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https://www.readbyqxmd.com/read/28214932/theoretical-and-experimental-study-of-polycyclic-aromatic-compounds-as-%C3%AE-tubulin-inhibitors
#1
Fabian E Olazarán, Carlos A García-Pérez, Debasish Bandyopadhyay, Isaias Balderas-Rentería, Angel D Reyes-Figueroa, Lars Henschke, Gildardo Rivera
In this work, through a docking analysis of compounds from the ZINC chemical library on human β-tubulin using high performance computer cluster, we report new polycyclic aromatic compounds that bind with high energy on the colchicine binding site of β-tubulin, suggesting three new key amino acids. However, molecular dynamic analysis showed low stability in the interaction between ligand and receptor. Results were confirmed experimentally in in vitro and in vivo models that suggest that molecular dynamics simulation is the best option to find new potential β-tubulin inhibitors...
March 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28214686/enhanced-anticancer-effect-of-combretastatin-a-4-phosphate-when-combined-with-vincristine-in-the-treatment-of-hepatocellular-carcinoma
#2
Esam M Aboubakr, Ashraf Taye, Omar M Aly, A M Gamal-Eldeen, Mohamed A El-Moselhy
Tubulin targeting agents have received considerable interest as a potential tumor-selective vascular disrupting agents, which represent another avenue for cancer growing therapeutic opportunities. Hence, the present study was conducted to investigate the anti-tumor activity of Combretastatin A-4 phosphate (CA4-P) and vincristine against hepatocellular carcinoma in rats, by individual administration and in combination. In vitro study was conducted using human hepatocellular carcinoma cell lines, showed that CA4-P and vincristine have a potent cell cytotoxic and tubulin inhibitory effect...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28214655/identification-of-microrna-biomarkers-for-response-of-advanced-soft-tissue-sarcomas-to-eribulin-translational-results-of-the-eortc-62052-trial
#3
Erik A C Wiemer, Agnieszka Wozniak, Herman Burger, Marcel Smid, Giuseppe Floris, Axelle Nzokirantevye, Raf Sciot, Stefan Sleijfer, Patrick Schöffski
BACKGROUND: Recent phase II and III clinical trials demonstrated anti-tumour activity of eribulin, a tubulin-interacting cytotoxic agent, in patients with metastatic soft tissue sarcoma (STS). In this exploratory study, we aimed to identify putative microRNA biomarkers that associate with eribulin sensitivity or resistance in STS. MATERIALS AND METHODS: Archival tumour tissue from primary tumours or metastatic lesions was collected prior to eribulin treatment, from 65 consenting patients involved in the EORTC trial 62052...
February 16, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28213947/select-noxious-stimuli-induce-changes-on-corneal-nerve-morphology
#4
Deborah M Hegarty, Sam M Hermes, Katherine Yang, Sue A Aicher
The surface of the cornea contains the highest density of nociceptive nerves of any tissue in the body. These nerves are responsive to a variety of modalities of noxious stimuli and can signal pain even when activated by low threshold stimulation. Injury of corneal nerves can lead to altered nerve morphology, including neuropathic changes which can be associated with chronic pain. Emerging technologies that allow imaging of corneal nerves in vivo are spawning questions regarding the relationship between corneal nerve density, morphology and function...
February 18, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28212984/hiv-1-vpr-disrupts-mitochondria-axonal-transport-and-accelerates-neuronal-aging
#5
Ying Wang, Maryline Santerre, Italo Tempera, Kayla Martin, Ruma Mukerjee, Bassel E Sawaya
Disruption of mitochondria axonal transport, essential for the maintenance of synaptic and neuronal integrity and function, has been identified in neurodegenerative diseases. Whether HIV-1 viral proteins affect mitochondria axonal transport is unknown, albeit HIV-associated neurocognitive disorders occur in around half of the patients living with HIV. Therefore, we sought to examine the effect of HIV-1 viral protein R (Vpr) on mitochondria axonal transport. Using mice primary neuronal cultures, we demonstrated that 4-day Vpr treatment reduced the ratio of moving mitochondria associated with (i) less energy (ATP) supply, (ii) reduction in Miro-1 and (iii) increase of α-synuclein which led to loss of microtubule stability as demonstrated by inconsecutive distribution of acetylated α-tubulin along the axons...
