine/threonine-specific protein kinases by piceatannol. Planta Med 1998;64:195-9
  • Azmi AS, Bhat SH, Hadi SM. Resveratrol-Cu(II) induced DNA breakage in human peripheral lymphocytes: implications for anticancer properties. FEBS Lett 2005;579:3131-5
  • Gururajan M, Jennings CD, Bondada S. Cutting edge: constitutive B cell receptor signaling is critical. J Immunol 2006;176:5715-19
  • Ovesna Z, Kozics K, Bader Y, Antioxidant activity of resveratrol, piceatannol and 3,3′,4,4′,5,5′-hexahydroxy-trans-stilbene in three leukemia cell lines. Oncol Rep 2006;16:617-24
  • Leseux L, Hamdi SM, Al Saati T, Syk dependent mTOR activation in follicular lymphoma cells. Blood 2006;108:4156-62
  • Moriya K, Rivera J, Odom S, ER-27319, an acridone-related compound, inhibits release of antigen-induced allergic mediators from mast cells by selective inhibition of fcepsilon receptor I-mediated activation of Syk. Proc Natl Acad Sci USA 1997;94:12539-44
  • Andrews RP, Kepley CL, Youssef L, Regulation of the very late antigen-4-mediated adhesive activity of normal and nonreleaser basophils: roles for Src, Syk, and phosphatidylinositol 3-kinase. J Leukoc Biol 2001;70:776-82
  • Liddle J, Atkinson FL, Barker MD, Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg Med Chem Lett 2011;21:6188-94
  • Uckun FM, Qazi S, Ma H, STAT3 is a substrate of SYK tyrosine kinase in B-lineage leukemia/lymphoma cells exposed to oxidative stress. Proc Natl Acad Sci USA 2010;107:2902-7
  • Uckun FM, Ek RO, Jan ST, Targeting SYK kinase-dependent anti-apoptotic resistance pathway in B-lineage acute lymphoblastic leukaemia (ALL) cells with a potent SYK inhibitory pentapeptide mimic. Br J Haematol 2010;149:508-17
  • Uckun FM, Qazi S, Ozer Z, Inducing apoptosis in chemotherapy-resistant B-lineage acute lymphoblastic leukaemia cells by targeting HSPA5, a master regulator of the anti-apoptotic unfolded protein response signalling network. Br J Haematol 2011;153:741-52
  • Uckun FM, Dibirdik I, Qazi S. Augmentation of the antileukemia potency of total-body irradiation (TBI) by a novel P-site inhibitor of spleen tyrosine kinase (SYK). Radiat Res 2010;174:526-31
  • Villasen AG, Kondru R, Ho H, Structural insights for design of potent spleen tyrosine kinase inhibitors from crystallographic analysis of three inhibitor complexes. Chem Biol Drug Des 2009;73:466-70
  • Yamamoto N, Takeshita K, Shichijo M, The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]-nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther 2003;306:1174-81
  • Ruzza P, Biondi B, Calderan A. Therapeutic prospect of Syk inhibitors. Expert Opin Ther Patents 2009;19:1361-76
  • Aleshin A, Finn RS. SRC: a century of science brought to the clinic. Neoplasia 2010;12:599-607
  • Chatzizacharias NA, Kouraklis GP, Giaginis CT, Theocharis SE. Clinical significance of Src expression and activity in human neoplasia. Histol Histopathol 2012;27:677-92
  • Creedon H, Brunton VG. SRC kinase inhibitors: promising cancer therapeutics? Crit Rev Oncog 2012;17:145-59
  • Alvarez RH, Kantarjian HM, Cortes JE. The role of Src in solid and hematologic malignancies: development of new-generation Src inhibitors. Cancer 2006;107:1918-29
  • Brunton VG, Avizienyte E, Fincham VJ, Identification of srcspecific phosphorylation site on focal adhesion kinase: dissection of the role of Src SH2 and catalytic functions and their consequences for tumor cell behavior. Cancer Res 2005;65:1335-42
  • Scapini P, Pereira S, Zhang H, Lowell CA. Multiple roles of Lyn kinase in myeloid cell signaling and function. Immunol Rev 2009;228:23-40
  • Niiro H, Clark EA. Regulation of B-cell fate by antigen-receptor signals. Nat Rev Immunol 2002;2:945-56
  • Contri A, Brunati AM, Trentin L, Chronic lymphocytic leukemia B cells contain anomalous Lyn tyrosine kinase, a putative contribution to defective apoptosis. J Clin Invest 2005;115:369-78
