Search Results - "Maruta, Hiroshi"
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Chemical evolution for taming the ‘pathogenic kinase’ PAK1
Published in Drug discovery today (01-06-2020)“…•PAK1 is the major ‘pathogenic’ kinase.•Several potent PAK1 blockers developed are introduced for treatment of a wide variety of PAK1-dependent diseases…”
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Rapamycin vs TORin-1 or Gleevec vs Nilotinib: Simple chemical evolution that converts PAK1-blockers to TOR-blockers or vice versa?
Published in Drug Discoveries & Therapeutics (06-06-2024)“…Both PAK1 (RAC/CDC42-activating kinase 1) and TOR (Target of Rapamycin) are among the major oncogenic/ageing kinases. However, they play the opposite role in…”
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From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy
Published in European journal of medicinal chemistry (15-12-2017)“…PAK family kinases are RAC/CDC42-activated kinases that were first found in a soil amoeba 4 decades ago, and 2 decades later, were discovered in mammals as…”
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Probiotic microbes: Are their anti-melanogenicity and longevity promoting activities closely linked through the major "pathogenic" kinase PAK1?
Published in Drug Discoveries & Therapeutics (28-02-2022)“…PAK1-deficient mutant of C. elegans lives 60% longer than the wild-type. Interestingly, PAK1-deficient mutant of melanocytes produces less melanin (only a half…”
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1,2,3-Triazolyl ester of Ketorolac: A “Click Chemistry”-based highly potent PAK1-blocking cancer-killer
Published in European journal of medicinal chemistry (27-01-2017)“…An old anti-inflammatory/analgesic drug called Toradol is a racemic form of Ketorolac (50% R-form and 50% S-form) that blocks the oncogenic RAC-PAK1-COX-2…”
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Artepillin C and Other Herbal PAK1‐blockers: Effects on Hair Cell Proliferation and Related PAK1‐dependent Biological Function in Cell Culture
Published in Phytotherapy research (01-01-2016)“…PAK1 (RAC/CDC42‐activated kinase 1) is the major oncogenic kinase, and a number of herbal PAK1‐blockers such as propolis and curcumin have been shown to be…”
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PAK1-blockers: Potential Therapeutics against COVID-19
Published in Medicine in drug discovery (01-06-2020)“…PAK1 (RAC/CDC42-activated kinase 1) is the major “pathogenic” kinase whose abnormal activation causes a wide variety of diseases/disorders including cancers,…”
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Frondoside A from sea cucumber and nymphaeols from Okinawa propolis: Natural anti-cancer agents that selectively inhibit PAK1 in vitro
Published in Drug Discoveries & Therapeutics (30-05-2017)“…A sulfated saponin called "Frondoside A" (FRA) from sea cucumber and ingredients from Okinawa propolis (OP) have been previously shown to suppress the…”
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Alert Regarding Cisplatin-induced Severe Adverse Events in Cancer Patients with Xeroderma Pigmentosum
Published in Internal Medicine (01-01-2017)“…Xeroderma pigmentosum (XP) is a genetic disease in which DNA repair mechanisms are impaired. Cisplatin (CDDP) exerts cytotoxic effects by forming mainly…”
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1,2,3-Triazolyl esterization of PAK1-blocking propolis ingredients, artepillin C (ARC) and caffeic acid (CA), for boosting their anti-cancer/anti-PAK1 activities along with cell-permeability
Published in Drug Discoveries & Therapeutics (30-05-2017)“…Artepillin C (ARC) and caffeic acid (CA) are among the major anti-cancer ingredients of propolis, and block the oncogenic/melanogenic/ageing kinase PAK1…”
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Effective neurofibromatosis therapeutics blocking the oncogenic kinase PAK1
Published in Drug Discoveries & Therapeutics (01-01-2011)“…Neurofibromatosis (NF) is a family of genetic diseases which are caused by dysfunction of either NF1 gene or NF2 gene. One in 3,000 people suffer from this…”
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1,2,3-Triazolyl ester of ketorolac (15K), a potent PAK1 blocker, inhibits both growth and metastasis of orthotopic human pancreatic cancer xenografts in mice
Published in Drug Discoveries & Therapeutics (31-10-2019)“…More than 90% of human pancreatic cancers carry the oncogenic mutant of Ki-RAS and their growth depends on its downstream kinase PAK1, mainly because PAK1…”
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Artepillin C (ARC) in Brazilian green propolis selectively blocks oncogenic PAK1 signaling and suppresses the growth of NF tumors in mice
Published in Phytotherapy research (01-03-2009)“…There are mainly three types of propolis whose major anticancer ingredients are entirely different: (1) CAPE (caffeic acid phenethyl ester)-based propolis in…”
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1,2,3-Triazolyl ester of ketorolac (15K): Boosting both heat-endurance and lifespan of C. elegans by down-regulating PAK1 at nM levels
Published in Drug Discoveries & Therapeutics (30-04-2018)“…PAK1 (RAC/CDC42-activated kinase 1) is the major oncogenic/ageing kinase, and its dysfunction extends the healthy lifespan of C. elegans by activating HSP16…”
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PAK1-deficiency/down-regulation reduces brood size, activates HSP16.2 gene and extends lifespan in Caenorhabditis elegans
Published in Drug Discoveries & Therapeutics (01-02-2013)“…There is an increasing evidence that the oncogenic kinase PAK1 is responsible not only for malignant transformation, but also for several other diseases such…”
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Both triazolyl ester of ketorolac (15K) and YM155 inhibit the embryonic angiogenesis in ovo (fertilized eggs) via their common PAK1-survivin/VEGF signaling pathway
Published in Drug Discoveries & Therapeutics (2017)“…15 K is 1,2, 3-triazolyl ester of ketorolac, an old pain-killer, that blocks PAK1 by its R-form and inhibits COX-2 by its S-form. Mainly due to a robust…”
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Herbal Therapeutics that Block the Oncogenic Kinase PAK1: A Practical Approach towards PAK1‐dependent Diseases and Longevity
Published in Phytotherapy research (01-05-2014)“…Over 35 years research on PAKs, RAC/CDC42(p21)‐activated kinases, comes of age, and in particular PAK1 has been well known to be responsible for a variety of…”
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Combination of immunoprecipitation (IP)-ATP_Glo kinase assay and melanogenesis for the assessment of potent and safe PAK1-blockers in cell culture
Published in Drug Discoveries & Therapeutics (01-08-2015)“…Cucurbitacin I (CBI) is a triterpene from a bitter melon called Goya grown in Okinawa, Japan, and directly inhibits both the Tyr-kinase JAK2 and the G protein…”
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The serum/PDGF-dependent "melanogenic" role of the minute level of the oncogenic kinase PAK1 in melanoma cells proven by the highly sensitive kinase assay
Published in Drug Discoveries & Therapeutics (2016)“…We previously demonstrated that the oncogenic kinase PAK4, which both melanomas and normal melanocytes express at a very high level, is essential for their…”
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Signal therapy of human pancreatic cancer and NF1 -deficient breast cancer xenograft in mice by a combination of PP1 and GL-2003, anti-PAK1 drugs (Tyr-kinase inhibitors)
Published in Cancer letters (08-01-2007)“…Abstract The majority of cancers are caused by mutations of a few signal transducers such as the GTPase RAS, the kinase Src and the tumor suppressor p53. Thus,…”
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