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Kidger et al. “Dual-mechanism ERK1/2 inhibitors exploit a distinct binding mode to block phosphorylation and nuclear accumulation of ERK1/2”, Molecular Cancer Therapeutics, 2019

Kidger et al., “Dual-mechanism ERK1/2 inhibitors exploit a distinct binding mode to block phosphorylation and nuclear accumulation of ERK1/2“, Molecular Cancer Therapeutics, 2019 https://mct.aacrjournals.org/content/early/2019/11/20/1535-7163.MCT-19-0505

2019: Dual-mechanism ERK1/2 inhibitors exploit a distinct binding mode to block phosphorylation and nuclear accumulation of ERK1/2

Summary The RAS-regulated RAF-MEK1/2-ERK1/2 signalling pathway is frequently deregulated in cancer due to activating mutations of growth factor receptors, RAS or BRAF. Both RAF and MEK1/2 inhibitors are clinically approved and various ERK1/2 inhibitors (ERKi) are currently undergoing clinical trials. To date ERKi display two distinct mechanisms of action (MoA); catalytic ERKi solely inhibit ERK1/2 […]

A novel ERK inhibitor has potent activity in NRAS-mutant melanoma cancer models

Introduction NRAS mutations occur in 15-20% of mutant melanoma cancer patients. Currently there is no approved therapy for NRAS-mutant melanoma, an indication which is associated with aggressive clinical outcome and a poor prognosis. The NRAS mutation leads to constitutive activation of the MAPK pathway. ERK is the primary downstream effector of MAPK and its direct […]

Murray et al., “A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA”; MedChemComm, 2019

Murray et al., “A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA”, MedChemComm, 2019; https://pubs.rsc.org/en/content/articlepdf/2019/MD/C9MD90044F

British Company Behind Groundbreaking Breast Cancer Treatment

Astex welcomes positive, new data showing breast cancer drug, Kisqali® (ribociclib), cuts risk of death by up to a third when given with hormone therapy Cambridge, UK, 7 June 2019. A new set of statistically significant overall survival (OS) data unveiled at the 2019 American Society of Clinical Oncology (ASCO) Annual Meeting (Abstract# LBA1008), and published in The New […]

Heightman et al., “Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction.” J. Med. Chem., 2019; DOI: 10.1021/acs.jmedchem.9b00279

Heightman et al., “Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction.” J. Med. Chem., 2019; DOI: 10.1021/acs.jmedchem.9b00279