-
1
-
-
77956513286
-
Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
-
Bollag, G., Hirth, P., Tsai, J., Zhang, J., Ibrahim, P.N., Cho, H., Spevak, W., Zhang, C., Zhang, Y., Habets, G., et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 467 (2010), 596–599.
-
(2010)
Nature
, vol.467
, pp. 596-599
-
-
Bollag, G.1
Hirth, P.2
Tsai, J.3
Zhang, J.4
Ibrahim, P.N.5
Cho, H.6
Spevak, W.7
Zhang, C.8
Zhang, Y.9
Habets, G.10
-
2
-
-
79959795786
-
Improved survival with vemurafenib in melanoma with BRAF V600E mutation
-
Chapman, P.B., Hauschild, A., Robert, C., Haanen, J.B., Ascierto, P., Larkin, J., Dummer, R., Garbe, C., Testori, A., Maio, M., et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N. Engl. J. Med. 364 (2011), 2507–2516.
-
(2011)
N. Engl. J. Med.
, vol.364
, pp. 2507-2516
-
-
Chapman, P.B.1
Hauschild, A.2
Robert, C.3
Haanen, J.B.4
Ascierto, P.5
Larkin, J.6
Dummer, R.7
Garbe, C.8
Testori, A.9
Maio, M.10
-
3
-
-
84960131814
-
Oncogenic BRAF deletions that function as homodimers and are sensitive to inhibition by RAF dimer inhibitor LY3009120
-
Chen, S.H., Zhang, Y., Van Horn, R.D., Yin, T., Buchanan, S., Yadav, V., Mochalkin, I., Wong, S.S., Yue, Y.G., Huber, L., et al. Oncogenic BRAF deletions that function as homodimers and are sensitive to inhibition by RAF dimer inhibitor LY3009120. Cancer Discov. 6 (2016), 300–315.
-
(2016)
Cancer Discov.
, vol.6
, pp. 300-315
-
-
Chen, S.H.1
Zhang, Y.2
Van Horn, R.D.3
Yin, T.4
Buchanan, S.5
Yadav, V.6
Mochalkin, I.7
Wong, S.S.8
Yue, Y.G.9
Huber, L.10
-
4
-
-
80053307869
-
Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers
-
Corcoran, R.B., Settleman, J., Engelman, J.A., Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers. Oncotarget 2 (2011), 336–346.
-
(2011)
Oncotarget
, vol.2
, pp. 336-346
-
-
Corcoran, R.B.1
Settleman, J.2
Engelman, J.A.3
-
5
-
-
84861863158
-
EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib
-
Corcoran, R.B., Ebi, H., Turke, A.B., Coffee, E.M., Nishino, M., Cogdill, A.P., Brown, R.D., Della Pelle, P., Dias-Santagata, D., Hung, K.E., et al. EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib. Cancer Discov. 2 (2012), 227–235.
-
(2012)
Cancer Discov.
, vol.2
, pp. 227-235
-
-
Corcoran, R.B.1
Ebi, H.2
Turke, A.B.3
Coffee, E.M.4
Nishino, M.5
Cogdill, A.P.6
Brown, R.D.7
Della Pelle, P.8
Dias-Santagata, D.9
Hung, K.E.10
-
6
-
-
18444374405
-
Mutations of the BRAF gene in human cancer
-
Davies, H., Bignell, G.R., Cox, C., Stephens, P., Edkins, S., Clegg, S., Teague, J., Woffendin, H., Garnett, M.J., Bottomley, W., et al. Mutations of the BRAF gene in human cancer. Nature 417 (2002), 949–954.
-
(2002)
Nature
, vol.417
, pp. 949-954
-
-
Davies, H.1
Bignell, G.R.2
Cox, C.3
Stephens, P.4
Edkins, S.5
Clegg, S.6
Teague, J.7
Woffendin, H.8
Garnett, M.J.9
Bottomley, W.10
-
7
-
-
84861083983
-
Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial
-
Falchook, G.S., Long, G.V., Kurzrock, R., Kim, K.B., Arkenau, T.H., Brown, M.P., Hamid, O., Infante, J.R., Millward, M., Pavlick, A.C., et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 379 (2012), 1893–1901.