February 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28211616/design-synthesis-and-biological-evaluation-of-chalcone-containing-shikonin-derivatives-as-inhibitors-of-tubulin-polymerization
#6
Han-Yue Qiu, Fang Wang, Xue Wang, Wen-Xue Sun, Jin-Liang Qi, Yan-Jun Pang, Rong-Wu Yang, Gui-Hua Lu, Xiao-Ming Wang, Yong-Hua Yang
The biological importance of microtubules in mitosis makes them an interesting target for the development of anticancer agents. In this study, a series of novel chalcone-containing shikonin derivatives was designed, synthesized, and evaluated for biological activities. Among them, derivative PMMB-259 [(R)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-en-1-yl (E)-2-(4-(3-oxo-3-(3-(trifluoromethoxy)phenyl)prop-1-en-1-yl)phenoxy)acetate] was identified as a potent inhibitor of tubulin polymerization...
February 17, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28210976/regenerative-medicine-for-parkinson-s-disease-using-differentiated-nerve-cells-derived-from-human-buccal-fat-pad-stem-cells
#7
Haruka Takahashi, Hiroshi Ishikawa, Akira Tanaka
The purpose of this study was to evaluate the utility of human adipose stem cells derived from the buccal fat pad (hBFP-ASCs) for nerve regeneration. Parkinson's disease (PD) is a neurodegenerative disorder characterized by progressive death of dopaminergic neurons. PD is a candidate disease for cell replacement therapy because it has no fundamental therapeutic methods. We examined the properties of neural-related cells induced from hBFP-ASCs as a cell source for PD treatment. hBFP-ASCs were cultured in neurogenic differentiation medium for about 2 weeks...
February 16, 2017: Human Cell
https://www.readbyqxmd.com/read/28209915/exclusive-destruction-of-mitotic-spindles-in-human-cancer-cells
#8
Leonid Visochek, Asher Castiel, Leonid Mittelman, Michael Elkin, Dikla Atias, Talia Golan, Shai Izraeli, Tamar Peretz, Malka Cohen-Armon
We identified target proteins modified by phenanthrenes that cause exclusive eradication of human cancer cells. The cytotoxic activity of the phenanthrenes in a variety of human cancer cells is attributed by these findings to post translational modifications of NuMA and kinesins HSET/kifC1 and kif18A. Their activity prevented the binding of NuMA to α-tubulin and kinesins in human cancer cells, and caused aberrant spindles. The most efficient cytotoxic activity of the phenanthridine PJ34, caused significantly smaller aberrant spindles with disrupted spindle poles and scattered extra-centrosomes and chromosomes...
February 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28209899/gtpase-activity-coupled-treadmilling-of-the-bacterial-tubulin-ftsz-organizes-septal-cell-wall-synthesis
#9
Xinxing Yang, Zhixin Lyu, Amanda Miguel, Ryan McQuillen, Kerwyn Casey Huang, Jie Xiao
The bacterial tubulin FtsZ is the central component of the cell division machinery, coordinating an ensemble of proteins involved in septal cell wall synthesis to ensure successful constriction. How cells achieve this coordination is unknown. We found that in Escherichia coli cells, FtsZ exhibits dynamic treadmilling predominantly determined by its guanosine triphosphatase activity. The treadmilling dynamics direct the processive movement of the septal cell wall synthesis machinery but do not limit the rate of septal synthesis...
February 17, 2017: Science
https://www.readbyqxmd.com/read/28209780/microtubule-associated-protein-4-map4-controls-nanovesicle-dynamics-and-t-cell-activation
#10
Eugenio Bustos-Morán, Noelia Blas-Rus, Noa Martin-Cófreces, Francisco Sánchez-Madrid
The Immune Synapse (IS) is a specialized structure formed at the contact area between T lymphocytes and antigen-presenting cells (APC), essential for the adaptive immune response. Proper T cell activation requires its polarization towards the APC, which is highly dependent on the tubulin cytoskeleton. Microtubule associated protein-4 (MAP4) is a microtubule (MT)-stabilizing protein that controls MTs in physiological processes such as cell division, migration, vesicular transport or primary cilia formation. In this study, we have assessed the role of MAP4 in T cell activation...
