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2d
Computational validation of inhibitors for human phosphatidylinositol 4-phosphate 5-kinase-type 1 α protein implicated in cancer. (PubMed, J Biomol Struct Dyn)
Four protein kinase inhibitors, R547, GDC-0879, JNJ-7706621 and ABT-869 were found to bind hPIP5K1α via a stable complex formation. The hit molecules display favorable ADME properties and are predicted to be non-carcinogenic. The hit molecules in particular R547, have better binding free energies compared to reference molecule, ISA-2011B.
Journal
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PIP5K1A (Phosphatidylinositol-4-Phosphate 5-Kinase Type 1 Alpha)
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GDC 0879 • linifanib (ABT-869) • R-547
17d
Benign Keratoses With Inverted Follicular Keratosis-Like Features in a Patient Receiving Ripretinib: A Case Report. (PubMed, J Cutan Pathol)
Inverted follicular keratosis (IFK) is a rare benign neoplasm of the follicular infundibulum and typically presents as a solitary, nonpigmented verrucous papule on the head and neck of older males and can mimic viral warts, basal cell carcinoma (BCC), or squamous cell carcinoma (SCC). To the best of our knowledge, this represents the first reported association between repretinib treatment and benign keratoses with IFK-like features. Further studies are needed to clarify the clinical significance and biological implications of this observation.
Journal
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PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
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Qinlock (ripretinib)
22d
Ultrasound-triggered dissolving microneedle platform for cGAS-STING-mediated precision immunotherapy of melanoma. (PubMed, Mater Today Bio)
Herein, we reported an ultrasound (US)-controllable all-in-one dissolving microneedle (dMN) platform that integrated a ROS-cleavable prodrug, formed by conjugating the VEGF inhibitor linifanib, with ROS-responsive liposomes encapsulating the sonosensitizer MnTCPP (Mn@CTL-LPs dMNs)...This spatiotemporally controllable activation ensured high therapeutic precision and safety. Overall, this work presented a noninvasive and US-triggered strategy to potentiate sonodynamic immunotherapy for melanoma.
Journal
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CD8 (cluster of differentiation 8) • STING (stimulator of interferon response cGAMP interactor 1)
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linifanib (ABT-869)
1m
EGFR/KIT-linked proliferative bias in normal breast lobules from matched non-Hispanic Black and White women is rapidly reversible by RTK inhibition. (PubMed, Am J Pathol)
Functional plausibility was assessed in pre-stasis human mammary epithelial cells (HMECs) exposed for 24 h to clinically relevant EGFR (lapatinib) or KIT (ripretinib) inhibitors. Together, matched normal tissue and primary-cell data indicate a coordinated EGFR/KIT-linked proliferative bias in NHBW epithelium that is rapidly reversible in vitro. These findings motivate composition-aware validation in larger normal-tissue cohorts and pharmacodynamic window studies to test whether short-term RTK modulation can reset proliferation-biased states in at-risk breast epithelium.
Journal
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EGFR (Epidermal growth factor receptor) • CDK4 (Cyclin-dependent kinase 4)
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lapatinib • Qinlock (ripretinib)
1m
EMBARQ-CSU1: A Phase 3 Study of Barzolvolimab in Participants With Chronic Spontaneous Urticaria (clinicaltrials.gov)
P3, N=963, Active, not recruiting, Celldex Therapeutics | Recruiting --> Active, not recruiting
Enrollment closed
1m
EMBARQ-CSU2: A Phase 3 Study of Barzolvolimab in Participants With Chronic Spontaneous Urticaria (CSU) (clinicaltrials.gov)
P3, N=976, Active, not recruiting, Celldex Therapeutics | Recruiting --> Active, not recruiting
Enrollment closed
1m
A Phase 2, Open-Label, Extension Study to Evaluate Long Term Safety and Clinical Activity of Briquilimab in Participants From Jasper-Sponsored Chronic Urticaria Trials (clinicaltrials.gov)
P2, N=67, Active, not recruiting, Jasper Therapeutics, Inc. | Enrolling by invitation --> Active, not recruiting | Trial primary completion date: Dec 2026 --> Aug 2026
Enrollment closed • Trial primary completion date
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briquilimab (JSP191)
1m
New P1/2 trial