Article

Development and utility of a PAK1-selective degrader

2022-05-13

Abstract excerpt

Amplification and/or overexpression of the PAK1 gene is common in several malignancies, and inhibition of PAK1 by small molecules has been shown to impede the growth and survival of such cells. Potent inhibitors of PAK1 and its close relatives, PAK2, and PAK3, have been described, but clinical development has been hindered by recent findings that PAK2 function is required for normal cardiovascular function in adu...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 445ad6cc-6deb-5237-be56-d9a7722ebea2
DOI: 10.1101/2022.05.12.491715

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Development and utility of a PAK1-selective degraderDOI 10.1101/2022.05.12.491715Read

Molecular Pathways: Targeting P21-Activated Kinase 1 Signaling in Cancer—Opportunities, Challenges, and LimitationsSemantic proximity Read

The response to PAK1 inhibitor IPA3 distinguishes between cancer cells with mutations in BRAF and Ras oncogenes.Semantic proximity Read

Brain-Restricted mTOR Inhibition with Binary PharmacologySemantic proximity Read

Rational Design of Potent and Orally Efficacious PI3Kα/δ Degrader for PIK3CA Mutant Breast Cancer without Hyperglycemic Liability.Semantic proximity Read

Brain-Restricted mTOR Inhibition with Binary PharmacologySemantic proximity Read

Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions.Semantic proximity Read

Therapeutic Potential of Targeting PAK SignalingSemantic proximity Read

p21-activated kinase 1 (PAK1) as a therapeutic target for cardiotoxicitySemantic proximity Read

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.Semantic proximity Read

Discovery of a Novel Selective PAK1/HDAC6/HDAC10 Inhibitor ZMF-25 that Induces Mitochondrial Metabolic Breakdown and Autophagy-Related Cell Death in Triple-Negative Breast CancerSemantic proximity Read

Herbal Therapeutics that Block the Oncogenic Kinase PAK1: A Practical Approach towards PAK1-dependent Diseases and LongevitySemantic proximity Read

Structural Insights into the Development of Inhibitors Against Cancer-Specific Mutations of PI3Kα.Semantic proximity Read