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1.
Shubhandra Tripathi Akhil Kumar B. Sathish Kumar Arvind S. Negi 《Journal of biomolecular structure & dynamics》2016,34(6):1232-1240
Microtubule stabilizers provide an important mode of treatment via mitotic cell arrest of cancer cells. Recently, we reported two novel neolignans derivatives Cmp10 and Cmp19 showing anticancer activity and working as microtubule stabilizers at micromolar concentrations. In this study, we have explored the binding site, mode of binding, and stabilization by two novel microtubule stabilizers Cmp10 and Cmp19 using in silico molecular docking, molecular dynamics (MD) simulation, and binding free energy calculations. Molecular docking studies were performed to explore the β-tubulin binding site of Cmp10 and Cmp19. Further, MD simulations were used to probe the β-tubulin stabilization mechanism by Cmp10 and Cmp19. Binding affinity was also compared for Cmp10 and Cmp19 using binding free energy calculations. Our docking results revealed that both the compounds bind at Ptxl binding site in β-tubulin. MD simulation studies showed that Cmp10 and Cmp19 binding stabilizes M-loop (Phe272-Val288) residues of β-tubulin and prevent its dynamics, leading to a better packing between α and β subunits from adjacent tubulin dimers. In addition, His229, Ser280 and Gln281, and Arg278, Thr276, and Ser232 were found to be the key amino acid residues forming H-bonds with Cmp10 and Cmp19, respectively. Consequently, binding free energy calculations indicated that Cmp10 (?113.655 kJ/mol) had better binding compared to Cmp19 (?95.216 kJ/mol). This study provides useful insight for better understanding of the binding mechanism of Cmp10 and Cmp19 and will be helpful in designing novel microtubule stabilizers. 相似文献
2.
The Korean species of the genus Eudorylas Aczél have been studied. A total of 16 species are arranged herein. Among them, E. paraappendiculatus sp. nov. is new to science, and E. nomurai Morakote et Yano, 1990 is newly recorded in the Korean fauna. 相似文献
3.
H+/sugar symport in the obligatory aerobic yeastRhodotorula glutinis was analyzed under conditions where the plasma membrane was selectively depolarized by the lipophilic cation tetraphenylphosphonium (TPP+). Control experiments showed that this treatment did not impair the transmembrane pH, the cell energy charge, and the function of plasma membrane H+-ATPase. The kinetic data were fitted to elementary functions derived from a model constructed on the basis of some simplifying premises for ordered (either C + H+ + S or C + S + H+) and random reaction mechanisms. In addition, the comparison of the kinetic parameters in fully energized and depolarized cells provided information about the free carrier charge. It was concluded that the binding sequence of formation of the ternary carrier/H+/substrate complex follows a random mechanism and that the carrier bears a negative charge. 相似文献
4.
Summary The recent addition of restriction endonucleases in obtaining selective bands in the human genome has added a new dimension to molecular genetics. However, a considerable discrepancy exists in banding patterns produced by AluI in chromosomes 19 and 20, by MboI in chromosomes 4, 5, 8, 21 and 22 and by RsaI in chromosomes 12, 21 and 22. The principal causes of these differences are highlighted. 相似文献
5.
Arvind Kumar Bhatt Tek Chand Bhalla Hari Om Agrawal N. Sharma 《Letters in applied microbiology》1992,15(1):1-4
An extracellular chitosanase produced by Rhodotorula gracilis CFR-1 that catalyses a limited degradation of chitosan with no detectable generation of glucosamine or reducing groups was identified. Ultracentrifugation, polyacrylamide gel electrophoresis and gel permeation studies suggest that chitosan of average molecular mass 36000 Da was reduced by the enzymic catalysis to nearly one-fourth this size without further hydrolysis of the products. The enzyme, produced constitutively by this yeast, was partially purified and some of its properties were studied. 相似文献
6.
Milan Höfer Klaas Nicolay George Robillard 《Journal of bioenergetics and biomembranes》1985,17(3):175-182
The electrochemical gradient of protons,
, was estimated in the obligatory aerobic yeastRhodotorula glutinis in the pH0 range from 3 to 8.5. The membrane potential, , was measured by steady-state distribution of the hydrophobic ions, tetraphenylphosphonium (TPP+) for negative above pH0 4.5, and thiocyanate (SCN–) for positive below pH0 4.5. The chemical gradient of H+ was determined by measuring the chemical shift of intracellular Pi by31P-NMR at given pH0 values. The values of pHi increased almost linearly from 7.3 at pH0 3 to 7.8 at pH0 8.5. In the physiological pH0 range from 3.5 to 6,
was fairly constant at values between 17–18 KJ mol–1, gradually decreasing at pH0 above 6. In deenergized cells, the intracellular pHi decreased to values as low as 6, regardless of whether the cell suspension was buffered at pH0 4.5 or 7.5. There was no membrane potential detectable in deenergized cells. 相似文献
7.
8.
A simple procedure for obtaining useful narrow-pH-range ampholytes from inexpensive laboratory-synthesized ampholytes by preparative isoelectric focusing in Pevikon is described. The narrow range ampholytes prepared in this way are comparable to commercial ampholyte preparation as judged by conductivity, buffer capacity, pH gradient formation, and resolving power. These inexpensive narrow-range ampholytes are particularly well suited to preparative isoelectric focusing applications requiring large quantities of ampholytes. 相似文献
9.
