Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Helen A. Manne"'
Autor:
Steven R. Whittaker, Helen A. Manne, Ruth S. Kirk, Alfonso Zambon, Richard Marais, Delphine Menard, Lesley Ogilvie, Douglas Hedley, Jorge S. Reis-Filho, Natasha Preece, Maryou B K Lambros, Filipa Lopes, Caroline J. Springer, Sareena Rana
Publikováno v:
Cancer Research. 70:8036-8044
Oncogenic BRAF is a critical driver of proliferation and survival and is thus a validated therapeutic target in cancer. We have developed a potent inhibitor, termed 1t (CCT239065), of the mutant protein kinase, V600EBRAF. 1t inhibits signaling downst
Autor:
Ion Niculescu-Duvaz, Alfonso Zambon, Natasha Preece, Delphine Menard, Lawrence Davies, Steven R. Whittaker, Lesley Ogilvie, Arnaud Nourry, Dan Niculescu-Duvaz, Bart M. J. M. Suijkerbuijk, Richard Marais, Filipa Lopes, Caroline J. Springer, Ruth Kirk, Helen A. Manne, Douglas Hedley
Publikováno v:
Journal of Medicinal Chemistry. 53:5639-5655
Mutated BRAF serine/threonine kinase is implicated in several types of cancer, with particularly high frequency in melanoma and colorectal carcinoma. We recently reported on the development of BRAF inhibitors based on a tripartite A-B-C system featur
Autor:
Florence I. Raynaud, Ion Niculescu-Duvaz, Catherine Gaulon, Douglas Hedley, Bart M. J. M. Suijkerbuijk, Caroline J. Springer, Ruth Kirk, Arnaud Nourry, Frank Friedlos, Javier Moreno-Farre, Richard Marais, Lesley Ogilvie, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard, Harmen P. Dijkstra, Adrian Liam Gill, Helen A. Manne, Richard D. Taylor, Lawrence Davies, Steven R. Whittaker
Publikováno v:
Journal of Medicinal Chemistry. 52:2255-2264
BRAF is a serine/threonine kinase that is mutated in a range of cancers, including 50-70% of melanomas, and has been validated as a therapeutic target. We have designed and synthesized mutant BRAF inhibitors containing pyridoimidazolone as a new hing
Autor:
Catherine Gaulon, Filipa Lopes, Arnaud Nourry, Steven R. Whittaker, Richard Marais, Frank Friedlos, Alfonso Zambon, Delphine Menard, Bart M. J. M. Suijkerbuijk, Lesley Ogilvie, Helen A. Manne, Ion Niculescu-Duvaz, Lawrence Davies, Harmen P. Dijkstra, Javier Moreno-Farre, Dan Niculescu-Duvaz, Natasha Preece, Douglas Hedley, Caroline J. Springer, Ruth Kirk, Florence I. Raynaud
Publikováno v:
Journal of medicinal chemistry. 53(7)
We describe the design, synthesis, and optimization of a series of new inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF), a kinase whose mutant form (V600E) is implicated in several types of cancer, with a particularly high freque
Autor:
Dan Niculescu-Duvaz, Helen A. Manne, Steven R. Whittaker, Lawrence Davies, Florence I. Raynaud, Frank Friedlos, Bart M. J. M. Suijkerbuijk, Ion Niculescu-Duvaz, Caroline J. Springer, Richard D. Taylor, Ruth Kirk, Javier Moreno-Farre, Catherine Gaulon, Richard Marais, Alfonso Zambon, Delphine Menard, Lesley Ogilvie, Arnaud Nourry, Adrian Liam Gill, Douglas Hedley, Harmen P. Dijkstra
Publikováno v:
Journal of Medicinal Chemistry. 52:5770-5770
Autor:
Caroline J. Springer, Ruth Kirk, Richard Marais, David Matthew Wilson, Bart M. J. M. Suijkerbuijk, Frank Friedlos, Alfonso Zambon, Delphine Menard, Coulter Thomas, Andrew K. Takle, Jean-François Pons, Arnaud Nourry, Neus Cantarino, Dan Niculescu-Duvaz, Douglas Hedley, Ion Niculescu-Duvaz, Lesley Ogilvie, Lawrence Davies, Helen A. Manne, Steven R. Whittaker
Publikováno v:
Bioorganic & Medicinal Chemistry
Graphical abstract 1j IC50 (BRAF) = 0.24 μM; IC50 (pERK) = 0.58 μM; GI50 (SRB) = 0.87 μM.
V-RAF murine sarcoma viral oncogene homolog B1 (BRAF) is a serine/threonine-specific protein kinase that is mutated with high frequency in cutaneous mel
V-RAF murine sarcoma viral oncogene homolog B1 (BRAF) is a serine/threonine-specific protein kinase that is mutated with high frequency in cutaneous mel