-
(2012)
Lancet
, vol.379
, pp. 1893-1901
-
-
Falchook, G.S.1
Long, G.V.2
Kurzrock, R.3
Kim, K.B.4
Arkenau, T.H.5
Brown, M.P.6
Hamid, O.7
Infante, J.R.8
Millward, M.9
Pavlick, A.C.10
-
8
-
-
77956030786
-
Inhibition of mutated, activated BRAF in metastatic melanoma
-
Flaherty, K.T., Puzanov, I., Kim, K.B., Ribas, A., McArthur, G.A., Sosman, J.A., O'Dwyer, P.J., Lee, R.J., Grippo, J.F., Nolop, K., et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N. Engl. J. Med. 363 (2010), 809–819.
-
(2010)
N. Engl. J. Med.
, vol.363
, pp. 809-819
-
-
Flaherty, K.T.1
Puzanov, I.2
Kim, K.B.3
Ribas, A.4
McArthur, G.A.5
Sosman, J.A.6
O'Dwyer, P.J.7
Lee, R.J.8
Grippo, J.F.9
Nolop, K.10
-
9
-
-
84961219427
-
Activation mechanism of oncogenic deletion mutations in BRAF, EGFR, and HER2
-
Foster, S.A., Whalen, D.M., Ozen, A., Wongchenko, M.J., Yin, J., Yen, I., Schaefer, G., Mayfield, J.D., Chmielecki, J., Stephens, P.J., et al. Activation mechanism of oncogenic deletion mutations in BRAF, EGFR, and HER2. Cancer Cell 29 (2016), 477–493.
-
(2016)
Cancer Cell
, vol.29
, pp. 477-493
-
-
Foster, S.A.1
Whalen, D.M.2
Ozen, A.3
Wongchenko, M.J.4
Yin, J.5
Yen, I.6
Schaefer, G.7
Mayfield, J.D.8
Chmielecki, J.9
Stephens, P.J.10
-
10
-
-
84874225181
-
Effects of Raf dimerization and its inhibition on normal and disease-associated Raf signaling
-
Freeman, A.K., Ritt, D.A., Morrison, D.K., Effects of Raf dimerization and its inhibition on normal and disease-associated Raf signaling. Mol. Cell 49 (2013), 751–758.
-
(2013)
Mol. Cell
, vol.49
, pp. 751-758
-
-
Freeman, A.K.1
Ritt, D.A.2
Morrison, D.K.3
-
11
-
-
84922223009
-
Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma
-
Girotti, M.R., Lopes, F., Preece, N., Niculescu-Duvaz, D., Zambon, A., Davies, L., Whittaker, S., Saturno, G., Viros, A., Pedersen, M., et al. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell 27 (2015), 85–96.
-
(2015)
Cancer Cell
, vol.27
, pp. 85-96
-
-
Girotti, M.R.1
Lopes, F.2
Preece, N.3
Niculescu-Duvaz, D.4
Zambon, A.5
Davies, L.6
Whittaker, S.7
Saturno, G.8
Viros, A.9
Pedersen, M.10
-
12
-
-
77949354563
-
PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells
-
Halaban, R., Zhang, W., Bacchiocchi, A., Cheng, E., Parisi, F., Ariyan, S., Krauthammer, M., McCusker, J.P., Kluger, Y., Sznol, M., PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. Pigment Cell Melanoma Res. 23 (2010), 190–200.
-
(2010)
Pigment Cell Melanoma Res.
, vol.23
, pp. 190-200
-
-
Halaban, R.1
Zhang, W.2
Bacchiocchi, A.3
Cheng, E.4
Parisi, F.5
Ariyan, S.6
Krauthammer, M.7
McCusker, J.P.8
Kluger, Y.9
Sznol, M.10
-
13
-
-
84908664886
-
Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling
-
Haling, J.R., Sudhamsu, J., Yen, I., Sideris, S., Sandoval, W., Phung, W., Bravo, B.J., Giannetti, A.M., Peck, A., Masselot, A., et al. Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling. Cancer Cell 26 (2014), 402–413.
