메뉴 건너뛰기




Volumn 12, Issue 5, 2017, Pages 1183-1187

Selective Downregulation of JAK2 and JAK3 by an ATP-Competitive pan-JAK Inhibitor

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATE; BENZYLOXYCARBONYLLEUCYLLEUCYLLEUCINAL; JANUS KINASE 2; JANUS KINASE 3; JANUS KINASE INHIBITOR; MESSENGER RNA; PROTEIN KINASE TYK2; STAT PROTEIN; JAK2 PROTEIN, HUMAN; PF 956980; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; PYRROLE DERIVATIVE;

EID: 85019578794     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/acschembio.7b00116     Document Type: Article
Times cited : (21)

References (53)
  • 1
    • 84996848891 scopus 로고    scopus 로고
    • Induced protein degradation: An emerging drug discovery paradigm
    • Lai, A. C. and Crews, C. M. (2017) Induced protein degradation: an emerging drug discovery paradigm Nat. Rev. Drug Discovery 16, 101-114 10.1038/nrd.2016.211
    • (2017) Nat. Rev. Drug Discovery , vol.16 , pp. 101-114
    • Lai, A.C.1    Crews, C.M.2
  • 4
    • 85006459403 scopus 로고    scopus 로고
    • Boc3Arg-linked ligands induce degradation by localizing target proteins to the 20S proteasome
    • Shi, Y., Long, M. J. C., Rosenberg, M. M., Li, S., Kobjack, A., Lessans, P., Coffey, R. T., and Hedstrom, L. (2016) Boc3Arg-linked ligands induce degradation by localizing target proteins to the 20S proteasome ACS Chem. Biol. 11, 3328-3337 10.1021/acschembio.6b00656
    • (2016) ACS Chem. Biol. , vol.11 , pp. 3328-3337
    • Shi, Y.1    Long, M.J.C.2    Rosenberg, M.M.3    Li, S.4    Kobjack, A.5    Lessans, P.6    Coffey, R.T.7    Hedstrom, L.8
  • 5
    • 0035289779 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski, C. A., Lombardo, F., Dominy, B. W., and Feeney, P. J. (2001) Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Delivery Rev. 46, 3-26 10.1016/S0169-409X(00)00129-0
    • (2001) Adv. Drug Delivery Rev. , vol.46 , pp. 3-26
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 6
    • 85016141998 scopus 로고    scopus 로고
    • Protein degradation by in-cell self-assembly of proteolysis targeting chimeras
    • Lebraud, H., Wright, D. J., Johnson, C. N., and Heightman, T. D. (2016) Protein degradation by in-cell self-assembly of proteolysis targeting chimeras ACS Cent. Sci. 2, 927-934 10.1021/acscentsci.6b00280
    • (2016) ACS Cent. Sci. , vol.2 , pp. 927-934
    • Lebraud, H.1    Wright, D.J.2    Johnson, C.N.3    Heightman, T.D.4
  • 7
    • 84939552495 scopus 로고    scopus 로고
    • Protein degradation: Prime time for PROTACS
    • Deshaies, R. J. (2015) Protein degradation: prime time for PROTACS Nat. Chem. Biol. 11, 634-635 10.1038/nchembio.1887
    • (2015) Nat. Chem. Biol. , vol.11 , pp. 634-635
    • Deshaies, R.J.1
  • 8
    • 84961285814 scopus 로고    scopus 로고
    • Small-molecule PROTACS: New approaches to protein degradation
    • Toure, M. and Crews, C. M. (2016) Small-molecule PROTACS: new approaches to protein degradation Angew. Chem., Int. Ed. 55, 1966-1973 10.1002/anie.201507978
    • (2016) Angew. Chem., Int. Ed. , vol.55 , pp. 1966-1973
    • Toure, M.1    Crews, C.M.2
  • 10
    • 84879098944 scopus 로고    scopus 로고
    • ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system
    • Polier, S., Samant, R. S., Clarke, P. A., Workman, P., Prodromou, C., and Pearl, L. H. (2013) ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system Nat. Chem. Biol. 9, 307-312 10.1038/nchembio.1212
    • (2013) Nat. Chem. Biol. , vol.9 , pp. 307-312
    • Polier, S.1    Samant, R.S.2    Clarke, P.A.3    Workman, P.4    Prodromou, C.5    Pearl, L.H.6
  • 13
    • 84988569312 scopus 로고    scopus 로고
    • Pharmacological LRRK2 kinase inhibition induces LRRK2 protein destabilization and proteasomal degradation
