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https://www.readbyqxmd.com/read/29667555/synthesis-cytotoxicity-and-antioxidant-activity-of-new-analogues-of-rc-121-synthetic-derivatives-of-somatostatin
#1
Diana Wesselinova, Emilia D Naydenova, S Staykova, I G Goshev, L Vezenkov
BACKGROUND: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. OBJECTIVES: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). METHODS: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (human colorectal cancer cell line), MDA-MB-23 (human breast cancer cell line), Hep G-2 (human hepatocellular carcinoma cell line) and HeLa (cervical cancer cell line)...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29665367/suppression-of-akt-mediated-hdac3-expression-and-cdk2-t39-phosphorylation-by-a-bichalcone-analog-contributes-to-s-phase-retardation-of-cancer-cells
#2
Kuang-Chen Hung, Meng-Liang Lin, Shih-Wei Hsu, Chuan-Chun Lee, Ren-Yu Huang, Tian-Shung Wu, Shih-Shun Chen
Targeting cell cycle regulators has been a suggested mechanism for therapeutic cancer strategies. We report here that the bichalcone analog TSWU-CD4 induces S phase arrest of human cancer cells by inhibiting the formation of cyclin A-phospho (p)-cyclin-dependent kinase 2 (CDK2, threonine [Thr] 39) complexes, independent of mutant p53 expression. Ectopic expression of CDK2 (T39E), which mimics phosphorylation of the Thr 39 residue of CDK2, partially rescues the cells from TSWU-CD4-induced S phase arrest, whereas phosphorylation-deficient CDK2 (T39A) expression regulates cell growth with significant S phase arrest and enhances TSWU-CD4-triggered S phase arrest...
April 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29662197/mekk2-and-mekk3-suppress-hedgehog-pathway-dependent-medulloblastoma-by-inhibiting-gli1-function
#3
Jinqiu Lu, Liansheng Liu, Mingjie Zheng, Xiaoling Li, Ailing Wu, Qingzhe Wu, Cheng Liao, Jian Zou, Hai Song
Hedgehog (Hh) pathway plays a pivotal role in diverse aspects of development and postnatal physiology. Perturbation of Hh signaling and activation of GLI1 (glioma-associated oncogene 1), a dedicated transcription factor for Hh pathway, are highly associated with several cancers, such as medulloblastoma and basal cell carcinoma. Dynamic and precise control of GLI1 activity is thus important to ensure proper homeostasis and tumorigenesis. Here we show that MEKK2 (MAP3K2) and MEKK3 (MAP3K3) inhibit GLI1 transcriptional activity and oncogenic function through phosphorylation on multiple Ser/Thr sites of GLI1, which reduces GLI1 protein stability, DNA-binding ability, and increases the association of GLI1 with SUFU...
April 17, 2018: Oncogene
https://www.readbyqxmd.com/read/29618060/tn-and-stn-are-members-of-a-family-of-carbohydrate-tumor-antigens-that-possess-carbohydrate-carbohydrate-interactions
#4
Marit Sletmoen, Thomas A Gerken, Bjørn T Stokke, Joy Burchell, C Fred Brewer
The mucin-type O-glycome in cancer aberrantly expresses the truncated glycans Tn (GalNAcα1-Ser/Thr) and STn (Neu5Acα2,6GalNAcα1Ser/Thr). However, the role of Tn and STn in cancer and other diseases is not well understood. Our recent discovery of the self-binding properties (carbohydrate-carbohydrate interactions) of Tn (Tn - Tn) and STn (STn - STn) provides a model for their possible roles in cellular transformation. We also review evidence that Tn and STn are members of a larger family of glycan tumor antigens that possess carbohydrate-carbohydrate interactions, which may participate in oncogenesis...
