GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition
…, MR Bleam, A Groy, KG Moss, EA Minthorn… - Clinical cancer …, 2011 - AACR
Purpose: Despite their preclinical promise, previous MEK inhibitors have shown little benefit
for patients. This likely reflects the narrow therapeutic window for MEK inhibitors due to the …
for patients. This likely reflects the narrow therapeutic window for MEK inhibitors due to the …
Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective …
…, WHH Li, DA Heerding, E Minthorn… - Journal of medicinal …, 2012 - ACS Publications
Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response
to a variety of endoplasmic reticulum stresses implicated in numerous disease states. …
to a variety of endoplasmic reticulum stresses implicated in numerous disease states. …
Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity
C Atkins, Q Liu, E Minthorn, SY Zhang, DJ Figueroa… - Cancer research, 2013 - AACR
The unfolded protein response (UPR) is a signal transduction pathway that coordinates cellular
adaptation to microenvironmental stresses that include hypoxia, nutrient deprivation, and …
adaptation to microenvironmental stresses that include hypoxia, nutrient deprivation, and …
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia
…, CS Kershaw, M Bantscheff, AJ Jurewicz, E Minthorn… - Nature cancer, 2021 - nature.com
DNA methylation, a key epigenetic driver of transcriptional silencing, is universally dysregulated
in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine …
in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine …
Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity
…, AE Choudhry, Z Lai, JD Leber, EA Minthorn… - Cancer research, 2008 - AACR
Akt kinases 1, 2, and 3 are important regulators of cell survival and have been shown to be
constitutively active in a variety of human tumors. GSK690693 is a novel ATP-competitive, low…
constitutively active in a variety of human tumors. GSK690693 is a novel ATP-competitive, low…
Preclinical efficacy and safety of mepolizumab (SB-240563), a humanized monoclonal antibody to IL-5, in cynomolgus monkeys
…, RM Cook, P Zia-Amirhosseini, E Minthorn… - Journal of allergy and …, 2001 - Elsevier
Background: Allergic respiratory diseases are characterized by large numbers of eosinophils
and their reactive products in airways and blood; these are believed to be involved in …
and their reactive products in airways and blood; these are believed to be involved in …
Discovery of GSK2656157: an optimized PERK inhibitor selected for preclinical development
…, SW Grant, DA Heerding, E Minthorn… - ACS medicinal …, 2013 - ACS Publications
We recently reported the discovery of GSK2606414 (1), a selective first in class inhibitor of
protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which inhibited PERK …
protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which inhibited PERK …
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
…, K Federowicz, J Yang, SY Zhang, E Minthorn… - Nature chemical …, 2014 - nature.com
Although therapeutic interventions of signal-transduction cascades with targeted kinase
inhibitors are a well-established strategy, drug-discovery efforts to identify targeted phosphatase …
inhibitors are a well-established strategy, drug-discovery efforts to identify targeted phosphatase …
Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a …
…, RT McConnell, SY Zhang, EA Minthorn… - Journal of medicinal …, 2008 - ACS Publications
Overexpression of AKT has an antiapoptotic effect in many cell types, and expression of
dominant negative AKT blocks the ability of a variety of growth factors to promote survival. …
dominant negative AKT blocks the ability of a variety of growth factors to promote survival. …
[HTML][HTML] Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor
…, D Levy, K Robell, Q Liu, DJ Figueroa, EA Minthorn… - PloS one, 2014 - journals.plos.org
Tumor cells upregulate many cell signaling pathways, with AKT being one of the key kinases
to be activated in a variety of malignancies. GSK2110183 and GSK2141795 are orally …
to be activated in a variety of malignancies. GSK2110183 and GSK2141795 are orally …