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https://www.readbyqxmd.com/read/28098826/hair-growth-promoting-and-anticancer-effects-of-p21-activated-kinase-1-pak1-inhibitors-isolated-from-different-parts-of-alpinia-zerumbet
#1
Nozomi Taira, Binh Cao Quan Nguyen, Shinkichi Tawata
PAK1 (p21-activated kinase 1) is an emerging target for the treatment of hair loss (alopecia) and cancer; therefore, the search for PAK1 blockers to treat these PAK1-dependent disorders has received much attention. In this study, we evaluated the anti-alopecia and anticancer effects of PAK1 inhibitors isolated from Alpinia zerumbet (alpinia) in cell culture. The bioactive compounds isolated from alpinia were found to markedly promote hair cell growth. Kaempferol-3-O-β-d-glucuronide (KOG) and labdadiene, two of the isolated compounds, increased the proliferation of human follicle dermal papilla cells by approximately 117%-180% and 132%-226%, respectively, at 10-100 μM...
January 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28087248/corrigendum-to-git1-beta-pix-signaling-proteins-and-pak1-kinase-regulate-microtubule-nucleation-biochim-biophys-acta-1863-6pa-2016-1282-1297
#2
Markéta Černohorská, Vadym Sulimenko, Zuzana Hájková, Tetyana Sulimenko, Vladimíra Sládková, Stanislav Vinopal, Eduarda Dráberová, Pavel Dráber
No abstract text is available yet for this article.
January 10, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28055013/microrna-494-inhibits-breast-cancer-progression-by-directly-targeting-pak1
#3
Meng-Na Zhan, Xiao-Ting Yu, Jun Tang, Ci-Xiang Zhou, Chen-Long Wang, Qian-Qian Yin, Xiu-Feng Gong, Ming He, Jian-Rong He, Guo-Qiang Chen, Qian Zhao
MicroRNA (miRNA) is involved in the progression and metastasis of diverse human cancers, including breast cancer, as strong evidence has been found that miRNAs can act as oncogenes or tumor suppressor genes. Here, we show that miR-494 is decreased in human breast cancer specimens and breast cancer cell lines. Ectopic expression of miR-494 in basal-like breast cancer cell lines MDA-MB-231-LUC-D2H3LN and BT-549 inhibits clonogenic ability and metastasis-relevant traits in vitro. Moreover, ectopic expression of miR-494 suppresses neoplasm initiation as well as pulmonary metastasis in vivo...
January 5, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28052407/p21-activated-kinase-1-regulates-resistance-to-braf-inhibition-in-human-cancer-cells
#4
Mahamat Babagana, Sydney Johnson, Hannah Slabodkin, Wiam Bshara, Carl Morrison, Eugene S Kandel
BRAF is a commonly mutated oncogene in various human malignancies and a target of a new class of anti-cancer agents, BRAF-inhibitors (BRAFi). The initial enthusiasm for these agents, based on the early successes in the management of metastatic melanoma, is now challenged by the mounting evidence of intrinsic BRAFi-insensitivity in many BRAF-mutated tumors, by the scarcity of complete responses, and by the inevitable emergence of drug resistance in initially responsive cases. These setbacks put an emphasis on discovering the means to increase the efficacy of BRAFi and to prevent or overcome BRAFi-resistance...
January 4, 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/28007610/structure-biochemistry-and-biology-of-pak-kinases
#5
REVIEW
Rakesh Kumar, Rahul Sanawar, Xiaodong Li, Feng Li
PAKs, p21-activated kinases, play central roles and act as converging junctions for discrete signals elicited on the cell surface and for a number of intracellular signaling cascades. PAKs phosphorylate a vast number of substrates and act by remodeling cytoskeleton, employing scaffolding, and relocating to distinct subcellular compartments. PAKs affect wide range of processes that are crucial to the cell from regulation of cell motility, survival, redox, metabolism, cell cycle, proliferation, transformation, stress, inflammation, to gene expression...
