-
1
-
-
84876249574
-
MEK and the inhibitors: From bench to bedside
-
Akinleye, A., Furqan, M.,Mukhi, N., Ravella, P.&Liu, D.MEK and the inhibitors: from bench to bedside. J. Hematol. Oncol. 6, 27 (2013).
-
(2013)
J. Hematol. Oncol.
, vol.6
, Issue.27
-
-
Akinleye, A.1
Furqan, M.2
Mukhi, N.3
Ravella, P.4
Liu, D.5
-
2
-
-
79955980366
-
C-Raf, but not B-Raf, is essential for development of K-Ras oncogene-driven non-small cell lung carcinoma
-
Blasco, R. B. et al. c-Raf, but not B-Raf, is essential for development of K-Ras oncogene-driven non-small cell lung carcinoma. Cancer Cell 19, 652-663 (2011).
-
(2011)
Cancer Cell
, vol.19
, pp. 652-663
-
-
Blasco, R.B.1
-
3
-
-
18444374405
-
Mutations of the BRAF gene in human cancer
-
Davies, H. et al. Mutations of the BRAF gene in human cancer. Nature 417, 949-954 (2002).
-
(2002)
Nature
, vol.417
, pp. 949-954
-
-
Davies, H.1
-
4
-
-
0037264633
-
Targeting RAS signalling pathways in cancer therapy
-
Downward, J. Targeting RAS signalling pathways in cancer therapy. Nature Rev. Cancer 3, 11-22 (2003).
-
(2003)
Nature Rev. Cancer
, vol.3
, pp. 11-22
-
-
Downward, J.1
-
5
-
-
3843084078
-
The COSMIC (Catalogue of Somatic Mutations in Cancer) database and website
-
Bamford, S. et al. The COSMIC (Catalogue of Somatic Mutations in Cancer) database and website. Br. J. Cancer 91, 355-358 (2004).
-
(2004)
Br. J. Cancer
, vol.91
, pp. 355-358
-
-
Bamford, S.1
-
6
-
-
77949685981
-
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
-
Hatzivassiliou, G. et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464, 431-435 (2010).
-
(2010)
Nature
, vol.464
, pp. 431-435
-
-
Hatzivassiliou, G.1
-
7
-
-
74849109743
-
Kinase-deadBRAF andoncogenicRAS cooperate to drive tumor progression through CRAF
-
Heidorn, S. J. et al. Kinase-deadBRAF andoncogenicRAS cooperate to drive tumor progression through CRAF. Cell 140, 209-221 (2010).
-
(2010)
Cell
, vol.140
, pp. 209-221
-
-
Heidorn, S.J.1
-
8
-
-
77949732073
-
RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
-
Poulikakos, P. I., Zhang, C., Bollag, G., Shokat, K. M. & Rosen, N. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 464, 427-430 (2010).
-
(2010)
Nature
, vol.464
, pp. 427-430
-
-
Poulikakos, P.I.1
Zhang, C.2
Bollag, G.3
Shokat, K.M.4
Rosen, N.5
-
9
-
-
31144453233
-
BRAF mutation predicts sensitivity to MEK inhibition
-
Solit, D. B. et al. BRAF mutation predicts sensitivity to MEK inhibition. Nature 439, 358-362 (2006).
-
(2006)
Nature
, vol.439
, pp. 358-362
-
-
Solit, D.B.1
-
10
-
-
8444238236
-
The RAF proteins take centre stage
-
Wellbrock, C., Karasarides, M. & Marais, R. The RAF proteins take centre stage. Nature Rev. Mol. Cell Biol. 5, 875-885 (2004).
-
(2004)
Nature Rev. Mol. Cell Biol.
, vol.5
, pp. 875-885
-
-
Wellbrock, C.1
Karasarides, M.2
Marais, R.3
-
11
-
-
79951928689
-
Novel mitogen-activated protein kinase kinase inhibitors
-
Chapman, M. S. & Miner, J. N. Novel mitogen-activated protein kinase kinase inhibitors. Expert Opin. Investig. Drugs 20, 209-220 (2011).
-
(2011)
Expert Opin. Investig. Drugs
, vol.20
, pp. 209-220
-
-
Chapman, M.S.1
Miner, J.N.2
-
12
-
-
57349194139
-
Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers
-
Engelman, J. A. et al. Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nature Med. 14, 1351-1356 (2008).
-
(2008)
Nature Med.
, vol.14
, pp. 1351-1356
-
-
Engelman, J.A.1
-
13
-
-
79952261716
-
GSK1120212 (JTP-74057) (JTP-74057) is an inhibitor ofMEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition
-
is an inhibitor ofMEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin. Cancer Res. 17, 989-1000 (2011).
-
(2011)
Clin. Cancer Res.
, vol.17
, pp. 989-1000
-
-
Gilmartin, A.G.1
-
14
-
-
84855415767
-
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition
-
Hoeflich, K. P. et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 72, 210-219 (2012).
-
(2012)
Cancer Res.
, vol.72
, pp. 210-219
-
-
Hoeflich, K.P.1
-
15
-
-
51049113834
-
BRAF V600E disrupts AZD6244-induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins
-
Friday, B. B. et al. BRAF V600E disrupts AZD6244-induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins. Cancer Res. 68, 6145-6153 (2008).
-
(2008)
Cancer Res.