April 3, 2018: Glycobiology
https://www.readbyqxmd.com/read/29581234/traf-interacting-protein-with-forkhead-associated-domain-tifa-transduces-dna-damage-induced-activation-of-nf-%C3%AE%C2%BAb
#5
Jingxuan Fu, Daoyuan Huang, Fuwen Yuan, Nan Xie, Qian Li, Xinpei Sun, Xuehong Zhou, Guodong Li, Tanjun Tong, Yu Zhang
DNA damage-induced NF-kB activation and the secretion of inflammatory cytokines play crucial roles in carcinogenesis and cellular senescence. However, the underlying mechanisms, especially the initial sensors and transducers connecting the nuclear DNA damage signal with cytoplasmic NF-kB activation remain incompletely understood. Here, we report that TRAF-interacting protein with forkhead-associated domain (TIFA), an established NF-kB activator in the cytosol, unexpectedly exhibited nuclear translocation and accumulation on damaged chromatin following genotoxic stress...
March 26, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29577356/ser-486-491-phosphorylation-and-inhibition-of-ampk%C3%AE-activity-is-positively-associated-with-gleason-score-metastasis-and-castration-resistance-in-prostate-cancer-a-retrospective-clinical-study
#6
Melissa A Babcook, Mahmut Akgul, Seunghee Margevicius, Gregory T MacLennan, Pingfu Fu, Robert Abouassaly, Sanjay Gupta
BACKGROUND: We previously demonstrated that adenosine monophosphate-activated protein kinase (AMPKα) activity is significantly inhibited by Ser-486/491 phosphorylation in cell culture and in vivo models of metastatic and castration-resistant prostate cancer, and hypothesized these findings may translate to clinical specimens. METHODS: In this retrospective, single-institution pilot study, 45 metastatic prostate cancer cases were identified within the University Hospitals Cleveland Medical Center Pathology Archive with both metastasis and matched primary prostate tumor specimens in formalin-fixed, paraffin-embedded blocks, and complete electronic medical records...
March 26, 2018: Prostate
https://www.readbyqxmd.com/read/29559668/identification-of-new-inhibitors-against-human-great-wall-kinase-using-in-silico-approaches
#7
Ummi Ammarah, Amit Kumar, Rajesh Pal, Naresh C Bal, Gauri Misra
Microtubule associated serine/threonine kinase (MASTL) is an important Ser/Thr kinase belonging to the family of AGC kinases. It is the human orthologue of Greatwall kinase (Gwl) that plays a significant role in mitotic progression and cell cycle regulation. Upregulation of MASTL in various cancers and its association with poor patient survival establishes it as an important drug target in cancer therapy. Nevertheless, the target remains unexplored with the paucity of studies focused on identification of inhibitors against MASTL, which emphasizes the relevance of our present study...
March 20, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29547267/cytotoxic-effects-of-24-methylenecyloartanyl-ferulate-on-a549-non-small-cell-lung-cancer-cells-through-mybbp1a-up-regulation-and-akt-and-aurora-b-kinase-inhibition
#8
Sofia Doello, Zhibin Liang, Il Kyu Cho, Jung Bong Kim, Qing X Li
Lung cancer is the second most prevalent cancer. Non-small cell lung cancer (NSCLC) is the most common type of lung cancer. The low efficacy in current chemotherapies impels to find new alternatives to prevent or treat NSCLC. Rice bran oil is cytotoxic to A549 cells, a NSCLC cell line. Here, we identified 24-methylenecyloartanyl ferulate (24-mCAF) as the main component responsible for the cytotoxicity in A549 cells. An iTRAQ-based quantitative proteomics analysis revealed that 24-mCAF inhibits cell proliferation and activates cell death and apoptosis...
