Publications by authors named "T Heffron"
Article Synopsis
- HPK1 is a negative regulator of T-cell receptor signaling, and its inhibition can enhance immune responses and work well with immune checkpoint inhibitors in cancer models.
- Researchers have discovered a new series of isoquinoline compounds that effectively inhibit HPK1 and promote T-cell activity through fragment-based screening.
- The best candidate from these efforts showed strong inhibition of HPK1, excellent selectivity for other kinases, a good safety profile, and favorable pharmacokinetic properties for potential cancer immunotherapy use.
Unlabelled: Challenges exist in access to high-quality care for insomnia disorder. After the recent publication of a clinical practice guideline on behavioral and psychological treatments for insomnia in adults, the American Academy of Sleep Medicine (AASM) hosted a 1-day virtual Insomnia Summit in September 2022 to discuss improving care for patients with insomnia disorder. Fifty participants representing a variety of organizations (eg, medical, psychological, and nursing associations; patient advocacy groups; and federal institutions) participated in the event.
View Article and Find Full Text PDFArticle Synopsis
- KRAS G12C is a commonly mutated oncogene that presents a new opportunity for targeted cancer treatment, with GDC-6036 being a specific inhibitor.
- The drug works by binding to KRAS G12C in its inactive state, preventing it from activating and promoting tumor growth.
- Researchers developed a highly sensitive test to measure how well GDC-6036 binds to KRAS G12C in biopsy samples, achieving a level of sensitivity that could enhance cancer drug development and monitoring.
Hematopoietic progenitor kinase 1 (HPK1) is implicated as a negative regulator of T-cell receptor-induced T-cell activation. Studies using HPK1 kinase-dead knock-in animals have demonstrated the loss of HPK1 kinase activity resulted in an increase in T-cell function and tumor growth inhibition in glioma models. Herein, we describe the discovery of a series of small molecule inhibitors of HPK1.
View Article and Find Full Text PDFArticle Synopsis
- The p110a protein, a frequently mutated oncogene, is crucial for tumor growth, and new small-molecule inhibitors like GDC-0077 are showing promise in clinical trials for treating mutant breast cancer.
- Early studies highlight that while these inhibitors can effectively attack tumor cells, they may inadvertently activate compensatory signaling pathways that reduce their effectiveness.
- Recent findings reveal that GDC-0077 and taselisib uniquely degrade the mutant p110a protein, offering a more effective and targeted approach to inhibiting cancer pathways, especially in HER2-positive breast cancer patients.