-
(2014)
Cancer Cell
, vol.26
, pp. 402-413
-
-
Haling, J.R.1
Sudhamsu, J.2
Yen, I.3
Sideris, S.4
Sandoval, W.5
Phung, W.6
Bravo, B.J.7
Giannetti, A.M.8
Peck, A.9
Masselot, A.10
-
14
-
-
77949685981
-
RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
-
Hatzivassiliou, G., Song, K., Yen, I., Brandhuber, B.J., Anderson, D.J., Alvarado, R., Ludlam, M.J., Stokoe, D., Gloor, S.L., Vigers, G., et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464 (2010), 431–435.
-
(2010)
Nature
, vol.464
, pp. 431-435
-
-
Hatzivassiliou, G.1
Song, K.2
Yen, I.3
Brandhuber, B.J.4
Anderson, D.J.5
Alvarado, R.6
Ludlam, M.J.7
Stokoe, D.8
Gloor, S.L.9
Vigers, G.10
-
15
-
-
84884127318
-
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
-
Hatzivassiliou, G., Haling, J.R., Chen, H., Song, K., Price, S., Heald, R., Hewitt, J.F., Zak, M., Peck, A., Orr, C., et al. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature 501 (2013), 232–236.
-
(2013)
Nature
, vol.501
, pp. 232-236
-
-
Hatzivassiliou, G.1
Haling, J.R.2
Chen, H.3
Song, K.4
Price, S.5
Heald, R.6
Hewitt, J.F.7
Zak, M.8
Peck, A.9
Orr, C.10
-
16
-
-
84864285704
-
Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial
-
Hauschild, A., Grob, J.J., Demidov, L.V., Jouary, T., Gutzmer, R., Millward, M., Rutkowski, P., Blank, C.U., Miller, W.H. Jr., Kaempgen, E., et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial. Lancet 380 (2012), 358–365.
-
(2012)
Lancet
, vol.380
, pp. 358-365
-
-
Hauschild, A.1
Grob, J.J.2
Demidov, L.V.3
Jouary, T.4
Gutzmer, R.5
Millward, M.6
Rutkowski, P.7
Blank, C.U.8
Miller, W.H.9
Kaempgen, E.10
-
17
-
-
74849109743
-
Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF
-
Heidorn, S.J., Milagre, C., Whittaker, S., Nourry, A., Niculescu-Duvas, I., Dhomen, N., Hussain, J., Reis-Filho, J.S., Springer, C.J., Pritchard, C., et al. Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell 140 (2010), 209–221.
-
(2010)
Cell
, vol.140
, pp. 209-221
-
-
Heidorn, S.J.1
Milagre, C.2
Whittaker, S.3
Nourry, A.4
Niculescu-Duvas, I.5
Dhomen, N.6
Hussain, J.7
Reis-Filho, J.S.8
Springer, C.J.9
Pritchard, C.10
-
18
-
-
66149126085
-
Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression
-
Hoeflich, K.P., Herter, S., Tien, J., Wong, L., Berry, L., Chan, J., O'Brien, C., Modrusan, Z., Seshagiri, S., Lackner, M., et al. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Cancer Res. 69 (2009), 3042–3051.
-
(2009)
Cancer Res.
, vol.69
, pp. 3042-3051
-
-
Hoeflich, K.P.1
Herter, S.2
Tien, J.3
Wong, L.4
Berry, L.5
Chan, J.6
O'Brien, C.7
Modrusan, Z.8
Seshagiri, S.9
Lackner, M.10
-
19
-
-
84877825519
-
RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation
-
Holderfield, M., Merritt, H., Chan, J., Wallroth, M., Tandeske, L., Zhai, H., Tellew, J., Hardy, S., Hekmat-Nejad, M., Stuart, D.D., et al. RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation. Cancer Cell 23 (2013), 594–602.