February 16, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28209268/inorganic-mercury-prevents-the-differentiation-of-sh-sy5y-cells-amyloid-precursor-protein-microtubule-associated-proteins-and-ros-as-potential-targets
#11
Miguel Chin Chan, Elizabeth Bautista, Isabel Alvarado-Cruz, Betzabet Quintanilla-Vega, José Segovia
Exposure to mercury (Hg) occurs through different pathways and forms including methylmecury (MeHg) from seafood and rice, ethylmercury (EtHg), and elemental Hg (Hg(0)) from dental amalgams and artisanal gold mining. Once in the brain all these forms are transformed to inorganic Hg (I-Hg), where it bioaccumulates and remains for long periods. Hg is a well-known neurotoxicant, with its most damaging effects reported during brain development, when cellular key events, such as cell differentiation take place. A considerable number of studies report an impairment of neuronal differentiation due to MeHg exposure, however the effects of I-Hg, an important form of Hg found in brain, have received less attention...
February 6, 2017: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/28208696/valproate-attenuates-endoplasmic-reticulum-stress-induced-apoptosis-in-sh-sy5y-cells-via-the-akt-gsk3%C3%AE-signaling-pathway
#12
Zhengmao Li, Fenzan Wu, Xie Zhang, Yi Chai, Daqing Chen, Yuetao Yang, Kebin Xu, Jiayu Yin, Rui Li, Hongxue Shi, Zhouguang Wang, Xiaokun Li, Jian Xiao, Hongyu Zhang
Endoplasmic reticulum (ER) stress-induced apoptosis plays an important role in a range of neurological disorders, such as neurodegenerative diseases, spinal cord injury, and diabetic neuropathy. Valproate (VPA), a typical antiepileptic drug, is commonly used in the treatment of bipolar disorder and epilepsy. Recently, VPA has been reported to exert neurotrophic effects and promote neurite outgrowth, but its molecular mechanism is still unclear. In the present study, we investigated whether VPA inhibited ER stress and promoted neuroprotection and neuronal restoration in SH-SY5Y cells and in primary rat cortical neurons, respectively, upon exposure to thapsigargin (TG)...
February 8, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28207984/structural-basis-of-microtubule-stabilization-by-discodermolide
#13
Andrea E Prota, Katja Bargsten, Mariano Redondo, Amos B Smith Iii, Chia-Ping H Yang, Hayley M McDaid, Ian Paterson, Susan B Horwitz, José Fernando Díaz, Michel O Steinmetz
Microtubule-stabilizing agents (MSAs) are widely used in chemotherapy. Here, using X-ray crystallography we describe the detailed binding modes of two potent MSAs, (+)-discodermolide (DDM) and the DDM-paclitaxel-hybrid KS-1-199-32, in the taxane pocket of ß-tubulin. Both compounds bind in a very similar hairpin conformation as previously observed in solution. However, they differentially stabilize the M-loop of ß-tubulin: KS-1-199-32 induces an M-loop helical conformation that is not observed for DDM. In the context of the microtubule structure, both MSAs connect the ß-tubulin helices H6 and H7 and loop S9-S10 with the M-loop, which is similar to the structural effects elicited by epothilone A, but distinct from paclitaxel...
February 16, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28204846/regulation-of-end-binding-protein-eb1-in-the-control-of-microtubule-dynamics
#14
REVIEW
Anne Nehlig, Angie Molina, Sylvie Rodrigues-Ferreira, Stéphane Honoré, Clara Nahmias
The regulation of microtubule dynamics is critical to ensure essential cell functions, such as proper segregation of chromosomes during mitosis or cell polarity and migration. End-binding protein 1 (EB1) is a plus-end-tracking protein (+TIP) that accumulates at growing microtubule ends and plays a pivotal role in the regulation of microtubule dynamics. EB1 autonomously binds an extended tubulin-GTP/GDP-Pi structure at growing microtubule ends and acts as a molecular scaffold that recruits a large number of regulatory +TIPs through interaction with CAP-Gly or SxIP motifs...
February 15, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28199900/diagnosis-of-resistance-alleles-in-codon-167-of-the-beta-tubulin-cya-tbb-1-gene-from-third-stage-larvae-of-horse-cyathostomins
#15
Juliana Bana Ishii, Amilcar Arenal, Aline Felix, Ursula Yoshitani, Robin Beech, Marcelo Beltrão Molento
Anthelmintic resistance is a serious problem for the control of equine gastrointestinal nematodes. In the present survey, 173 third stage larvae of cyathostomins were investigated from three different locations for the presence of the resistant genotype at codon 167 of the beta-tubulin gene, as this is the most prevalent mutation. The larvae from the state of Parana (n=67), Sao Paulo (n=54) and Santa Catarina (n=52), showed 61.2; 31.5 and 38.5% of the heterozygous resistant genotype - TTC/TAC, respectively...
