Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

BRAF/MEK inhibitors for BRAF V600E-mutant cancers in non-approved setting: a case series

Butt, Sabeeh-ur-Rehman
Mejias, Alberto
Morelli, Cristina
Torga, Gonzalo
Happe, Marlene
Patrikidou, Anna
Arkenau, Hendrik-Tobias

January 2021

The management of cancer has been traditionally dependent on the primary tumour type and specific hi...

August 2016

inh ll l BRAF mutation, the MAPK pathway, and therefore the growth of melanoma cells, can be efficie...

RESEARCH BRIEF Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors

Erick J. Morris
Sharda Jha
Clifford R. Restaino
Priya Dayananth
Hugh Zhu
Alan Cooper
Donna Carr
Yongi Deng
Weihong Jin
Stuart Black
Brian Long
Jenny Liu
Edward Dinunzio
William Windsor
Rumin Zhang
Shuxia Zhao
Minilik H. Angagaw
Elaine M. Pinheiro
Jagdish Desai
Li Xiao
Alan Hruza
James Wang
Joe Kelly
Sunil Paliwal
Xiaolei Gao
Boga Sobhana Babu
Liang Zhu
Pierre Daublain
Ling Zhang
Bart A. Lutterbach
Marc R. Pelletier
Phieng Siliphaivanh
David Witter
Paul Kirschmeier
W. Robert Bishop
Daniel Hicklin
D. Gary Gillil
Lata Jayaraman
Leigh Zawel
Stephen Fawell
Ahmed A. Samatar

October 2016

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Del Curatolo, Anais
Conciatori, Fabiana
Cesta Incani, Ursula
Bazzichetto, Chiara
Falcone, Italia
Corbo, Vincenzo
D’Agosto, Sabrina
Eramo, Adriana
Sette,Giovann i
Sperduti, Isabella
De Luca, Teresa
Marabese, Mirko
Shirasawa, Senji
De Maria, Ruggero
Scarpa, Aldo
Broggini, Massimo
Del Bufalo, Donatella
Cognetti, Francesco
Milella, Michele
Ciuffreda, Ludovica

January 2018

Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in paradox MAPK (re...

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Del Curatolo, Anais
Conciatori, Fabiana
Cesta Incani, Ursula
Bazzichetto, Chiara
Falcone, Italia
Corbo, Vincenzo
D'Agosto, Sabrina
Eramo, Adriana
Sette, Giovanni
Sperduti, Isabella
De Luca, Teresa
Marabese, Mirko
Shirasawa, Senji
De Maria Marchiano, Ruggero (ORCID:0000-0003-2255-0583)
Scarpa, Aldo
Broggini, Massimo
Del Bufalo, Donatella
Cognetti, Francesco
Milella, Michele
Ciuffreda, Ludovica

January 2018

Background: Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in para...

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Anais Del Curatolo
Fabiana Conciatori
Ursula Cesta Incani
Chiara Bazzichetto
Italia Falcone
Vincenzo Corbo
Sabrina D’Agosto
Adriana Eramo
Giovanni Sette
Isabella Sperduti
Teresa De Luca
Mirko Marabese
Senji Shirasawa
Ruggero De Maria
Aldo Scarpa
Massimo Broggini
Donatella Del Bufalo
Francesco Cognetti
Michele Milella
Ludovica Ciuffreda

July 2018

Abstract Background Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role...

THERAPEUTIC TARGETING OF RAF-INDUCED PARADOXICAL ERK ACTIVATION WITH A VERTICAL COMBINATION HITTING MULTIPLE STEPS ALONG THE MAPK CASCADE

Cesta Incani, U.
Del Curatolo, A.
Falcone, I.
Eramo, A.
Sette, G.
Sperduti, I.
Matteoni, S.
Shirasawa, S.
Broggini, M.
De Maria, R. (ORCID:0000-0003-2255-0583)
Cognetti, F.
Ciuffreda, L.
Milella, M.

January 2014

Aim: Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in paradox MAP...

