p21-activated kinase 1 (PAK1) has attracted much attention as a potential therapeutic target due to its central role in many oncogenic signaling pathways, its frequent dysregulation in cancers and neurological disorders, and its tractability as a target for small-molecule inhibition.

Studies have revealed that miR-485-5p 79, miR-140-5p 80, miR-96 81, miR-7 82, miR-494 83, miR-34b 84, and miR-145 85 can directly target and degrade the mRNA of PAK1 in order to block the translation of PAK1.

Recently, for a clinical application, a few potent (highly cell-permeable and water-soluble) PAK1 blockers have been developed from natural or synthetic PAK1 blockers (triptolide, vitamin D3 and ketorolac) via a series of ‘chemical evolutions’ that boost pharmacological activities >500 times.

Jun 1, 2020 · Several PAK1-blockers such as propolis, melatonin, anti-malaria drugs, ivermectin, cicloresonide and ketorolac are readily available in the market. PAK1-blockers, interfering with the pathogenic process as well as promoting immune system, could serve as potential therapeutic agents against COVID-19.

Here, I outline mainly pathological phenotypes of hyper-activated PAK1 and a list of herbal therapeutics that block PAK1, but cause no side (harmful) effect on healthy people or animals.

Recently we and others found that even a few synthetic PAK1-blockers such as 15K, highly cell-permeable 1,2,3-triazolyl ester of an old pain killer called Ketorolac are able to boost both lifespan and heat-endurance of C. elegans, while they down-regulate the fertility.

Here we provide the first evidence that extracts of Chinese/ Japanese peppercorns (Zanthoxyli Fructus) from the plant Zanthoxylum piperitum called "Hua Jiao"/"Sansho", block selectively the key kinase PAK1, leading to the downregulation of cyclin D1.

Dec 15, 2017 · Our major aim in the “PAK1-blocker project” is to identify and develop the clinically useful (“highly cell-permeable” and “water-soluble”) compounds that block the oncogenic PAK1 signalling pathway somehow without any side effect.

The p21-activated kinase (PAK1), a serine/threonine protein kinase, is critical in regulating various cellular processes, including muscle contraction, neutrophil chemotaxis, neuronal polarization, and endothelial barrier function.

Sep 25, 2006 · p21-activated kinase 1 (PAK1) is a mediator of downstream signaling from the small GTPases Rac and Cdc42. In its inactive state, PAK1 forms a homodimer where two kinases inhibit each other...