The Raf/MEK/ERK pathway is an important mediator of tumor cell proliferation and angiogenesis. Here, we investigated the growth-inhibitory and antiangiogenic properties of PD0325901, a novel MEK inhibitor, in human melanoma cells. PD0325901 effects were determined in a panel of melanoma cell lines with different genetic aberrations. PD0325901 markedly inhibited ERK phosphorylation and growth of both BRAF mutant and wild-type melanoma cell lines, with IC(50) in the nanomolar range even in the least responsive models. Growth inhibition was observed both in vitro and in vivo in xenograft models, regardless of BRAF mutation status, and was due to G(1)-phase cell cycle arrest and subsequent induction of apoptosis. Cell cycle (cyclin D1, c-Myc, a...
The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth ...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...
The Raf/MEK/ERK pathway is an importantmediator of tumor cell proliferation and angiogenesis. Here, ...
AbstractThe Raf/MEK/ERK pathway is an importantmediator of tumor cell proliferation and angiogenesis...
: The Raf/MEK/ERK pathway is an important mediator of tumor cell proliferation and angiogenesis. Her...
One of the key oncogenic pathways involved in melanoma aggressiveness, development and progression i...
This is an open-access article distributed under the terms of the Creative Commons Attribution Licen...
BackgroundApproximately 20% of melanomas contain a mutation in NRAS. However no direct inhibitor of ...
Although melanoma is the most aggressive skin cancer, recent advances in BRAF and/or MEK inhibitors ...
The melanoma treatment landscape has been revolutionized by the rational design of small molecules t...
Purpose: Disseminated melanoma is highly therapy resistant. The finding that 66% of melanomas harbor...
BACKGROUND: Melanoma is the most lethal form of skin cancer, but recent advances in molecularly targ...
AbstractBackgroundTAK733 is a novel allosteric, non-ATP-binding, inhibitor of the BRAF substrates ME...
Inhibitors of the mitogen-activated protein kinases (MAPK), BRAF, and MAP–ERK kinase (MEK) induce tu...
The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth ...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...
The Raf/MEK/ERK pathway is an importantmediator of tumor cell proliferation and angiogenesis. Here, ...
AbstractThe Raf/MEK/ERK pathway is an importantmediator of tumor cell proliferation and angiogenesis...
: The Raf/MEK/ERK pathway is an important mediator of tumor cell proliferation and angiogenesis. Her...
One of the key oncogenic pathways involved in melanoma aggressiveness, development and progression i...
This is an open-access article distributed under the terms of the Creative Commons Attribution Licen...
BackgroundApproximately 20% of melanomas contain a mutation in NRAS. However no direct inhibitor of ...
Although melanoma is the most aggressive skin cancer, recent advances in BRAF and/or MEK inhibitors ...
The melanoma treatment landscape has been revolutionized by the rational design of small molecules t...
Purpose: Disseminated melanoma is highly therapy resistant. The finding that 66% of melanomas harbor...
BACKGROUND: Melanoma is the most lethal form of skin cancer, but recent advances in molecularly targ...
AbstractBackgroundTAK733 is a novel allosteric, non-ATP-binding, inhibitor of the BRAF substrates ME...
Inhibitors of the mitogen-activated protein kinases (MAPK), BRAF, and MAP–ERK kinase (MEK) induce tu...
The advent of mitogen-activated protein kinase (MAPK) inhibitors that directly inhibit tumor growth ...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...
PURPOSE: About 65% to 70% of melanomas harbor a mutation in v-raf murine sarcoma viral oncogene homo...