Publications by authors named "Rebecca Hong Thibodeau"
Article Synopsis
- * Inavolisib (GDC-0077) is a selective PI3Kα inhibitor that efficiently degrades mutated p110α proteins and has been studied for its absorption, distribution, metabolism, and excretion (ADME) characteristics.
- * Preclinical studies showed that inavolisib is effective against mutant KPL-4 breast cancer models, and predictions suggest a 3 mg dose could yield a clinical response; it is currently in phase 3 trials.
Article Synopsis
- Small molecule inhibitors targeting the PI3K signaling pathway are being researched as cancer treatments, particularly for solid tumors linked to the PI3Kα isoform.
- The study focuses on developing benzoxazepin-oxazolidinone inhibitors that selectively degrade mutant p110α, the active part of PI3Kα, with impressive isoform specificity.
- The resulting clinical candidate, GDC-0077 (inavolisib), shows strong effectiveness in animal models and is currently in a Phase III clinical trial for treating patients with breast cancer harboring PI3Kα mutations.
We examined hematopoietic protein kinase 1 (HPK1), whose reliance on scaffold versus kinase functions for negative immune cell regulation is poorly understood and critical to its assessment as a viable drug target. We identify kinase-dependent roles for HPK1 in CD8 T cells that restrict their anti-viral and anti-tumor responses by using HPK1 kinase-dead (HPK1.kd) knockin mice.
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