, vol.68
, pp. 6145-6153
-
-
Friday, B.B.1
-
16
-
-
63149194964
-
V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway
-
Pratilas, C. A. et al. V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway. Proc. Natl Acad. Sci. USA 106, 4519-4524 (2009).
-
(2009)
Proc. Natl Acad. Sci. USA
, vol.106
, pp. 4519-4524
-
-
Pratilas, C.A.1
-
17
-
-
0036837671
-
Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352
-
Delaney, A. M., Printen, J. A., Chen, H., Fauman, E. B.& Dudley, D. T. Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352. Mol. Cell. Biol. 22, 7593-7602 (2002).
-
(2002)
Mol. Cell. Biol.
, Issue.22
, pp. 7593-7602
-
-
Delaney, A.M.1
Printen, J.A.2
Chen, H.3
Fauman, E.B.4
Dudley, D.T.5
-
18
-
-
84861494447
-
Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions
-
Heald, R. A. et al. Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions. J. Med. Chem. 55, 4594-4604 (2012).
-
(2012)
J. Med. Chem.
, vol.55
, pp. 4594-4604
-
-
Heald, R.A.1
-
19
-
-
38149016915
-
Understanding organofluorine chemistry An introduction to the C-F bond
-
OHagan, D. Understanding organofluorine chemistry. An introduction to the C-F bond. Chem. Soc. Rev. 37, 308-319 (2008).
-
(2008)
Chem. Soc. Rev.
, vol.37
, pp. 308-319
-
-
Ohagan, D.1
-
20
-
-
0037424509
-
Negative regulation of MAPKK by phosphorylation of a conserved serine residue equivalent to Ser212 of MEK1
-
Gopalbhai, K. et al. Negative regulation of MAPKK by phosphorylation of a conserved serine residue equivalent to Ser212 of MEK1. J. Biol. Chem. 278, 8118-8125 (2003).
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 8118-8125
-
-
Gopalbhai, K.1
-
21
-
-
80052727104
-
Fully activatedMEK1 exhibits compromised affinity for binding of allosteric inhibitors U0126 and PD0325901
-
Sheth, P. R. et al. Fully activatedMEK1 exhibits compromised affinity for binding of allosteric inhibitors U0126 and PD0325901. Biochemistry 50, 7964-7976 (2011).
-
(2011)
Biochemistry
, vol.50
, pp. 7964-7976
-
-
Sheth, P.R.1
-
22
-
-
0032512423
-
Deuterium exchange mass spectrometry as a probe of protein kinase activation. Analysis of wild-type and constitutively activemutants of MAP kinase kinase-1
-
Resing, K. A. & Ahn, N. G. Deuterium exchange mass spectrometry as a probe of protein kinase activation. Analysis of wild-type and constitutively activemutants of MAP kinase kinase-1. Biochemistry 37, 463-475 (1998).
-
(1998)
Biochemistry
, vol.37
, pp. 463-475
-
-
Resing, K.A.1
Ahn, N.G.2
-
23
-
-
84861017745
-
Novel carboxamide-based allosteric MEK inhibitors: Discovery and optimization efforts toward XL518 (GDC-0973
-
Rice, K. D. et al. Novel carboxamide-based allosteric MEK inhibitors: discovery and optimization efforts toward XL518 (GDC-0973). ACS Med. Chem. Lett. 3, 416-421 (2012)
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 416-421
-
-
Rice, K.D.1
-
24
-
-
0028884033
-
PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo
-
Alessi, D. R., Cuenda, A., Cohen, P., Dudley, D. T. & Saltiel, A. R. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J. Biol. Chem. 270, 27489-27494 (1995).
-
(1995)
J. Biol. Chem.
, vol.270
, pp. 27489-27494
-
-
Alessi, D.R.1
Cuenda, A.2
Cohen, P.3
Dudley, D.T.4
Saltiel, A.R.5
-
25
-
-
15744380263
-
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
-
Ohren, J. F. et al. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nature Struct. Mol. Biol. 11, 1192-1197 (2004).
-
(2004)
Nature Struct. Mol. Biol.
, vol.11
, pp. 1192-1197
-
-
Ohren, J.F.1
-
26
-
-
29144462587
-
Wild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerization
-
Garnett, M. J., Rana, S., Paterson, H., Barford, D. & Marais, R. Wild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerization. Mol. Cell 20, 963-969 (2005).
-
(2005)
Mol. Cell
, vol.20
, pp. 963-969
-
-
Garnett, M.J.1
Rana, S.2
Paterson, H.3
Barford, D.4
Marais, R.5
-
27
-
-
84861885576
-
Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signaling
-
Ro ring, M. et al. Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 31, 2629-2647 (2012).
-
(2012)
EMBO J.
, vol.31
, pp. 2629-2647
-
-
Ro Ring, M.1
-
28
-
-
84859922941
-
A first-in-human phase 1 study to evaluate the MEK1/2 inhibitor GDC-0973 administered daily in patients with advanced solid tumors
-
Rosen, L. et al. A first-in-human phase 1 study to evaluate the MEK1/2 inhibitor GDC-0973 administered daily in patients with advanced solid tumors. Cancer Res. 71, 4716 (2011).
-
(2011)
Cancer Res.
, vol.71
, Issue.4716
-
-
Rosen, L.1
-
29
-
-
77957954252
-
Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor
-
Choo, E. F. et al. Preclinical disposition and pharmacokinetics- pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor. Xenobiotica 40, 751-762 (2010).
-
(2010)
Xenobiotica
, vol.40
, pp. 751-762
-
-
Choo, E.F.1
|