-
(2013)
Cancer Cell
, vol.23
, pp. 594-602
-
-
Holderfield, M.1
Merritt, H.2
Chan, J.3
Wallroth, M.4
Tandeske, L.5
Zhai, H.6
Tellew, J.7
Hardy, S.8
Hekmat-Nejad, M.9
Stuart, D.D.10
-
20
-
-
77957089182
-
The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner
-
Joseph, E.W., Pratilas, C.A., Poulikakos, P.I., Tadi, M., Wang, W., Taylor, B.S., Halilovic, E., Persaud, Y., Xing, F., Viale, A., et al. The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc. Natl. Acad. Sci. USA 107 (2010), 14903–14908.
-
(2010)
Proc. Natl. Acad. Sci. USA
, vol.107
, pp. 14903-14908
-
-
Joseph, E.W.1
Pratilas, C.A.2
Poulikakos, P.I.3
Tadi, M.4
Wang, W.5
Taylor, B.S.6
Halilovic, E.7
Persaud, Y.8
Xing, F.9
Viale, A.10
-
21
-
-
33845730781
-
Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885
-
King, A.J., Patrick, D.R., Batorsky, R.S., Ho, M.L., Do, H.T., Zhang, S.Y., Kumar, R., Rusnak, D.W., Takle, A.K., Wilson, D.M., et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 66 (2006), 11100–11105.
-
(2006)
Cancer Res.
, vol.66
, pp. 11100-11105
-
-
King, A.J.1
Patrick, D.R.2
Batorsky, R.S.3
Ho, M.L.4
Do, H.T.5
Zhang, S.Y.6
Kumar, R.7
Rusnak, D.W.8
Takle, A.K.9
Wilson, D.M.10
-
22
-
-
84879422871
-
Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization
-
Lavoie, H., Thevakumaran, N., Gavory, G., Li, J.J., Padeganeh, A., Guiral, S., Duchaine, J., Mao, D.Y., Bouvier, M., Sicheri, F., et al. Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization. Nat. Chem. Biol. 9 (2013), 428–436.
-
(2013)
Nat. Chem. Biol.
, vol.9
, pp. 428-436
-
-
Lavoie, H.1
Thevakumaran, N.2
Gavory, G.3
Li, J.J.4
Padeganeh, A.5
Guiral, S.6
Duchaine, J.7
Mao, D.Y.8
Bouvier, M.9
Sicheri, F.10
-
23
-
-
79960064432
-
Raf family kinases: old dogs have learned new tricks
-
Matallanas, D., Birtwistle, M., Romano, D., Zebisch, A., Rauch, J., von Kriegsheim, A., Kolch, W., Raf family kinases: old dogs have learned new tricks. Genes Cancer 2 (2011), 232–260.
-
(2011)
Genes Cancer
, vol.2
, pp. 232-260
-
-
Matallanas, D.1
Birtwistle, M.2
Romano, D.3
Zebisch, A.4
Rauch, J.5
von Kriegsheim, A.6
Kolch, W.7
-
24
-
-
38049097938
-
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling
-
McDermott, U., Sharma, S.V., Dowell, L., Greninger, P., Montagut, C., Lamb, J., Archibald, H., Raudales, R., Tam, A., Lee, D., et al. Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc. Natl. Acad. Sci. USA 104 (2007), 19936–19941.
-
(2007)
Proc. Natl. Acad. Sci. USA
, vol.104
, pp. 19936-19941
-
-
McDermott, U.1
Sharma, S.V.2
Dowell, L.3
Greninger, P.4
Montagut, C.5
Lamb, J.6
Archibald, H.7
Raudales, R.8
Tam, A.9
Lee, D.10
-
25
-
-
84877631604
-
Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas
-
Montero-Conde, C., Ruiz-Llorente, S., Dominguez, J.M., Knauf, J.A., Viale, A., Sherman, E.J., Ryder, M., Ghossein, R.A., Rosen, N., Fagin, J.A., Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas. Cancer Discov. 3 (2013), 520–533.
-
(2013)
Cancer Discov.