March 16, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29541394/selective-targeting-of-collagen-iv-in-the-cancer-cell-microenvironment-reduces-tumor-burden
#9
Fernando Revert, Francisco Revert-Ros, Raül Blasco, Aida Artigot, Ernesto López-Pascual, Roberto Gozalbo-Rovira, Ignacio Ventura, Elain Gutiérrez-Carbonell, Nuria Roda, Daniel Ruíz-Sanchis, Jerónimo Forteza, Javier Alcácer, Alejandra Pérez-Sastre, Ana Díaz, Enrique Pérez-Payá, Juan F Sanz-Cervera, Juan Saus
Goodpasture antigen-binding protein (GPBP) is an exportable1 Ser/Thr kinase that induces collagen IV expansion and has been associated with chemoresistance following epithelial-to-mesenchymal transition (EMT). Here we demonstrate that cancer EMT phenotypes secrete GPBP (mesenchymal GPBP) which displays a predominant multimeric oligomerization and directs the formation of previously unrecognized mesh collagen IV networks (mesenchymal collagen IV). Yeast two-hybrid (YTH) system was used to identify a260 SHCIE264 motif critical for multimeric GPBP assembly which then facilitated design of a series of potential peptidomimetics...
February 16, 2018: Oncotarget
https://www.readbyqxmd.com/read/29541386/atp-competitive-plk1-inhibitors-induce-caspase-3-mediated-plk1-cleavage-and-activation-in-hematopoietic-cell-lines
#10
Maeva Dufies, Damien Ambrosetti, Sonia Boulakirba, Anne Calleja, Coline Savy, Nathan Furstoss, Marwa Zerhouni, Julien Parola, Lazaro Aira-Diaz, Sandrine Marchetti, Francois Orange, Sandra Lacas-Gervais, Frederic Luciano, Arnaud Jacquel, Guillaume Robert, Gilles Pagès, Patrick Auberger
Polo-like kinases (Plks) define a highly conserved family of Ser/Thr kinases with crucial roles in the regulation of cell division. Here we show that Plk1 is cleaved by caspase 3, but not by other caspases in different hematopoietic cell lines treated with competitive inhibitors of the ATP-binding pocket of Plk1. Intriguingly, Plk1 was not cleaved in cells treated with Rigosertib, a non-competitive inhibitor of Plk1, suggesting that binding of the inhibitor to the ATP binding pocket of Plk1 triggers a conformational change and unmasks a cryptic caspase 3 cleavage site on the protein...
February 16, 2018: Oncotarget
https://www.readbyqxmd.com/read/29535359/eya3-partners-with-pp2a-to-induce-c-myc-stabilization-and-tumor-progression
#11
Lingdi Zhang, Hengbo Zhou, Xueni Li, Rebecca L Vartuli, Michael Rowse, Yongna Xing, Pratyaydipta Rudra, Debashis Ghosh, Rui Zhao, Heide L Ford
Eya genes encode a unique family of multifunctional proteins that serve as transcriptional co-activators and as haloacid dehalogenase-family Tyr phosphatases. Intriguingly, the N-terminal domain of Eyas, which does not share sequence similarity to any known phosphatases, contains a separable Ser/Thr phosphatase activity. Here, we demonstrate that the Ser/Thr phosphatase activity of Eya is not intrinsic, but arises from its direct interaction with the protein phosphatase 2A (PP2A)-B55α holoenzyme. Importantly, Eya3 alters the regulation of c-Myc by PP2A, increasing c-Myc stability by enabling PP2A-B55α to dephosphorylate pT58, in direct contrast to the previously described PP2A-B56α-mediated dephosphorylation of pS62 and c-Myc destabilization...
March 13, 2018: Nature Communications
https://www.readbyqxmd.com/read/29514980/pyruvate-kinase-m2-interacts-with-nuclear-sterol-regulatory-element-binding-protein-1a-and-thereby-activates-lipogenesis-and-cell-proliferation-in-hepatocellular-carcinoma
#12
Xiaoping Zhao, Li Zhao, Hao Yang, Jiajin Li, Xuejie Min, Fajun Yang, Jianjun Liu, Gang Huang
Dysregulation of lipid metabolism is common in cancer cells, but the underlying mechanisms are poorly understood. Sterol regulatory element-binding proteins (SREBPs) stimulate lipid biosynthesis through transcriptional activation of lipogenic enzymes. However, SREBPs' roles and potential interacting partners in cancer cells are not fully defined. Using a biochemical approach, we found here that pyruvate kinase M2 (PKM2) physically interacts with the nuclear form of SREBP-1a (nBP1a), by binding to amino acids 43-56 in nBP1a...