A vertical combination strategy hitting multiple steps along the MAPK cascade: Molecular mechanisms of action and putative genetic determinants of synergism

Del Curatolo, A.
Cesta Incani, U.
Ciuffreda, L.
Falcone, I
Shirasawa, S.
Broggini, M.
Sperduti, I
Eramo, A.
De Maria, R. (ORCID:0000-0003-2255-0583)
Cognetti, F.
Milella, M.

January 2014

Preclinical evidence shows that hitting a single point along the RAF/MEK/ERK cascade disrupts intra-...

Pan-RAF and MEK vertical inhibition enhances therapeutic response in non-V600 BRAF mutant cells

Molnár, Eszter
Rittler D
Baranyi, Marcell
Grusch M
Berger W
Döme, Balázs
Tóvári, József
Aigner C
Tímár, József
Garay, Tamás
Hegedűs, Balázs

May 2018

BACKGROUND: Currently, there are no available targeted therapy options for non-V600 BRAF mutated tum...

Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors.

Whittaker, SR
Cowley, GS
Wagner, S
Luo, F
Root, DE
Garraway, LA

December 2015

RAF and MEK inhibitors are effective in BRAF-mutant melanoma but not in BRAF-mutant colorectal cance...

Combination of RAF and MEK Inhibition for the Treatment of BRAF-Mutated Melanoma: Feedback Is Not Encouraged

Chapman, Paul B.
Solit, David B.
Rosen, Neal

November 2014

In BRAF V600E melanoma patients, RAF inhibitor treatment causes a MEK-inhibitor-sensitive, RAF-inhib...

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

Hatzivassiliou, G
Haling, JR
Chen, H
Song, K
Price, S
Heald, R
Hewitt, JFM
Zak, M
Peck, A
Orr, C
Merchant, M
Hoeflich, KP
Chan, J
Luoh, S
Anderson, DJ
Ludlam, MJC
Wiesmann, C
Ultsch, M
Friedman, LS
Malek, S
Belvin, M

January 2013

KRAS and BRAF activating mutations drive tumorigenesis through constitutive activation of the MAPK p...

Effective MAPK Inhibition is critical for therapeutic responses in colorectal cancer with BRAF mutations

Ahronian, Leanne G.
Corcoran, Ryan B.

July 2016

ABSTRACT RAF inhibitor monotherapy is ineffective in BRAF-mutant colorectal cancer (CRC) but RAF inh...

Immunomodulatory Properties of BRAF and MEK Inhibitors Used for Melanoma Therapy—Paradoxical ERK Activation and Beyond

Thomas Jung
Maximilian Haist
Michael Kuske
Stephan Grabbe
Matthias Bros

September 2021

The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth ...

Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAFV600E-Mutant Colorectal Cancer

Corcoran, Ryan B
André, Thierry
Atreya, Chloe E
Schellens, Jan HM
Yoshino, Takayuki
Bendell, Johanna C
Hollebecque, Antoine
McRee, Autumn J
Siena, Salvatore
Middleton, Gary
Muro, Kei
Gordon, Michael S
Tabernero, Josep
Yaeger, Rona
O'Dwyer, Peter J
Humblet, Yves
De Vos, Filip
Jung, A Scott
Brase, Jan C
Jaeger, Savina
Bettinger, Severine
Mookerjee, Bijoyesh
Rangwala, Fatima
Van Cutsem, Eric

April 2018

Although BRAF inhibitor monotherapy yields response rates >50% in BRAFV600-mutant melanoma, only ...

BRAF/MEK inhibitors for BRAF V600E-mutant cancers in non-approved setting: a case series

Butt, Sabeeh-ur-Rehman
Mejias, Alberto
Morelli, Cristina
Torga, Gonzalo
Happe, Marlene
Patrikidou, Anna
Arkenau, Hendrik-Tobias

January 2021

The management of cancer has been traditionally dependent on the primary tumour type and specific hi...

d m

August 2016

inh ll l BRAF mutation, the MAPK pathway, and therefore the growth of melanoma cells, can be efficie...