January 25, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28198434/jerantinine-a-induces-tumor-specific-cell-death-through-modulation-of-splicing-factor-3b-subunit-1-sf3b1
#16
Felicia Fei-Lei Chung, Perry Faith Tze Ming Tan, Vijay Joseph Raja, Boon-Shing Tan, Kuan-Hon Lim, Toh-Seok Kam, Ling-Wei Hii, Si Hoey Tan, Sze-Jia See, Yuen-Fen Tan, Li-Zhe Wong, Wai Keat Yam, Chun Wai Mai, Tracey D Bradshaw, Chee-Onn Leong
Precursor mRNA (pre-mRNA) splicing is catalyzed by a large ribonucleoprotein complex known as the spliceosome. Numerous studies have indicated that aberrant splicing patterns or mutations in spliceosome components, including the splicing factor 3b subunit 1 (SF3B1), are associated with hallmark cancer phenotypes. This has led to the identification and development of small molecules with spliceosome-modulating activity as potential anticancer agents. Jerantinine A (JA) is a novel indole alkaloid which displays potent anti-proliferative activities against human cancer cell lines by inhibiting tubulin polymerization and inducing G2/M cell cycle arrest...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28195215/the-structural-switch-of-nucleotide-free-kinesin
#17
Luyan Cao, Soraya Cantos-Fernandes, Benoît Gigant
Kinesin-1 is an ATP-dependent motor protein that moves towards microtubules (+)-ends. Whereas structures of isolated ADP-kinesin and of complexes with tubulin of apo-kinesin and of ATP-like-kinesin are available, structural data on apo-kinesin-1 in the absence of tubulin are still missing, leaving the role of nucleotide release in the structural cycle unsettled. Here, we identified mutations in the kinesin nucleotide-binding P-loop motif that interfere with ADP binding. These mutations destabilize the P-loop (T87A mutant) or magnesium binding (T92V), highlighting a dual mechanism for nucleotide release...
February 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28194270/total-synthesis-of-a-key-series-of-vinblastines-modified-at-c4-that-define-the-importance-and-surprising-trends-in-activity
#18
Shouliang Yang, Kuppusamy Sankar, Colin K Skepper, Timothy J Barker, John C Lukesh, Daniel M Brody, Manuela M Brütsch, Dale L Boger
The total synthesis and evaluation of a key systematic series of vinblastines that incorporate the first deep-seated changes to the substituent at C4 are detailed. The synthetic approach features an expanded and redefined scope of a 1,3,4-oxadiazole [4 + 2]/[3 + 2] cycloaddition cascade in which electronically mismatched electron-deficient trisubstituted alkenes and unactivated trisubstituted alkenes were found to productively initiate the cycloaddition cascade with tethered electron-deficient 1,3,4-oxadiazoles...
February 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28193841/dual-roles-of-akirin2-during-xenopus-neural-development
#19
Xiaoliang Liu, Yingjie Xia, Jixin Tang, Li Ma, Chaocui Li, Pengcheng Ma, Bingyu Mao
To ensure correct spatial and temporal patterning, embryos must maintain pluripotent cell populations and control when cells undergo commitment. The newly identified nucleoprotein Akirin has been shown to modulate the innate immune response through epigenetic regulation and to play important roles in other physiological processes, but its role in neural development remains unknown. Here, we show that Akirin2 is required for neural development in Xenopus and knockdown of Akirin2 expands the expression of the neural progenitor marker Sox2 and inhibits expression of the differentiated neuronal marker N-tubulin...
February 13, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28193732/error-prone-meiotic-division-and-subfertility-in-mice-with-oocyte-conditional-knockdown-of-pericentrin
#20
Claudia Baumann, Xiaotian Wang, Luhan Yang, Maria M Viveiros
Mouse oocytes lack canonical centrosomes and instead contain unique acentriolar microtubule-organizing centers (aMTOCs). To test the function of these distinct aMTOCs in meiotic spindle formation -Pericentrin (Pcnt), an essential centrosome/MTOC protein, was knocked down exclusively in oocytes using transgenic RNAi. Here we provide evidence that disruption of aMTOC function in oocytes promotes spindle instability and severe meiotic errors that lead to pronounced female subfertility. Pcnt-depleted oocytes from transgenic (Tg) mice are ovulated at metaphase-II, but show significant chromosome misalignment, aneuploidy and premature sister chromatid separation...
February 13, 2017: Journal of Cell Science
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