, vol.3
, pp. 520-533
-
-
Montero-Conde, C.1
Ruiz-Llorente, S.2
Dominguez, J.M.3
Knauf, J.A.4
Viale, A.5
Sherman, E.J.6
Ryder, M.7
Ghossein, R.A.8
Rosen, N.9
Fagin, J.A.10
-
26
-
-
84890284472
-
Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma
-
Nakamura, A., Arita, T., Tsuchiya, S., Donelan, J., Chouitar, J., Carideo, E., Galvin, K., Okaniwa, M., Ishikawa, T., Yoshida, S., Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res. 73 (2013), 7043–7055.
-
(2013)
Cancer Res.
, vol.73
, pp. 7043-7055
-
-
Nakamura, A.1
Arita, T.2
Tsuchiya, S.3
Donelan, J.4
Chouitar, J.5
Carideo, E.6
Galvin, K.7
Okaniwa, M.8
Ishikawa, T.9
Yoshida, S.10
-
27
-
-
78650303507
-
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
-
Nazarian, R., Shi, H., Wang, Q., Kong, X., Koya, R.C., Lee, H., Chen, Z., Lee, M.K., Attar, N., Sazegar, H., et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 468 (2010), 973–977.
-
(2010)
Nature
, vol.468
, pp. 973-977
-
-
Nazarian, R.1
Shi, H.2
Wang, Q.3
Kong, X.4
Koya, R.C.5
Lee, H.6
Chen, Z.7
Lee, M.K.8
Attar, N.9
Sazegar, H.10
-
28
-
-
84883173554
-
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives
-
Okaniwa, M., Hirose, M., Arita, T., Yabuki, M., Nakamura, A., Takagi, T., Kawamoto, T., Uchiyama, N., Sumita, A., Tsutsumi, S., et al. Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J. Med. Chem. 56 (2013), 6478–6494.
-
(2013)
J. Med. Chem.
, vol.56
, pp. 6478-6494
-
-
Okaniwa, M.1
Hirose, M.2
Arita, T.3
Yabuki, M.4
Nakamura, A.5
Takagi, T.6
Kawamoto, T.7
Uchiyama, N.8
Sumita, A.9
Tsutsumi, S.10
-
29
-
-
84942323259
-
Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers
-
Peng, S.B., Henry, J.R., Kaufman, M.D., Lu, W.P., Smith, B.D., Vogeti, S., Rutkoski, T.J., Wise, S., Chun, L., Zhang, Y., et al. Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers. Cancer Cell 28 (2015), 384–398.
-
(2015)
Cancer Cell
, vol.28
, pp. 384-398
-
-
Peng, S.B.1
Henry, J.R.2
Kaufman, M.D.3
Lu, W.P.4
Smith, B.D.5
Vogeti, S.6
Rutkoski, T.J.7
Wise, S.8
Chun, L.9
Zhang, Y.10
-
30
-
-
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 (2010), 427–430.
-
(2010)
Nature
, vol.464
, pp. 427-430
-
-
Poulikakos, P.I.1
Zhang, C.2
Bollag, G.3
Shokat, K.M.4
Rosen, N.5
-
31
-
-
83455254767
-
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
-
Poulikakos, P.I., Persaud, Y., Janakiraman, M., Kong, X., Ng, C., Moriceau, G., Shi, H., Atefi, M., Titz, B., Gabay, M.T., et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 480 (2011), 387–390.
-
(2011)
Nature
, vol.480
, pp. 387-390
-
-
Poulikakos, P.I.1
Persaud, Y.2
Janakiraman, M.3
Kong, X.4
Ng, C.5
Moriceau, G.6
Shi, H.7
Atefi, M.8
Titz, B.9
Gabay, M.T.10
-
32
-
-
84863230465
-
Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR
-
Prahallad, A., Sun, C., Huang, S., Di Nicolantonio, F., Salazar, R., Zecchin, D., Beijersbergen, R.L., Bardelli, A., Bernards, R., Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 483 (2012), 100–103.
-
(2012)
Nature
, vol.483
, pp. 100-103
-
-
Prahallad, A.1
Sun, C.2
Huang, S.3
Di Nicolantonio, F.4
Salazar, R.5
Zecchin, D.6
Beijersbergen, R.L.7
Bardelli, A.8
Bernards, R.9
-
33
-
-
70349438995
-
A dimerization-dependent mechanism drives RAF catalytic activation
-
Rajakulendran, T., Sahmi, M., Lefrancois, M., Sicheri, F., Therrien, M., A dimerization-dependent mechanism drives RAF catalytic activation. Nature 461 (2009), 542–545.