RESEARCH BRIEF Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors

Erick J. Morris
Sharda Jha
Clifford R. Restaino
Priya Dayananth
Hugh Zhu
Alan Cooper
Donna Carr
Yongi Deng
Weihong Jin
Stuart Black
Brian Long
Jenny Liu
Edward Dinunzio
William Windsor
Rumin Zhang
Shuxia Zhao
Minilik H. Angagaw
Elaine M. Pinheiro
Jagdish Desai
Li Xiao
Alan Hruza
James Wang
Joe Kelly
Sunil Paliwal
Xiaolei Gao
Boga Sobhana Babu
Liang Zhu
Pierre Daublain
Ling Zhang
Bart A. Lutterbach
Marc R. Pelletier
Phieng Siliphaivanh
David Witter
Paul Kirschmeier
W. Robert Bishop
Daniel Hicklin
D. Gary Gillil
Lata Jayaraman
Leigh Zawel
Stephen Fawell
Ahmed A. Samatar

October 2016

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Del Curatolo, Anais
Conciatori, Fabiana
Cesta Incani, Ursula
Bazzichetto, Chiara
Falcone, Italia
Corbo, Vincenzo
D’Agosto, Sabrina
Eramo, Adriana
Sette,Giovann i
Sperduti, Isabella
De Luca, Teresa
Marabese, Mirko
Shirasawa, Senji
De Maria, Ruggero
Scarpa, Aldo
Broggini, Massimo
Del Bufalo, Donatella
Cognetti, Francesco
Milella, Michele
Ciuffreda, Ludovica

January 2018

Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in paradox MAPK (re...

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Del Curatolo, Anais
Conciatori, Fabiana
Cesta Incani, Ursula
Bazzichetto, Chiara
Falcone, Italia
Corbo, Vincenzo
D'Agosto, Sabrina
Eramo, Adriana
Sette, Giovanni
Sperduti, Isabella
De Luca, Teresa
Marabese, Mirko
Shirasawa, Senji
De Maria Marchiano, Ruggero (ORCID:0000-0003-2255-0583)
Scarpa, Aldo
Broggini, Massimo
Del Bufalo, Donatella
Cognetti, Francesco
Milella, Michele
Ciuffreda, Ludovica

January 2018

Background: Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in para...

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Anais Del Curatolo
Fabiana Conciatori
Ursula Cesta Incani
Chiara Bazzichetto
Italia Falcone
Vincenzo Corbo
Sabrina D’Agosto
Adriana Eramo
Giovanni Sette
Isabella Sperduti
Teresa De Luca
Mirko Marabese
Senji Shirasawa
Ruggero De Maria
Aldo Scarpa
Massimo Broggini
Donatella Del Bufalo
Francesco Cognetti
Michele Milella
Ludovica Ciuffreda

July 2018

Abstract Background Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role...

THERAPEUTIC TARGETING OF RAF-INDUCED PARADOXICAL ERK ACTIVATION WITH A VERTICAL COMBINATION HITTING MULTIPLE STEPS ALONG THE MAPK CASCADE

Cesta Incani, U.
Del Curatolo, A.
Falcone, I.
Eramo, A.
Sette, G.
Sperduti, I.
Matteoni, S.
Shirasawa, S.
Broggini, M.
De Maria, R. (ORCID:0000-0003-2255-0583)
Cognetti, F.
Ciuffreda, L.
Milella, M.

January 2014

Aim: Mounting evidence suggests that RAF-mediated MEK activation plays a crucial role in paradox MAP...

A vertical combination strategy hitting multiple steps along the MAPK cascade: Molecular mechanisms of action and putative genetic determinants of synergism

Del Curatolo, A.
Cesta Incani, U.
Ciuffreda, L.
Falcone, I
Shirasawa, S.
Broggini, M.
Sperduti, I
Eramo, A.
De Maria, R. (ORCID:0000-0003-2255-0583)
Cognetti, F.
Milella, M.

January 2014

Preclinical evidence shows that hitting a single point along the RAF/MEK/ERK cascade disrupts intra-...

Pan-RAF and MEK vertical inhibition enhances therapeutic response in non-V600 BRAF mutant cells

Molnár, Eszter
Rittler D
Baranyi, Marcell
Grusch M
Berger W
Döme, Balázs
Tóvári, József
Aigner C
Tímár, József
Garay, Tamás
Hegedűs, Balázs

May 2018

BACKGROUND: Currently, there are no available targeted therapy options for non-V600 BRAF mutated tum...

Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors.

Whittaker, SR
Cowley, GS
Wagner, S
Luo, F
Root, DE
Garraway, LA

December 2015

RAF and MEK inhibitors are effective in BRAF-mutant melanoma but not in BRAF-mutant colorectal cance...

Combination of RAF and MEK Inhibition for the Treatment of BRAF-Mutated Melanoma: Feedback Is Not Encouraged

Chapman, Paul B.
Solit, David B.
Rosen, Neal

November 2014

In BRAF V600E melanoma patients, RAF inhibitor treatment causes a MEK-inhibitor-sensitive, RAF-inhib...

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

Hatzivassiliou, G
Haling, JR
Chen, H
Song, K
Price, S
Heald, R
Hewitt, JFM
Zak, M
Peck, A
Orr, C
Merchant, M
Hoeflich, KP
Chan, J
Luoh, S
Anderson, DJ
Ludlam, MJC
Wiesmann, C
Ultsch, M
Friedman, LS
Malek, S
Belvin, M

January 2013

KRAS and BRAF activating mutations drive tumorigenesis through constitutive activation of the MAPK p...

Effective MAPK Inhibition is critical for therapeutic responses in colorectal cancer with BRAF mutations

Ahronian, Leanne G.
Corcoran, Ryan B.

July 2016

ABSTRACT RAF inhibitor monotherapy is ineffective in BRAF-mutant colorectal cancer (CRC) but RAF inh...

Immunomodulatory Properties of BRAF and MEK Inhibitors Used for Melanoma Therapy—Paradoxical ERK Activation and Beyond

Thomas Jung
Maximilian Haist
Michael Kuske
Stephan Grabbe
Matthias Bros

September 2021

The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth ...

Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAFV600E-Mutant Colorectal Cancer

Corcoran, Ryan B
André, Thierry
Atreya, Chloe E
Schellens, Jan HM
Yoshino, Takayuki
Bendell, Johanna C
Hollebecque, Antoine
McRee, Autumn J
Siena, Salvatore
Middleton, Gary
Muro, Kei
Gordon, Michael S
Tabernero, Josep
Yaeger, Rona
O'Dwyer, Peter J
Humblet, Yves
De Vos, Filip
Jung, A Scott
Brase, Jan C
Jaeger, Savina
Bettinger, Severine
Mookerjee, Bijoyesh
Rangwala, Fatima
Van Cutsem, Eric

April 2018

Although BRAF inhibitor monotherapy yields response rates >50% in BRAFV600-mutant melanoma, only ...

BRAF/MEK inhibitors for BRAF V600E-mutant cancers in non-approved setting: a case series

Butt, Sabeeh-ur-Rehman
Mejias, Alberto
Morelli, Cristina
Torga, Gonzalo
Happe, Marlene
Patrikidou, Anna
Arkenau, Hendrik-Tobias

January 2021

The management of cancer has been traditionally dependent on the primary tumour type and specific hi...

d m

August 2016

inh ll l BRAF mutation, the MAPK pathway, and therefore the growth of melanoma cells, can be efficie...

RESEARCH BRIEF Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors

Erick J. Morris
Sharda Jha
Clifford R. Restaino
Priya Dayananth
Hugh Zhu
Alan Cooper
Donna Carr
Yongi Deng
Weihong Jin
Stuart Black
Brian Long
Jenny Liu
Edward Dinunzio
William Windsor
Rumin Zhang
Shuxia Zhao
Minilik H. Angagaw
Elaine M. Pinheiro
Jagdish Desai
Li Xiao
Alan Hruza
James Wang
Joe Kelly
Sunil Paliwal
Xiaolei Gao
Boga Sobhana Babu
Liang Zhu
Pierre Daublain
Ling Zhang
Bart A. Lutterbach
Marc R. Pelletier
Phieng Siliphaivanh
David Witter
Paul Kirschmeier
W. Robert Bishop
Daniel Hicklin
D. Gary Gillil
Lata Jayaraman
Leigh Zawel
Stephen Fawell
Ahmed A. Samatar

October 2016

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Abstract

Extracted data

Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models

Abstract

Extracted data

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