  • Wiestner A, Rosenwald A, Barry TS, ZAP-70 expression identifies a chronic lymphocytic leukemia subtype with unmutated immunoglobulin genes, inferior clinical outcome, and distinct gene expression profile. Blood 2003;101:4944-51
  • Davis RE, Ngo VN, Lenz G, Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 2010;463:88-92
  • Ke J, Chelvarajan RL, Sindhava V, Anomalous constitutive Src kinase activity promotes B lymphoma survival and growth. Mol Cancer 2009;8:132
  • Chow KU, Nowak D, Hofmann W, Imatinib induces apoptosis in CLL lymphocytes with high expression of Par-4. Leukemia 2005;19:1103-5
  • Aloyz R, Grzywacz K, Xu ZY, Imatinib sensitizes CLL lymphocytes to chlorambucil. Leukemia 2004;18:409-14
  • Hebb J, Assouline S, Rousseau C, A phase I study of imatinib mesylate in combination with chlorambucil in previously treated chronic lymphocytic leukemia patients. Cancer Chemother Pharmacol 2011;68:643-51
  • Veldurthy A, Patz M, Hagist S, The kinase inhibitor dasatinib induces apoptosis in chronic lymphocytic leukemia cells in vitro with preference for a subgroup of patients with unmutated IgVH genes. Blood 2008;112:1443-52
  • Amrein L, Hernandez TA, Ferrario C, Dasatinib sensitizes primary chronic lymphocytic leukaemia lymphocytes to chlorambucil and fludarabine in vitro. Br J Haematol 2008;143:698-706
  • Contri A, Brunati AM, Trentin L, Chronic lymphocytic leukemia B cells contain anomalous Lyn tyrosine kinase, a putative contribution to defective apoptosis. J Clin Invest 2005;115:369-78
  • Lee M, Kim JY, Koh WS. Apoptotic effect of PP2 a Src tyrosine kinase inhibitor, in murine B cell leukemia. J Cell Biochem 2004;93:629-38
  • Veldurthy A, Patz M, Hagist S, The kinase inhibitor dasatinib induces apoptosis in chronic lymphocytic leukemia cells in vitro with preference for a subgroup of patients with unmutated IgVH genes. Blood 2008;112:1443-52
  • Aguillon RA, Llanos CA, Suarez CJ, Dasatinib induces apoptosis in chronic lymphocytic leukemia and enhances the activity of rituximab and fludarabine [abstract 1116]. Blood 2007;110:339a
  • Harr MW, Caimi PF, McColl K, The tyrosine kinase inhibitor dasatinib enhances glucocorticoid-induced apoptosis and sensitizes chronic lymphocytic leukemia cells to dexamethasone. Blood 2009;114:4811
  • Amrein PC, Attar EC, Takvorian T, Phase II study of dasatinib in relapsed or refractory chronic lymphocytic leukemia. Clin Cancer Res 2011;17:2977-86
  • Al-Ameri AM, Badoux X, Ferrajoli A, Phase II study of dasatinib in patients with relapsed chronic lymphocytic leukemia. Blood 2010;116:4488
  • Chow KU, Nowak D, Trepohl B, The tyrosine kinase inhibitor AMN107 (Nilotinib) exhibits off-target effects in lymphoblastic cell lines. Leuk Lymphoma 2007;48:1379-88
  • Santos FP, Kantarjian H, Cortes J, Quintas-Cardama A. Bafetinib, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Curr Opin Investig Drugs 2010;11:1450-65
  • Burkard TR, Rix U, Breitwieser FP, A computational approach to analyze the mechanism of action of the kinase inhibitor bafetinib. PLoS Comput Biol 2010;6:e1001001
  • Niwa T, Asaki T, Kiura S. NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor. Anal Chem Insights 2007;2:93-106
  • Kimura S, Naito H, Segawa H, NS-187, a potent and selective dual Bcr-Abl/Lyn tyrosine kinase inhibitor, is a novel agent for imatinib-resistant leukemia. Blood 2005;106:3948-54
  • Kadia T, Delioukina ML, Kantarjian HM, A pilot phase II study of the Lyn kinase inhibitor bafetinib in patients with relapsed or refractory B cell chronic lymphocytic leukemia [abstract 2858]. Blood 2011;118:1232
  • Lee M. Raf-1 kinase activation is uncoupled from downstream MEK/ERK pathway in cells treated with Src tyrosine kinase inhibitor PP2. Biochem Biophys Res Commun 2006;350:450-6
  • Congleton J, Macdonald R, Yen A. Src inhibitors, PP2 and dasatinib, increase retinoic acid-induced association of Lyn and c-Raf (S259) and enhance MAPK dependent differentiation of myeloid leukemia cells. Leukemia 2011; doi: 10.1038/leu.2011.390.