March 7, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29513138/protein-kinase-c-perfectly-balanced
#13
Alexandra C Newton
Protein kinase C (PKC) isozymes belong to a family of Ser/Thr kinases whose activity is governed by reversible release of an autoinhibitory pseudosubstrate. For conventional and novel isozymes, this is effected by binding the lipid second messenger, diacylglycerol, but for atypical PKC isozymes, this is effected by binding protein scaffolds. PKC shot into the limelight following the discovery in the 1980s that the diacylglycerol-sensitive isozymes are "receptors" for the potent tumor-promoting phorbol esters...
April 2018: Critical Reviews in Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/29476592/chemical-features-important-for-activity-in-a-class-of-inhibitors-targeting-the-wip1-flap-subdomain
#14
Harichandra D Tagad, Subrata Debnath, Victor Clausse, Mrinmoy Saha, Sharlyn Mazur, Ettore Appella, Daniel H Appella
The wild-type p53 induced phosphatase 1, Wip1 (PP2Cδ), is a PP2C family Ser/Thr phosphatase that negatively regulates the function of multiple proteins such as p53, ATM, Chk1, Chk2, Mdm2 and p38 MAPK involved in a DNA damage response. Wip1 dephosphorylates and inactivates its protein targets which are critical for cellular stress responses. Additionally, Wip1 frequently amplified and overexpressed in several human cancer types. Because of its negative role in regulating the function of essential proteins, Wip1 has been identified as a potential therapeutic target in various types of cancers...
February 23, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29459177/il-10-correlates-with-the-expression-of-carboxypeptidase-b2-and-lymphovascular-invasion-in-inflammatory-breast-cancer-the-potential-role-of-tumor-infiltrated-macrophages
#15
Hossam Taha Mohamed, Noura El-Husseiny, Eslam A El-Ghonaimy, Sherif Abdelaziz Ibrahim, Zainab A Bazzi, Dora Cavallo-Medved, Michael B Boffa, Mohamed El-Shinawi, Mona Mostafa Mohamed
Pro-carboxypeptidase B2 (pro-CPB2) or thrombin-activatable fibrinolysis inhibitor (TAFI) is a glycoprotein encoded by the CPB2 gene and deregulated in several cancer types, including breast cancer. Thrombin binding to thrombomodulin (TM), encoded by THBD, is important for TAFI activation. CPB2 gene expression is influenced by genetic polymorphism and cytokines such as interleukin 10 (IL-10). Our previous results showed that tumor infiltrating monocytes/macrophages (CD14+ /CD16+ ) isolated from inflammatory breast cancer (IBC) patients' secrete high levels of IL-10...
