Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

被引：0

作者：

Georgia Hatzivassiliou

Jacob R. Haling

Huifen Chen

Kyung Song

Steve Price

Robert Heald

Joanne F. M. Hewitt

Mark Zak

Ariana Peck

Christine Orr

Mark Merchant

Klaus P. Hoeflich

Jocelyn Chan

Shiuh-Ming Luoh

Daniel J. Anderson

Mary J. C. Ludlam

Christian Wiesmann

Mark Ultsch

Lori S. Friedman

Shiva Malek

Marcia Belvin

机构：

[1] Genentech,Department of Translational Oncology

[2] Inc.,Department of Biochemical and Cellular Pharmacology

[3] 1 DNA Way,Department of Discovery Chemistry

[4] South San Francisco,Department of Discovery Oncology

[5] California 94080,Department of Structural Biology

[6] USA,undefined

[7] Genentech,undefined

[8] Inc.,undefined

[9] 1 DNA Way,undefined

[10] South San Francisco,undefined

[11] California 94080,undefined

[12] USA,undefined

[13] Genentech,undefined

[14] Inc.,undefined

[15] 1 DNA Way,undefined

[16] South San Francisco,undefined

[17] California 94080,undefined

[18] USA,undefined

[19] Argenta,undefined

[20] 8/9 Spire Green Centre,undefined

[21] Flex Meadow,undefined

[22] Harlow,undefined

[23] Essex CM19 5TR,undefined

[24] UK,undefined

[25] Genentech,undefined

[26] Inc.,undefined

[27] 1 DNA Way,undefined

[28] South San Francisco,undefined

[29] California 94080,undefined

[30] USA,undefined

[31] Genentech,undefined

[32] Inc.,undefined

[33] 1 DNA Way,undefined

[34] South San Francisco,undefined

[35] California 94080,undefined

[36] USA,undefined

[37] Present addresses: WestCHEM,undefined

[38] School of Chemistry,undefined

[39] University of Glasgow,undefined

[40] Joseph Black Building,undefined

[41] University Avenue,undefined

[42] Glasgow G12 8QQ,undefined

[43] UK (J.F.M.H.); MRC Mitochondrial Biology Unit,undefined

[44] Wellcome Trust/MRC Building,undefined

[45] Hills Road,undefined

[46] Cambridge CB2 OXY,undefined

[47] UK (A.P.); Novartis Institutes for Biomedical Research,undefined

[48] Fabrikstrasse 16,undefined

[49] CH-4002 Basel,undefined

[50] Switzerland (C.W.); Cairn Biosciences Inc.,undefined

来源：

Nature | 2013年 / 501卷

关键词：

D O I：

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中图分类号：

学科分类号：

摘要：

The mechanism of action of three different allosteric MEK inhibitors that target the MAP kinase pathway is investigated, and their efficacy is shown to be explained by the distinct mechanisms regulating MEK activation in KRAS- versus BRAF-driven tumours; this work provides a rationale for designing more effective cancer therapies for these common genetic subtypes of cancer.