    • Lobbestael, E., Civiero, L., De Wit, T., Taymans, J.-M., Greggio, E., and Baekelandt, V. (2016) Pharmacological LRRK2 kinase inhibition induces LRRK2 protein destabilization and proteasomal degradation Sci. Rep. 6, 33897 10.1038/srep33897
    • (2016) Sci. Rep. , vol.6 , pp. 33897
    • Lobbestael, E.1    Civiero, L.2    De Wit, T.3    Taymans, J.-M.4    Greggio, E.5    Baekelandt, V.6
  • 14
    • 84935077167 scopus 로고    scopus 로고
    • LRRK2 dephosphorylation increases its ubiquitination
    • Zhao, J., Molitor, T. P., Langston, J. W., and Nichols, R. J. (2015) LRRK2 dephosphorylation increases its ubiquitination Biochem. J. 469, 107-120 10.1042/BJ20141305
    • (2015) Biochem. J. , vol.469 , pp. 107-120
    • Zhao, J.1    Molitor, T.P.2    Langston, J.W.3    Nichols, R.J.4
  • 16
    • 84891776413 scopus 로고    scopus 로고
    • Mutant LRRK2 toxicity in neurons depends on LRRK2 levels and synuclein but not kinase activity or inclusion bodies
    • Skibinski, G., Nakamura, K., Cookson, M. R., and Finkbeiner, S. (2014) Mutant LRRK2 toxicity in neurons depends on LRRK2 levels and synuclein but not kinase activity or inclusion bodies J. Neurosci. 34, 418-433 10.1523/JNEUROSCI.2712-13.2014
    • (2014) J. Neurosci. , vol.34 , pp. 418-433
    • Skibinski, G.1    Nakamura, K.2    Cookson, M.R.3    Finkbeiner, S.4
  • 19
    • 84903884326 scopus 로고    scopus 로고
    • Inhibition of the checkpoint kinase Chk1 induces DNA damage and cell death in human leukemia and lymphoma cells
    • Bryant, C., Scriven, K., and Massey, A. J. (2014) Inhibition of the checkpoint kinase Chk1 induces DNA damage and cell death in human leukemia and lymphoma cells Mol. Cancer 13, 147 10.1186/1476-4598-13-147
    • (2014) Mol. Cancer , vol.13 , pp. 147
    • Bryant, C.1    Scriven, K.2    Massey, A.J.3
  • 20
    • 84971619634 scopus 로고    scopus 로고
    • Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells
    • McNaughton, M., Pitman, M., Pitson, S. M., Pyne, N. J., and Pyne, S. (2016) Proteasomal degradation of sphingosine kinase 1 and inhibition of dihydroceramide desaturase by the sphingosine kinase inhibitors, SKi or ABC294640, induces growth arrest in androgen-independent LNCaP-AI prostate cancer cells Oncotarget 7, 16663-16675 10.18632/oncotarget.7693
    • (2016) Oncotarget , vol.7 , pp. 16663-16675
    • McNaughton, M.1    Pitman, M.2    Pitson, S.M.3    Pyne, N.J.4    Pyne, S.5
  • 23
  • 24
    • 84960894417 scopus 로고    scopus 로고
    • Janus kinase inhibitors for rheumatoid arthritis
    • Yamaoka, K. (2016) Janus kinase inhibitors for rheumatoid arthritis Curr. Opin. Chem. Biol. 32, 29-33 10.1016/j.cbpa.2016.03.006
    • (2016) Curr. Opin. Chem. Biol. , vol.32 , pp. 29-33
    • Yamaoka, K.1
  • 25
    • 40149094813 scopus 로고    scopus 로고
    • Inhibition of JAK1, 2/STAT3 signaling induces apoptosis, cell cycle arrest, and reduces tumor cell invasion in colorectal cancer cells
    • Xiong, H., Zhang, Z.-G., Tian, X.-Q., Sun, D.-F., Liang, Q.-C., Zhang, Y.-J., Lu, R., Chen, Y.-X., and Fang, J.-Y. (2008) Inhibition of JAK1, 2/STAT3 signaling induces apoptosis, cell cycle arrest, and reduces tumor cell invasion in colorectal cancer cells Neoplasia 10, 287-297 10.1593/neo.07971
    • (2008) Neoplasia , vol.10 , pp. 287-297
    • Xiong, H.1    Zhang, Z.-G.2    Tian, X.-Q.3    Sun, D.-F.4    Liang, Q.-C.5    Zhang, Y.-J.6    Lu, R.7    Chen, Y.-X.8    Fang, J.-Y.9
  • 26
    • 84866752972 scopus 로고    scopus 로고
    • Potency and selectivity assessment of small molecules against Janus kinase (JAK) 2: Widely used AG490 inhibitor is neither potent nor selective for JAK2
