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Click link to view article https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.1c00905 Abstract Aberrant activation of the mitogen-activated protein kinase pathway frequently drives tumor growth, and the ERK1/2 kinases are positioned at a key node in this pathway, making them important targets for therapeutic intervention. Recently, a number of ERK1/2 inhibitors have been advanced to investigational clinical trials in patients with […]

Munck et al., “ASTX029, a Novel Dual-Mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK”

15 August 2021/in 2021, ASTX029 - Solid Tumors, Products

Click link to view article https://mct.aacrjournals.org/content/early/2021/07/30/1535-7163.MCT-20-0909#:~:text=ASTX029%20is%20a%20highly%20potent,not%20directly%20inhibiting%20MEK%20activity Abstract The MAPK signaling pathway is commonly upregulated in human cancers. As the primary downstream effector of the MAPK pathway, ERK is an attractive therapeutic target for the treatment of MAPK-activated cancers and for overcoming resistance to upstream inhibition. ASTX029 is a highly potent and selective dual-mechanism ERK inhibitor, […]

Almeida et al., “NMR Reporter Assays for the Quantification of Weak-Affinity Receptor–Ligand Interactions”; SLAS Discovery, April 2021

25 May 2021/in 2021, Discovery, Publications

https://doi.org/10.1177/24725552211009782

Poon et al., “The role of SQSTM1 (p62) in mitochondrial function and clearance in human cortical neurons”; Stem Cell Reports 2021

22 April 2021/in 2021, Discovery, Publications

https://doi.org/10.1016/j.stemcr.2021.03.030

Chessari at al. Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction; Med Chem 2021

24 March 2021/in 2021, 2021, ASTX295 - Solid Tumors, Discovery, Products, Publications

https://doi.org/10.1021/acs.jmedchem.0c02188

Sethi et al., “Leveraging omic features with F3UTER enables identification of unannotated 3’UTRs for synaptic genes”

9 March 2021/in 2021, Discovery, Publications

https://www.nature.com/articles/s41467-022-30017-z
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de Esch et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2020”; J. Med. Chem. 2022

Rees., “Medicines for millions of patients”; RSC Medicinal Chemistry, Jan 2022

Norton et al., “Fragment-Guided Discovery of Pyrazole Carboxylic 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. 2021

Chessari et al., “C–H functionalisation tolerant to polar groups could transform fragment-based drug discovery (FBDD)”; Chemical Science, 2021

Heightman et al., “Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2”

Munck et al., “ASTX029, a Novel Dual-Mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK”

Almeida et al., “NMR Reporter Assays for the Quantification of Weak-Affinity Receptor–Ligand Interactions”; SLAS Discovery, April 2021

Poon et al., “The role of SQSTM1 (p62) in mitochondrial function and clearance in human cortical neurons”; Stem Cell Reports 2021

Chessari at al. Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction; Med Chem 2021

Sethi et al., “Leveraging omic features with F3UTER enables identification of unannotated 3’UTRs for synaptic genes”

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