引用

页码：232 / 236

页数：4

共 40 条

[1] Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, Georgia
Haling, Jacob R.
Chen, Huifen
Song, Kyung
Price, Steve
Heald, Robert
Hewitt, Joanne F. M.
Zak, Mark
Peck, Ariana
Orr, Christine
Merchant, Mark
Hoeflich, Klaus P.
Chan, Jocelyn
Luoh, Shiuh-Ming
Anderson, Daniel J.
Ludlam, Mary J. C.
Wiesmann, Christian
Ultsch, Mark
Friedman, Lori S.
Malek, Shiva
Belvin, Marcia
NATURE, 2013, 501 (7466) : 232 - 236
[2] Erratum: Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Georgia Hatzivassiliou
Jacob R. Haling
Huifen Chen
Kyung Song
Steve Price
Robert Heald
Joanne F. M. Hewitt
Mark Zak
Ariana Peck
Christine Orr
Mark Merchant
Klaus P. Hoeflich
Jocelyn Chan
Shiuh-Ming Luoh
Daniel J. Anderson
Mary J. C. Ludlam
Christian Wiesmann
Mark Ultsch
Lori S. Friedman
Shiva Malek
Marcia Belvin
Nature, 2013, 502 : 258 - 258
[3] Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers (vol 501, pg 232, 2013)
Hatzivassiliou, Georgia
Haling, Jacob R.
Chen, Huifen
Song, Kyung
Price, Steve
Heald, Robert
Hewitt, Joanne F. M.
Zak, Mark
Peck, Ariana
Orr, Christine
Merchant, Mark
Hoeflich, Klaus P.
Chan, Jocelyn
Luoh, Shiuh-Ming
Anderson, Daniel J.
Ludlam, Mary J. C.
Wiesmann, Christian
Ultsch, Mark
Friedman, Lori S.
Malek, Shiva
Belvin, Marcia
NATURE, 2013, 502 (7470) : 258 - 258
[4] Autophagy Inhibition in BRAF-Driven Cancers
Foth, Mona
McMahon, Martin
CANCERS, 2021, 13 (14)
[5] KRAS Mutation as a Resistance Mechanism to BRAF/MEK Inhibition in NSCLC
Niemantsverdriet, Maarten
Schuuring, Ed
ter Elst, Arja
van der Wekken, Antonie J.
van Kempen, Leon C.
van den Berg, Anke
Groen, Harry J. M.
JOURNAL OF THORACIC ONCOLOGY, 2018, 13 (12) : E249 - E251
[6] Adaptive Resistance to Dual BRAF/MEK Inhibition in BRAF-Driven Tumors through Autocrine FGFR Pathway Activation
Wang, Victoria E.
Xue, Jenny Y.
Frederick, Dennie T.
Cao, Yi
Lin, Eva
Wilson, Catherine
Urisman, Anatoly
Carbone, David P.
Flaherty, Keith T.
Bernards, Rene
Lito, Piro
Settleman, Jeff
McCormick, Frank
CLINICAL CANCER RESEARCH, 2019, 25 (23) : 7202 - 7217
[7] MEK1/2 Inhibition Decreases Lactate in BRAF-Driven Human Cancer Cells
Miniotis, Maria Falck
Arunan, Vaitha
Eykyn, Thomas R.
Marais, Richard
Workman, Paul
Leach, Martin O.
Beloueche-Babari, Mounia
CANCER RESEARCH, 2013, 73 (13) : 4039 - 4049
[8] Dual inhibition of SUMOylation and MEK for MYC-expressing KRAS mutant cancers
Kotani, Hiroshi
Yano, Seiji
CANCER SCIENCE, 2024, 115 : 395 - 395
[9] Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers
Dai, Xinyu
Xia, Hongwei
Zhou, Sheng
Tang, Qiulin
Bi, Feng
CANCER LETTERS, 2019, 442 : 202 - 212
[10] The discovery and characterization of CFT1946: A potent, selective, and orally bioavailable degrader of mutant BRAF for the treatment of BRAF-driven cancers
Liang, Yanke
Sowa, Mathew E.
Jackson, Katrina L.
Simard, Jeffrey R.
Kreger, Bridget
Li, Ping
Poling, Laura
Baddour, Joelle
Good, Andrew
Huang, Hongwei
Eron, Scott
Nasveschuk, Christopher G.
Yu, Robert
Fitzgerald, Mark
Garza, Victoria
O'Shea, Morgan W.
Veits, Gesine
Yap, Jeremy Y.
Moustakim, Moses
Hart, Ashley
Agafonov, Roman V.
Sarkissian, Grace
Patel, Joe S.
Deibler, Richard
Cole, Kyle S.
Cocozziello, David
Rahman, Fazlur
Phillips, Andrew J.
Norton, Elizabeth
Crystal, Adam S.
Pollock, Roy M.
Fisher, Stewart L.
CANCER RESEARCH, 2023, 83 (07)

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