  • Lee M, Ahn J-H, Eum K-H. The difference in biological properties between parental and v-Ha-ras transformed NIH3T3 cells. Cancer Res Treat 2009;41:93-9
  • Dos Santos C, Demur C, Bardet V, A critical role for Lyn in acute myeloid leukemia. Blood 2008;111:2269-79
  • Contri A, Brunati AM, Trentin L, Chronic lymphocytic leukemia B cells contain anomalous Lyn tyrosine kinase, a putative contribution to defective apoptosis. J Clin Invest 2005;115:369-78
  • Ungefroren H, Sebens S, Groth S, The Src family kinase inhibitors PP2 and PP1 block TGF-beta1-mediated cellular responses by direct and differential inhibition of type I and type II TGF-beta receptors. Curr Cancer Drug Targets 2011;11:524-35
  • Blake RA, Broome MA, Liu X, SU6656, a selective Src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol 2000;20:9018-27
  • Watzlawik J, Holicky E, Edberg DD, Human remyelination promoting antibody inhibits apoptotic signaling and differentiation through Lyn kinase in primary rat oligodendrocytes. Glia 2010;58:1782-93
  • Dussault N, Simard C, Neron S, Cote S. Human B lymphocytes and non-Hodgkin's lymphoma cells become polyploid in response to the protein kinase inhibitor SU6656. Blood Cells Mol Dis 2007;39:130-4
  • Cuneo KC, Geng L, Tan J, SRC family kinase inhibitor SU6656 enhances antiangiogenic effect of irradiation. Int J Radiat Oncol Biol Phys 2006;64:1197-203
  • Green TP, Fennell M, Whittaker R, Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol Oncol 2009;3:248-61
  • Hennequin LF, Allen J, Breed J, N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J Med Chem 2006;49:6465-88
  • Takai S, Sabzevari H, Farsaci B, Distinct effects of saracatinib on memory CD8+ T cell differentiation. J Immunol 2012; Epub ahead of print
  • Ngo HT, Azab AK, Farag M, Src tyrosine kinase regulates adhesion and chemotaxis in Waldenstrom macroglobulinemia. Clin Cancer Res 2009;15:6035-41
  • Baselga J, Cervantes A, Martinelli E, Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors. Clin Cancer Res 2010;16:4876-83
  • Anbalagan M, Carrier L, Glodowski S, KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor alpha positive breast cancer. Breast Cancer Res Treat 2012;132:391-409
  • Anbalagan M, Carrier L, Hangauer D, KX-01, a novel Src kinase inhibitor directed towards the peptide substrate site, induces robust apoptosis and synergizes with tamoxifen and chemotherapy in breast cancer [abstract]. Cancer Res 2009;69(Suppl 3): doi: 10.1158/0008-5472.SABCS-09-6104.
  • Warmuth M, Simon N, Mitina O, Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases. Blood 2003;10:664-72
  • Morinaga K, Yamauchi T, Kimura S. Overcoming imatinib resistance using Src inhibitor CGP76030, Abl inhibitor nilotinib and Abl/Lyn inhibitor INNO-406 in newly established K562 variants with BCR-ABL gene amplification. Int J Cancer 2008;122:2621-7
  • Tauzin S, Ding H, Burdevet D, Membrane-associated signaling in human B-lymphoma lines. Exp Cell Res 2011;317:151-62
  • Recchia I, Rucci N, Funari A, Reduction of c-Src activity by substituted 5,7-diphenyl-pyrrolo[2,3-d]-pyrimidines induces osteoclast apoptosis in vivo and in vitro. Involvement of ERK1/2 pathway. Bone 2004;34:65-79
  • Rucci N, Susa M, Teti A. Inhibition of protein kinase c-Src as a therapeutic approach for and bone metastases. Anticancer Agents Med Chem 2008;8:342-9
  • Missbach M, Jeschke M, Feyen J, Novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo. Bone 1999;24:437-49
  • Zhang Q, Fairchild RL, Reich MB, Miller GG. Inhibition of Src kinases combined with CD40 ligand blockade prolongs murine cardiac allograft survival. Transplantation 2005;80:1112-20
  • Cortes JE, Kantarjian HM, Brummendorf TH, Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive chronic myeloid leukemia patients with resistance or intolerance to imatinib. Blood 2011;118:4567-76
  • Ghosh AK, Secrto C, Boysen J, The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy. Blood 2011;117:1928-37
  • Cetkovic-Cvrlje M, Uckun FM. Dual targeting of Bruton's tyrosine kinase and Janus kinase 3 with rationally designed inhibitors prevents graft-versus-host disease (GVHD) in a murine allogeneic bone marrow transplantation model. Br J Haematol 2004;126:821-7

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