The “cyclopropyl fragment” is a versatile player that frequently appears in preclinical/clinical drug molecules
TT Talele - Journal of medicinal chemistry, 2016 - ACS Publications
Recently, there has been an increasing use of the cyclopropyl ring in drug development to
transition drug candidates from the preclinical to clinical stage. Important features of the …
transition drug candidates from the preclinical to clinical stage. Important features of the …
[HTML][HTML] Roles of the Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR pathways in controlling growth and sensitivity to therapy-implications for cancer and aging
LS Steelman, WH Chappell, SL Abrams… - Aging (Albany …, 2011 - ncbi.nlm.nih.gov
Dysregulated signaling through the Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR pathways
is often the result of genetic alterations in critical components in these pathways or upstream …
is often the result of genetic alterations in critical components in these pathways or upstream …
The MAP kinase signaling cascades: a system of hundreds of components regulates a diverse array of physiological functions
Y Keshet, R Seger - MAP Kinase Signaling Protocols: Second Edition, 2010 - Springer
Sequential activation of kinases within the mitogen-activated protein (MAP) kinase (MAPK)
cascades is a common, and evolutionary-conserved mechanism of signal transduction. Four …
cascades is a common, and evolutionary-conserved mechanism of signal transduction. Four …
[HTML][HTML] Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR inhibitors: rationale and importance to inhibiting these pathways in human health
WH Chappell, LS Steelman, JM Long, RC Kempf… - Oncotarget, 2011 - ncbi.nlm.nih.gov
Abstract The Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascades are often activated by
genetic alterations in upstream signaling molecules such as receptor tyrosine kinases …
genetic alterations in upstream signaling molecules such as receptor tyrosine kinases …
[HTML][HTML] Mutations and deregulation of Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascades which alter therapy response
JA McCubrey, LS Steelman, WH Chappell… - Oncotarget, 2012 - ncbi.nlm.nih.gov
Abstract The Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascades are often activated by
genetic alterations in upstream signaling molecules such as receptor tyrosine kinases …
genetic alterations in upstream signaling molecules such as receptor tyrosine kinases …
RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models
H Yang, B Higgins, K Kolinsky, K Packman, Z Go… - Cancer research, 2010 - AACR
The BRAFV600E mutation is common in several human cancers, especially melanoma.
RG7204 (PLX4032) is a small-molecule inhibitor of BRAFV600E kinase activity that is in …
RG7204 (PLX4032) is a small-molecule inhibitor of BRAFV600E kinase activity that is in …
Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer
H Yang, B Higgins, K Kolinsky, K Packman… - Cancer research, 2012 - AACR
The protein kinase BRAF is a key component of the RAS–RAF signaling pathway which
plays an important role in regulating cell proliferation, differentiation, and survival. Mutations …
plays an important role in regulating cell proliferation, differentiation, and survival. Mutations …
Mechanisms limiting distribution of the threonine-protein kinase B-RaFV600E inhibitor dabrafenib to the brain: implications for the treatment of melanoma brain …
RK Mittapalli, S Vaidhyanathan, AZ Dudek… - … of Pharmacology and …, 2013 - ASPET
Brain metastases are a common cause of death in stage IV metastatic melanoma.
Dabrafenib is a BRAF (gene encoding serine/threonine-protein kinase B-Raf) inhibitor that …
Dabrafenib is a BRAF (gene encoding serine/threonine-protein kinase B-Raf) inhibitor that …
Discovery of a highly potent and selective MEK inhibitor: GSK1120212 (JTP-74057 DMSO solvate)
H Abe, S Kikuchi, K Hayakawa, T Iida… - ACS medicinal …, 2011 - ACS Publications
Inhibition of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase
(MEK) represents a promising strategy for the discovery of a new generation of anticancer …
(MEK) represents a promising strategy for the discovery of a new generation of anticancer …
Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032)
RK Mittapalli, S Vaidhyanathan, R Sane… - Journal of Pharmacology …, 2012 - ASPET
Vemurafenib [N-(3-{[5-(4-chlorophenyl)-1 H-pyrrolo [2, 3-b] pyridin-3-yl] carbonyl}-2, 4-
difluorophenyl) propane-1-sulfonamide (PLX4032)] is a novel small-molecule BRAF …
difluorophenyl) propane-1-sulfonamide (PLX4032)] is a novel small-molecule BRAF …