    • Sinclair, A., Archibeque, I., Zhan, J., Liu, L., Emkey, R., Doherty, E., and Begley, C. G. (2011) Potency and selectivity assessment of small molecules against Janus kinase (JAK) 2: widely used AG490 inhibitor is neither potent nor selective for JAK2 Blood 118, 4780
    • (2011) Blood , vol.118 , pp. 4780
    • Sinclair, A.1    Archibeque, I.2    Zhan, J.3    Liu, L.4    Emkey, R.5    Doherty, E.6    Begley, C.G.7
  • 27
    • 0029083427 scopus 로고
    • Inhibition of protein phosphorylation modulates expression of the Jak family protein tyrosine kinases
    • Fiorucci, G., Percario, Z. A., Marcolin, C., Coccia, E. M., Affabris, E., and Romeo, G. (1995) Inhibition of protein phosphorylation modulates expression of the Jak family protein tyrosine kinases J. Virol. 69, 5833-5837
    • (1995) J. Virol. , vol.69 , pp. 5833-5837
    • Fiorucci, G.1    Percario, Z.A.2    Marcolin, C.3    Coccia, E.M.4    Affabris, E.5    Romeo, G.6
  • 29
    • 61349149899 scopus 로고    scopus 로고
    • Dissecting specificity in the Janus kinases: The structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains
    • Williams, N. K., Bamert, R. S., Patel, O., Wang, C., Walden, P. M., Wilks, A. F., Fantino, E., Rossjohn, J., and Lucet, I. S. (2009) Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains J. Mol. Biol. 387, 219-232 10.1016/j.jmb.2009.01.041
    • (2009) J. Mol. Biol. , vol.387 , pp. 219-232
    • Williams, N.K.1    Bamert, R.S.2    Patel, O.3    Wang, C.4    Walden, P.M.5    Wilks, A.F.6    Fantino, E.7    Rossjohn, J.8    Lucet, I.S.9
  • 31
    • 78649457614 scopus 로고    scopus 로고
    • The JAK3-selective inhibitor PF-956980 reverses the resistance to cytotoxic agents induced by interleukin-4 treatment of chronic lymphocytic leukemia cells: Potential for reversal of cytoprotection by the microenvironment
    • Steele, A. J., Prentice, A. G., Cwynarski, K., Hoffbrand, A. V., Hart, S. M., Lowdell, M. W., Samuel, E. R., and Wickremasinghe, R. G. (2010) The JAK3-selective inhibitor PF-956980 reverses the resistance to cytotoxic agents induced by interleukin-4 treatment of chronic lymphocytic leukemia cells: potential for reversal of cytoprotection by the microenvironment Blood 116, 4569-4577 10.1182/blood-2009-09-245811
    • (2010) Blood , vol.116 , pp. 4569-4577
    • Steele, A.J.1    Prentice, A.G.2    Cwynarski, K.3    Hoffbrand, A.V.4    Hart, S.M.5    Lowdell, M.W.6    Samuel, E.R.7    Wickremasinghe, R.G.8
  • 33
    • 84891942459 scopus 로고    scopus 로고
    • Interleukin-4 induces up-regulation of endothelial cell claudin-5 through activation of FoxO1: Role in protection from complement-mediated injury
    • Dalmasso, A. P., Goldish, D., Benson, B. A., Tsai, A. K., Wasiluk, K. R., and Vercellotti, G. M. (2014) Interleukin-4 induces up-regulation of endothelial cell claudin-5 through activation of FoxO1: role in protection from complement-mediated injury J. Biol. Chem. 289, 838-847 10.1074/jbc.M113.455766
    • (2014) J. Biol. Chem. , vol.289 , pp. 838-847
    • Dalmasso, A.P.1    Goldish, D.2    Benson, B.A.3    Tsai, A.K.4    Wasiluk, K.R.5    Vercellotti, G.M.6
  • 37
    • 50949110014 scopus 로고    scopus 로고
    • IL-7 activates the phosphatidylinositol 3-kinase/AKT pathway in normal human thymocytes but not normal human B cell precursors
    • Johnson, S. E., Shah, N. P., Bajer, A. A., and LeBien, T. W. (2008) IL-7 activates the phosphatidylinositol 3-kinase/AKT pathway in normal human thymocytes but not normal human B cell precursors J. Immunol. 180, 8109-8117 10.4049/jimmunol.180.12.8109
    • (2008) J. Immunol. , vol.180 , pp. 8109-8117
    • Johnson, S.E.1    Shah, N.P.2    Bajer, A.A.3    LeBien, T.W.4
  • 40
    • 85019584518 scopus 로고    scopus 로고