December 19, 2016: Gene
https://www.readbyqxmd.com/read/27997893/1%C3%AE-25-oh-2d3-induces-actin-depolymerization-in-endometrial-carcinoma-cells-by-targeting-rac1-and-pak1
#6
Ni Zeng, Madhuri S Salker, Shaqiu Zhang, Yogesh Singh, Bing Shi, Christos Stournaras, Florian Lang
BACKGROUND: Cell proliferation and motility require actin reorganization, which is under control of various signalling pathways including ras-related C3 botulinum toxin substrate 1 (RAC1), p21 protein-activated kinase 1 (PAK1) and actin related protein 2 (ARP2). Tumour cell proliferation is modified by 1α,25-Dihydroxy-Vitamin D3 (1α,25(OH)2D3), a steroid hormone predominantly known for its role in calcium and phosphorus metabolism. The present study explored whether 1α,25(OH)2D3 modifies actin cytoskeleton in Ishikawa cells, a well differentiated endometrial carcinoma cell line...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27994749/optimization-of-highly-kinase-selective-bis-anilino-pyrimidine-pak1-inhibitors
#7
William McCoull, Edward J Hennessy, Kevin Blades, Claudio Chuaqui, James E Dowling, Andrew D Ferguson, Frederick W Goldberg, Nicholas Howe, Christopher R Jones, Paul D Kemmitt, Gillian Lamont, Jeffrey G Varnes, Richard A Ward, Bin Yang
Group I p21-activated kinase (PAK) inhibitors are indicated as important in cancer progression, but achieving high kinase selectivity has been challenging. A bis-anilino pyrimidine PAK1 inhibitor was identified and optimized through structure-based drug design to improve PAK1 potency and achieve high kinase selectivity, giving in vitro probe compound AZ13705339 (18). Reduction of lipophilicity to lower clearance afforded AZ13711265 (14) as an in vivo probe compound with oral exposure in mouse. Such probes will allow further investigation of PAK1 biology...
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27989699/kalirin-a-gef-for-rac1-plays-an-important-role-in-fstl-1-mediated-glucose-uptake-in-skeletal-muscle-cells
#8
Hye Jeong Lee, Jung Ok Lee, Yong Woo Lee, Shin Ae Kim, Sun Hwa Park, Hyeon Soo Kim
Follistatin-like 1 (FSTL-1) is a novel myokine; however, little is known about its metabolic role. Here, FSTL-1 stimulated glucose uptake in an AMP-activated protein kinase (AMPK)-dependent manner in L6 rat skeletal muscle cells. FSTL-1 increased intracellular calcium concentration. Calcium/calmodulin-dependent protein kinase kinase (CaMKK) inhibition blocked FSTL-1-induced AMPK phosphorylation and glucose uptake. In addition, FSTL-1 stimulated the phosphorylation of p21-activated kinase 1 (PAK1), a small GTPase Rac1 downstream protein...
October 29, 2016: Cellular Signalling
https://www.readbyqxmd.com/read/27939839/pharmacological-inhibition-of-rac1-pak1-axis-restores-tamoxifen-sensitivity-in-human-resistant-breast-cancer-cells
#9
N Gonzalez, G A Cardama, M J Comin, V I Segatori, M Pifano, D F Alonso, D E Gomez, P L Menna
Tamoxifen is a standard endocrine therapy for estrogen receptor positive breast cancer patients. Despite its success, development of resistance mechanisms is still a serious clinical problem. Deregulation of survival signaling pathways play a key role in tamoxifen resistance, being upregulation of Rac1-PAK1 signaling pathway one of the most important. Here, we report the development of the breast cancer cell model MCF7::C1199 having Rac1 enhanced activity with the aim of evaluating the role of Rac1 in acquired endocrine resistance...
January 2017: Cellular Signalling
https://www.readbyqxmd.com/read/27939356/the-origins-of-rimmed-vacuoles-and-granulovacuolar-degeneration-bodies-are-associated-with-the-wnt-signaling-pathway
#10
Yukari Murata-Shinozaki, Tetsuya Takahashi, Tomoyasu Matsubara, Hirofumi Maruyama, Yuishin Izumi, Masayasu Matsumoto
Inclusion-body myositis (IBM) and Alzheimer's disease (AD) are biochemically characterized by the presence of aggregated β-amyloid protein and tau protein. In addition, both diseases are pathologically characterized by vacuolar changes, including rimmed vacuoles (RVs) in IBM and granulovacuolar degeneration (GVD) in AD. Previously, we demonstrated that RVs and GVD bodies are associated with a set of common molecules, leading us to speculate that both RVs and GVD bodies originate from similar structures on the plasma membrane of muscle cells and neuronal cells, namely, the neuromuscular junction (NMJ) and the postsynaptic spine especially in terms of Wnt signaling pathway...
