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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

Astex Pharmaceuticals Celebrates as Second New Cancer Drug Receives US Marketing Approval

Astex Pharmaceuticals Celebrates as Second New Cancer Drug Receives US Marketing Approval Further Milestone from Janssen on NDA Approval by the US FDA of BALVERSA™ (erdafitinib) for the Treatment of Urothelial Cancer Cambridge, UK, 12 April 2019. Astex Pharmaceuticals (Astex), a pharmaceutical company dedicated to the discovery and development of novel small molecule therapeutics for oncology and diseases of the central nervous system, announced […]