    • Discovery of selective dual inhibitors of bromodomain protein BRD4 and JAK2 for treatment of hematologic malignancies
    • Upadhayaya, R. S., Kethiri, R. R., Vellanki, A., Lightfoot, J., Local, A., and Rice, W. G. (2016) Discovery of selective dual inhibitors of bromodomain protein BRD4 and JAK2 for treatment of hematologic malignancies Blood 128, 5212
    • (2016) Blood , vol.128 , pp. 5212
    • Upadhayaya, R.S.1    Kethiri, R.R.2    Vellanki, A.3    Lightfoot, J.4    Local, A.5    Rice, W.G.6
  • 41
    • 84899936534 scopus 로고    scopus 로고
    • Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors
    • Ember, S. W. J., Zhu, J.-Y., Olesen, S. H., Martin, M. P., Becker, A., Berndt, N., Georg, G. I., and Schönbrunn, E. (2014) Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors ACS Chem. Biol. 9, 1160-1171 10.1021/cb500072z
    • (2014) ACS Chem. Biol. , vol.9 , pp. 1160-1171
    • Ember, S.W.J.1    Zhu, J.-Y.2    Olesen, S.H.3    Martin, M.P.4    Becker, A.5    Berndt, N.6    Georg, G.I.7    Schönbrunn, E.8
  • 44
    • 84991554797 scopus 로고    scopus 로고
    • Trypan blue exclusion test of cell viability
    • Strober, W. (2015) Trypan blue exclusion test of cell viability Curr. Protoc. Immunol. 111, A3.B.1-3 10.1002/0471142735.ima03bs111
    • (2015) Curr. Protoc. Immunol. , vol.111 , pp. A3-B13
    • Strober, W.1
  • 45
    • 84900789855 scopus 로고    scopus 로고
    • Chemotypes sensitivity and predictivity of in vivo outcomes for cytotoxic assays in THLE and HepG2 cell lines
    • Shah, F., Louise-May, S., and Greene, N. (2014) Chemotypes sensitivity and predictivity of in vivo outcomes for cytotoxic assays in THLE and HepG2 cell lines Bioorg. Med. Chem. Lett. 24, 2753-2757 10.1016/j.bmcl.2014.04.039
    • (2014) Bioorg. Med. Chem. Lett. , vol.24 , pp. 2753-2757
    • Shah, F.1    Louise-May, S.2    Greene, N.3
  • 46
    • 84961722011 scopus 로고    scopus 로고
    • Essential biphasic role for JAK3 catalytic activity in IL-2 receptor signaling
    • Smith, G. A., Uchida, K., Weiss, A., and Taunton, J. (2016) Essential biphasic role for JAK3 catalytic activity in IL-2 receptor signaling Nat. Chem. Biol. 12, 373-379 10.1038/nchembio.2056
    • (2016) Nat. Chem. Biol. , vol.12 , pp. 373-379
    • Smith, G.A.1    Uchida, K.2    Weiss, A.3    Taunton, J.4
  • 47
    • 84897020107 scopus 로고    scopus 로고
    • Important scaffold function of the Janus kinase 2 uncovered by a novel mouse model harboring a Jak2 activation-loop mutation
    • Keil, E., Finkenstädt, D., Wufka, C., Trilling, M., Liebfried, P., Strobl, B., Müller, M., and Pfeffer, K. (2014) Important scaffold function of the Janus kinase 2 uncovered by a novel mouse model harboring a Jak2 activation-loop mutation Blood 123, 520-529 10.1182/blood-2013-03-492157
    • (2014) Blood , vol.123 , pp. 520-529
    • Keil, E.1    Finkenstädt, D.2    Wufka, C.3    Trilling, M.4    Liebfried, P.5    Strobl, B.6    Müller, M.7    Pfeffer, K.8
  • 49
    • 73949136283 scopus 로고    scopus 로고
    • Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells
    • Wang, Y., Fiskus, W., Chong, D. G., Buckley, K. M., Natarajan, K., Rao, R., Joshi, A., Balusu, R., Koul, S., Chen, J., Savoie, A., Ustun, C., Jillella, A. P., Atadja, P., Levine, R. L., and Bhalla, K. N. (2009) Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells Blood 114, 5024-5033 10.1182/blood-2009-05-222133
    • (2009) Blood , vol.114 , pp. 5024-5033
    • Wang, Y.1    Fiskus, W.2    Chong, D.G.3    Buckley, K.M.4    Natarajan, K.5    Rao, R.6    Joshi, A.7    Balusu, R.8    Koul, S.9    Chen, J.10    Savoie, A.11    Ustun, C.12    Jillella, A.P.13    Atadja, P.14    Levine, R.L.15    Bhalla, K.N.16


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.