December 7, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27934900/corrigendum-pak1-confers-chemoresistance-and-poor-outcome-in-non-small-cell-lung-cancer-via-%C3%AE-catenin-mediated-stemness
#11
Ming-Jenn Chen, De-Wei Wu, Yao-Chen Wang, Chi-Yi Chen, Huei Lee
No abstract text is available yet for this article.
December 9, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27930339/growth-hormone-releasing-hormone-receptor-antagonists-inhibit-human-gastric-cancer-through-downregulation-of-pak1-stat3-nf-%C3%AE%C2%BAb-signaling
#12
Jinfeng Gan, Xiurong Ke, Jiali Jiang, Hongmei Dong, Zhimeng Yao, Yusheng Lin, Wan Lin, Xiao Wu, Shumei Yan, Yixuan Zhuang, Wai Kit Chu, Renzhi Cai, Xianyang Zhang, Herman S Cheung, Norman L Block, Chi Pui Pang, Andrew V Schally, Hao Zhang
Gastric cancer (GC) ranks as the fourth most frequent in incidence and second in mortality among all cancers worldwide. The development of effective treatment approaches is an urgent requirement. Growth hormone-releasing hormone (GHRH) and GHRH receptor (GHRH-R) have been found to be present in a variety of tumoral tissues and cell lines. Therefore the inhibition of GHRH-R was proposed as a promising approach for the treatment of these cancers. However, little is known about GHRH-R and the relevant therapy in human GC...
December 20, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27923043/clonal-evolutionary-analysis-during-her2-blockade-in-her2-positive-inflammatory-breast-cancer-a-phase-ii-open-label-clinical-trial-of-afatinib-vinorelbine
#13
Gerald Goh, Ramona Schmid, Kelly Guiver, Wichit Arpornwirat, Imjai Chitapanarux, Vinod Ganju, Seock-Ah Im, Sung-Bae Kim, Arunee Dechaphunkul, Jedzada Maneechavakajorn, Neil Spector, Thomas Yau, Mehdi Afrit, Slim Ben Ahmed, Stephen R Johnston, Neil Gibson, Martina Uttenreuther-Fischer, Javier Herrero, Charles Swanton
BACKGROUND: Inflammatory breast cancer (IBC) is a rare, aggressive form of breast cancer associated with HER2 amplification, with high risk of metastasis and an estimated median survival of 2.9 y. We performed an open-label, single-arm phase II clinical trial (ClinicalTrials.gov NCT01325428) to investigate the efficacy and safety of afatinib, an irreversible ErbB family inhibitor, alone and in combination with vinorelbine in patients with HER2-positive IBC. This trial included prospectively planned exome analysis before and after afatinib monotherapy...
December 2016: PLoS Medicine
https://www.readbyqxmd.com/read/27920252/group-i-paks-promote-skeletal-myoblast-differentiation-in-vivo-and-in-vitro
#14
Giselle A Joseph, Min Lu, Maria Radu, Jennifer K Lee, Steven J Burden, Jonathan Chernoff, Robert S Krauss
Skeletal myogenesis is regulated by signal transduction, but the factors and mechanisms involved are not well understood. The group I Paks, Pak1 and Pak2, are related protein kinases and direct effectors of Cdc42 and Rac1. Group I Paks are ubiquitously expressed and specifically required for myoblast fusion in Drosophila We report that both Pak1 and Pak2 are activated during mammalian myoblast differentiation. One pathway of activation is initiated by N-cadherin ligation, and involves the cadherin co-receptor Cdo with its downstream effector, Cdc42...
December 5, 2016: Molecular and Cellular Biology
https://www.readbyqxmd.com/read/27913610/whole-exome-sequencing-of-thymic-neuroendocrine-tumor-with-ectopic-acth-syndrome
#15
Yanli Li, Ying Peng, Xiuli Jiang, Yulong Cheng, Weiwei Zhou, Tingwei Su, Jing Xie, Xu Zhong, Dalong Song, Luming Wu, Liwen Fan, Min Li, Jie Hong, Weiqing Wang, Guang Ning, Yanan Cao
OBJECTIVE: Thymic neuroendocrine tumor is the second-most prevalent cause of ectopic adrenocorticotropic hormone (ACTH) syndrome (EAS), which is a rare disease characterized by ectopic ACTH oversecretion from nonpituitary tumors. However, the genetic abnormalities of thymic neuroendocrine tumors with EAS remain largely unknown. We aim to elucidate the genetic abnormalities and identify the somatic mutations of potential tumor-related genes of thymic neuroendocrine tumors with EAS by whole exome sequencing...