-
(2009)
Nature
, vol.461
, pp. 542-545
-
-
Rajakulendran, T.1
Sahmi, M.2
Lefrancois, M.3
Sicheri, F.4
Therrien, M.5
-
34
-
-
84875186930
-
Discovery of dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B-Raf-Driven tumors
-
Rheault, T.R., Stellwagen, J.C., Adjabeng, G.M., Hornberger, K.R., Petrov, K.G., Waterson, A.G., Dickerson, S.H., Mook, R.A. Jr., Laquerre, S.G., King, A.J., et al. Discovery of dabrafenib: a selective inhibitor of Raf kinases with antitumor activity against B-Raf-Driven tumors. ACS Med. Chem. Lett. 4 (2013), 358–362.
-
(2013)
ACS Med. Chem. Lett.
, vol.4
, pp. 358-362
-
-
Rheault, T.R.1
Stellwagen, J.C.2
Adjabeng, G.M.3
Hornberger, K.R.4
Petrov, K.G.5
Waterson, A.G.6
Dickerson, S.H.7
Mook, R.A.8
Laquerre, S.G.9
King, A.J.10
-
35
-
-
34248591612
-
Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer
-
Roberts, P.J., Der, C.J., Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer. Oncogene 26 (2007), 3291–3310.
-
(2007)
Oncogene
, vol.26
, pp. 3291-3310
-
-
Roberts, P.J.1
Der, C.J.2
-
36
-
-
84861885576
-
Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling
-
Roring, M., Herr, R., Fiala, G.J., Heilmann, K., Braun, S., Eisenhardt, A.E., Halbach, S., Capper, D., von Deimling, A., Schamel, W.W., et al. Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling. EMBO J. 31 (2012), 2629–2647.
-
(2012)
EMBO J.
, vol.31
, pp. 2629-2647
-
-
Roring, M.1
Herr, R.2
Fiala, G.J.3
Heilmann, K.4
Braun, S.5
Eisenhardt, A.E.6
Halbach, S.7
Capper, D.8
von Deimling, A.9
Schamel, W.W.10
-
37
-
-
84921270388
-
Targeting RAS-ERK signalling in cancer: promises and challenges
-
Samatar, A.A., Poulikakos, P.I., Targeting RAS-ERK signalling in cancer: promises and challenges. Nat. Rev. Drug Discov. 13 (2014), 928–942.
-
(2014)
Nat. Rev. Drug Discov.
, vol.13
, pp. 928-942
-
-
Samatar, A.A.1
Poulikakos, P.I.2
-
38
-
-
84859183431
-
Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance
-
Shi, H., Moriceau, G., Kong, X., Lee, M.K., Lee, H., Koya, R.C., Ng, C., Chodon, T., Scolyer, R.A., Dahlman, K.B., et al. Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nat. Commun., 3, 2012, 724.
-
(2012)
Nat. Commun.
, vol.3
, pp. 724
-
-
Shi, H.1
Moriceau, G.2
Kong, X.3
Lee, M.K.4
Lee, H.5
Koya, R.C.6
Ng, C.7
Chodon, T.8
Scolyer, R.A.9
Dahlman, K.B.10
-
39
-
-
84925283093
-
Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation
-
Thevakumaran, N., Lavoie, H., Critton, D.A., Tebben, A., Marinier, A., Sicheri, F., Therrien, M., Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation. Nat. Struct. Mol. Biol. 22 (2015), 37–43.
-
(2015)
Nat. Struct. Mol. Biol.
, vol.22
, pp. 37-43
-
-
Thevakumaran, N.1
Lavoie, H.2
Critton, D.A.3
Tebben, A.4
Marinier, A.5
Sicheri, F.6
Therrien, M.7
-
40
-
-
78650008177
-
Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K
-
Villanueva, J., Vultur, A., Lee, J.T., Somasundaram, R., Fukunaga-Kalabis, M., Cipolla, A.K., Wubbenhorst, B., Xu, X., Gimotty, P.A., Kee, D., et al. Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K. Cancer Cell 18 (2010), 683–695.