January 10, 2018: Current Problems in Cancer
https://www.readbyqxmd.com/read/29434871/mechanisms-for-dna-damaging-agent-induced-inactivation-of-erbb2-and-erbb3-via-the-erk-and-p38-signaling-pathways
#16
Chul Min Park, Yuki Kawasaki, Alaa Refaat, Hiroaki Sakurai
Cisplatin (CDDP) and doxorubicin (DOX) are chemotherapeutic drugs that trigger apoptosis by inducing DNA-damage. A previous study using breast cancer cells demonstrated the negative feedback modulation of the epidermal growth factor receptor (EGFR) and receptor tyrosine-protein kinase erbB-2 (ErbB2) via extracellular signal-regulated kinase (ERK)-mediated phosphorylation of conserved Thr-669 and Thr-677 residues, respectively, in the juxtamembrane domain. In addition, CDDP has been identified to cause negative feedback inhibition of activated EGFR in lung cancer cells...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29391601/the-oncogenic-tyrosine-kinase-lyn-impairs-the-pro-apoptotic-function-of-bim
#17
Lazaro E Aira, Elodie Villa, Pascal Colosetti, Parvati Gamas, Laurie Signetti, Sandrine Obba, Emma Proics, Fabien Gautier, Béatrice Bailly-Maitre, Arnaud Jacquel, Guillaume Robert, Frédéric Luciano, Philippe P Juin, Jean-Ehrland Ricci, Patrick Auberger, Sandrine Marchetti
Phosphorylation of Ser/Thr residues is a well-established modulating mechanism of the pro-apoptotic function of the BH3-only protein Bim. However, nothing is known about the putative tyrosine phosphorylation of this Bcl-2 family member and its potential impact on Bim function and subsequent Bax/Bak-mediated cytochrome c release and apoptosis. As we have previously shown that the tyrosine kinase Lyn could behave as an anti-apoptotic molecule, we investigated whether this Src family member could directly regulate the pro-apoptotic function of Bim...
February 2, 2018: Oncogene
https://www.readbyqxmd.com/read/29391154/o-glcnacylation-affects-%C3%AE-catenin-and-e-cadherin-expression-cell-motility-and-tumorigenicity-of-colorectal-cancer
#18
Shani Ben Harosh-Davidovich, Isam Khalaila
O-GlcNAcylation, the addition of β-N-acetylglucosamine (O-GlcNAc) moiety to Ser/Thr residues, is a sensor of the cell metabolic state. Cancer diseases such as colon, lung and breast cancer, possess deregulated O-GlcNAcylation. Studies during the last decade revealed that O-GlcNAcylation is implicated in cancer tumorigenesis and proliferation. The Wnt/β-catenin signaling pathway and cadherin-mediated adhesion are also implicated in epithelial-mesenchymal transition (EMT), a key cellular process in invasion and cancer metastasis...
January 30, 2018: Experimental Cell Research
https://www.readbyqxmd.com/read/29383184/stabilization-of-sur8-via-pkc%C3%AE-%C3%AE-degradation-promotes-transformation-and-migration-of-colorectal-cancer-cells
#19
Kug Hwa Lee, Woo-Jeong Jeong, Pu-Hyeon Cha, Sang-Kyu Lee, Do Sik Min, Kang-Yell Choi
Scaffold proteins of the mitogen activated protein kinase (MAPK) pathway recruit protein kinase cascades to confer context-specificity to cellular signaling. Varying concentrations of scaffold proteins determine different aspects of signaling outputs. However, regulatory mechanisms of scaffold proteins are poorly understood. Sur8, a scaffold protein in the Ras-MAPK pathway, is known to be involved in cell transformation and migration, and is increased in human colorectal cancer (CRC) patient tissue. Here we determine that regulation of Sur8 stability mediates transformation and migration of CRC cells...
December 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29375007/recognition-mechanism-of-wilms-tumour-suppressor-protein-and-dna-triplets-insights-from-molecular-dynamics-simulation-and-free-energy-analysis
#20
Ling-Fei Zhang, Qing-Chuan Zheng, Hong-Xing Zhang
The Wilms' tumour suppressor protein (WT1) plays a multifaceted role in human cancer processes. Mutations on its DNA recognition domain could lead to Denys-Drash syndrome (DDS), and alternate splicing results in insertion of the tripeptide Lys-Thr-Ser (KTS) between the third and fourth zinc fingers (ZFs), leading to changes in the DNA-binding function. However, detailed recognition mechanisms of the WT1-DNA complex have not been explored. To clarify the mutational effects upon WT1 towards DNA binding at the atomic level, molecular dynamics (MD) simulations and the molecular mechanics/Poisson Boltzmann surface area (MM/PBSA) method were employed...
January 29, 2018: Journal of Biomolecular Structure & Dynamics
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