February 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/27910850/the-guanine-nucleotide-exchange-factor-net1-facilitates-the-specification-of-dorsal-cell-fates-in-zebrafish-embryos-by-promoting-maternal-%C3%AE-catenin-activation
#16
Shi Wei, Miaomiao Dai, Zhaoting Liu, Yuanqing Ma, Hanqiao Shang, Yu Cao, Qiang Wang
Wnt/β-catenin signaling is essential for the initiation of dorsal-ventral patterning during vertebrate embryogenesis. Maternal β-catenin accumulates in dorsal marginal nuclei during cleavage stages, but its critical target genes essential for dorsalization are silent until mid-blastula transition (MBT). Here, we find that zebrafish net1, a guanine nucleotide exchange factor, is specifically expressed in dorsal marginal blastomeres after MBT, and acts as a zygotic factor to promote the specification of dorsal cell fates...
December 2, 2016: Cell Research
https://www.readbyqxmd.com/read/27889630/1-2-3-triazolyl-ester-of-ketorolac-a-click-chemistry-based-highly-potent-pak1-blocking-cancer-killer
#17
Binh Cao Quan Nguyen, Hideaki Takahashi, Yoshihiro Uto, M D Shahinozzaman, Shinkichi Tawata, Hiroshi Maruta
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 (cyclooxygenase-2) signaling, through the direct inhibition of RAC by the R-form and of COX-2 by the S-form, eventually down-regulating the production of prostaglandins. However, due to its COOH moiety which is clearly repulsive to negatively-charged phospholipid-based plasma membrane, its cell-permeability is rather poor (the IC50 against the growth of human cancer cells such as A549 is around 13 μM)...
November 20, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27889228/cardioprotective-effect-of-vitex-negundo-on-isoproterenol-induced-myocardial-necrosis-in-wistar-rats-a-dual-approach-study
#18
E Maruthi Prasad, Ramgopal Mopuri, Md Shahidul Islam, Lakshmi Devi Kodidhela
Cardiovascular diseases (CVDs) are becoming the major cause of deaths worldwide, and their treatment demands novel therapeutic strategies. In this connection, we have identified p21 activated kinase 1 (PAK1) as a novel therapeutic target for the treatment of myocardial infarction (MI), where its expression is decreased when MI is induced with isoproterenol (ISO), which was brought back normal with pretreatment of Vitex negundo leaf ethanolic extract (VNE). These results were also supported by histopathological studies, cardiac markers, antioxidants, and inflammatory cytokines (NF-κB and IL-1β)...
January 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27885255/tfap2c-mediated-upregulation-of-tgfbr1-promotes-lung-tumorigenesis-and-epithelial-mesenchymal-transition
#19
Wanyeon Kim, EunGi Kim, Sungmin Lee, Daehoon Kim, Jahyun Chun, Kang Hyun Park, HyeSook Youn, BuHyun Youn
TFAP2C (transcription factor-activating enhancer-binding protein 2C) expression has been positively correlated with poor prognosis in patients with certain types of cancer, but the mechanisms underlying TFAP2C-mediated tumorigenesis in non-small-cell lung cancer (NSCLC) are still unknown. We previously performed a microarray analysis to identify TFAP2C regulation genes, and TGFBR1 (transforming growth factor-β receptor type 1) was found to be upregulated by TFAP2C. We observed that TFAP2C or TGFBR1 overexpression led to oncogenic properties, such as cell viability, proliferation and cell cycle progression...
November 25, 2016: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/27861142/newcastle-disease-virus-employs-macropinocytosis-and-rab5a-dependent-intracellular-trafficking-to-infect-df-1-cells
#20
Lei Tan, Yuqiang Zhang, Yuan Zhan, Yanmei Yuan, Yingjie Sun, Xusheng Qiu, Chunchun Meng, Cuiping Song, Ying Liao, Chan Ding
Oncolytic Newcastle disease virus (NDV) reportedly employs direct fusion of the viral envelope with the plasma membrane and caveolae-dependent endocytosis to enter cells. Here, we show that macropinocytosis and clathrin-mediated endocytosis are involved in NDV entry into a galline embryonic fibroblast cell line. Upon specific inhibition of clathrin assembly, GTPase dynamin, Na+/H+ exchangers, Ras-related C3 botulinum toxin substrate 1, p21 activated kinase 1 or protein kinase C, entry of NDV and its propagation were suppressed...
November 15, 2016: Oncotarget
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