-
(2010)
Cancer Cell
, vol.18
, pp. 683-695
-
-
Villanueva, J.1
Vultur, A.2
Lee, J.T.3
Somasundaram, R.4
Fukunaga-Kalabis, M.5
Cipolla, A.K.6
Wubbenhorst, B.7
Xu, X.8
Gimotty, P.A.9
Kee, D.10
-
41
-
-
12144289677
-
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF
-
Wan, P.T., Garnett, M.J., Roe, S.M., Lee, S., Niculescu-Duvaz, D., Good, V.M., Jones, C.M., Marshall, C.J., Springer, C.J., Barford, D., et al. Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell 116 (2004), 855–867.
-
(2004)
Cell
, vol.116
, pp. 855-867
-
-
Wan, P.T.1
Garnett, M.J.2
Roe, S.M.3
Lee, S.4
Niculescu-Duvaz, D.5
Good, V.M.6
Jones, C.M.7
Marshall, C.J.8
Springer, C.J.9
Barford, D.10
-
42
-
-
0035328521
-
Active Ras induces heterodimerization of cRaf and BRaf
-
Weber, C.K., Slupsky, J.R., Kalmes, H.A., Rapp, U.R., Active Ras induces heterodimerization of cRaf and BRaf. Cancer Res. 61 (2001), 3595–3598.
-
(2001)
Cancer Res.
, vol.61
, pp. 3595-3598
-
-
Weber, C.K.1
Slupsky, J.R.2
Kalmes, H.A.3
Rapp, U.R.4
-
43
-
-
8444238236
-
The RAF proteins take centre stage
-
Wellbrock, C., Karasarides, M., Marais, R., The RAF proteins take centre stage. Nat. Rev. Mol. Cell Biol. 5 (2004), 875–885.
-
(2004)
Nat. Rev. Mol. Cell Biol.
, vol.5
, pp. 875-885
-
-
Wellbrock, C.1
Karasarides, M.2
Marais, R.3
-
44
-
-
84942319957
-
Braf mutants evade ERK-dependent feedback by different mechanisms that determine their sensitivity to pharmacologic inhibition
-
Yao, Z., Torres, N.M., Tao, A., Gao, Y., Luo, L., Li, Q., de Stanchina, E., Abdel-Wahab, O., Solit, D.B., Poulikakos, P.I., et al. Braf mutants evade ERK-dependent feedback by different mechanisms that determine their sensitivity to pharmacologic inhibition. Cancer Cell 28 (2015), 370–383.
-
(2015)
Cancer Cell
, vol.28
, pp. 370-383
-
-
Yao, Z.1
Torres, N.M.2
Tao, A.3
Gao, Y.4
Luo, L.5
Li, Q.6
de Stanchina, E.7
Abdel-Wahab, O.8
Solit, D.B.9
Poulikakos, P.I.10
-
45
-
-
67649770887
-
Ras signaling and therapies
-
Young, A., Lyons, J., Miller, A.L., Phan, V.T., Alarcon, I.R., McCormick, F., Ras signaling and therapies. Adv. Cancer Res. 102 (2009), 1–17.
-
(2009)
Adv. Cancer Res.
, vol.102
, pp. 1-17
-
-
Young, A.1
Lyons, J.2
Miller, A.L.3
Phan, V.T.4
Alarcon, I.R.5
McCormick, F.6
-
46
-
-
84945243598
-
RAF inhibitors that evade paradoxical MAPK pathway activation
-
Zhang, C., Spevak, W., Zhang, Y., Burton, E.A., Ma, Y., Habets, G., Zhang, J., Lin, J., Ewing, T., Matusow, B., et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature 526 (2015), 583–586.
-
(2015)
Nature
, vol.526
, pp. 583-586
-
-
Zhang, C.1
Spevak, W.2
Zhang, Y.3
Burton, E.A.4
Ma, Y.5
Habets, G.6
Zhang, J.7
Lin, J.8
Ewing, T.9
Matusow, B.10
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