The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of…

By A. Folkes, K. Ahmadi, W. Alderton, Sonia Alix, S. Baker, G. Box, Irina S. Chuckowree, P. Clarke, P. Depledge, S. Eccles and 24 more. Journal of Medicinal Chemistry, 2008

761 citations recorded by the source corpus.

Subfields: Genetics, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/f8325ea967c7bf19ff5fc382aee7e458187318e9

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In Molecular Biology

1. M. Sliwkowski
2. M. Lacouture

Citations in the corpus

• Targeting PI3K/Akt signal transduction for cancer therapy (2021, background): “As a pan-class I PI3K inhibitor, GDC-0941 shows the same activity (IC50= 3 nM) against p110α and p110δ enzymes, and in kinase assays, it exerts an inhibitory effect on p110β and p110γ at nanomolar concentrations.(196) Experiments have shown that monotherapy or combination therapy with GDC0941 and ot”
• Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941. (2009, background): “First, GDC-0941 is highly selective for class IA PI3K (Folkes et al., 2008).”
• Apoptosis as anticancer mechanism: function and dysfunction of its modulators and targeted therapeutic strategies (2016, background): “In this regard, KRAS and the PI3K/AKT/mTOR pathway are frequently dysregulated in cancer and, for such reason, are the most critical targets in clinical oncology.”