Summary The gross primary production of periphyton, grown on artificial substrata in the littoral of the Danube, was measured by the light and dark bottle method from April 1970 to March 1971. The periphyton used for the measurements was sampled from various depths, in order to cover the production of the whole littoral. In connection with this, the littoral area was divided into four zones limited by the heights 600 to 200 cm, according to the local water level gauge. The highest localized zone A (500–600 cm) was inundated only at maximum water levels for rather short period of time, the deepest zone D (200–300 cm) was permanently flooded.The zone A showed an average periphyton primary production of 22.5, the zone B of 54.8, the zone C of 28.9 and the zone D of 9.1 mg O2/dm2/day. When recalculated to periods when the individual zones were inundated, the annual production was as follows: in zone A: 0.94, zone B: 9.20, zone C: 7.29 and zone D: 3.06g O2/dm2. The highest primary production was always found in the zone just below the water level. Exceptions occurred only when this zone was inundated for a short time as a result of a temporary rise of the water level and the periphyton was insufficiently developed.In order to compare the values of primary production of periphyton obtained from shallower rivers, where the whole bottom is well illuminated, or from rivers that do not exhibit such frequent and extensive level oscillations as the Danube, average value calculated from results obtained from the zone closest to the water level at the time of measurements, were always used. These results represent a special zone following the water level changes which is called surface zone. Primary periphytic production in the surface zone was 43.8 mg O2/dm2/day. For the annual period it corresponds to the value of 14.74 g O2/dm2. Efficiently of gross photosynthesis in this zone was on the average 1.72%.The height of the water level and the water temperature were higly correlated with gross periphytic production. Close relationships between chlorophyll a concent, biomass and gross primary production of periphyton were found.
Zusammenfassung Die Bruttoprimärproduktion des auf künstlichem Substrat im litoralen Bereich der Donau wachsenden Periphytons, wurde vom April 1970 bis zum März 1971, mit Hilfe der Hell-Dunkelflaschenmethode, gemessen. Das für die Messung herangezogene Periphyton wurde aus verschiedenen Tiefenzonen entnommen, um die Produktion der gesamten Uferzone festzuhalten. Im Zusammenhang damit wurde der litorale Bereich der Donau in 4 Zonen gegliedert, welche ihre Grenzen bei einem Pegelstand von 600–200 cm des Ortspegels hatten. Die höchste Zone A (500–600 cm) wurde nur bei den höchsten Wasserstanden und nur für kurze Zeit vom Wasser überflutet, die tiefste Zone D (200–300 cm) war dauernd unter Wasser.In der Zone A war die durchschnittliche Produktion des Periphytons 22,5 mg O2/dm2/Tag, in Zone B 54,8 mg, in Zone C 28,9 mg und in Zone D 9.1 mg. Nach Berechnung für die Zeit, in der die einzelnen Zonen vom Wasser bedeckt waren war folgende Produktion in den einzelnen Zonen festzustellen: in Zone A 0,94 g O2/dm2, in Zone B 9,20 g, in Zone C 7,29 g und in Zone D 3,06 g. Die höchste Periphytonproduktion wurde jeweils in der Zone festgestellt, welche dem Wasserspiegel am nächsten war. Eine Ausnahme bildeten nur jene Fälle, in denen these Zone nach vorübergehender Erhöhung des Wasserspiegels erst kurze Zeit vom Wasser bedeckt war und das Periphyton ungenügend entwickelt war.Zum Vergleich mit den Werten der Primärproduktion des Aufwuchses aus seichteren Gewässern mit gut belichteter Sohle, oder aus Flüssen welche nicht so häufige und weitreichende Spiegelschwankungen aufweisen wie die Donau, wird in der vorgelegten Arbeit der Durchschnittswert aus den Ergebnissen der Zone verwendet, welche zur Zeit der Messungen dem Wasserspiegel am nächsten war. Diese Ergebnisse repräsentieren eine besondere Zone, welche den Schwankungen des Wasserspiegels folgt und von den Autoren durch den Begriff Oberflachenzone bezeichnet wird. Die Primärproduktion des Periphytons in dieser Oberflächenzone war 43,8 mg O2/dm2/Tag. Dem entspricht im Jahresverlauf ein Wert von 14,74 g O2/dm2. Die Ausnützung der Sonnenenergie war in dieser Zone im Durchschnitt 1,72%.Von den Umweltfaktoren zeigt die Höhe des Wasserspiegels und die Wassertemperatur den engsten Zusammenhang mit der Höhe der Bruttoprimärproduktion des Periphytons. In kürzeren Zeitabschnitten, in denen es zu keinen raschen ausgeprägten Schwankungen des Wasserspiegels des Flusses kommt, wurde eine enge Abhängigkeit zwischen den Werten der Primärproduktion und dem a-Chlorophylgehalt und auch der Biomasse festgestellt.相似文献
10.
Milan Fiala 《Applied microbiology》1968,16(10):1445-1450
Plaque production by 55 rhinoviruses in several lines of HeLa cells is reported. Forty-nine types produced macroscopic plaques under the conditions described previously employing 30 mM MgCl(2) and 30 mug/ml of DEAE-dextran in overlay and M HeLa cells. Basically three kinds of plaques were observed: clear large and intermediate sized plaques and small turbid plaques. Five rhinoviruses produced plaques only in a sensitive clonal line isolated from the M HeLa line. Rhinovirus type 4 produced plaques after the pretreatment of cells with actinomycin D. Enhancement of plaque formation by MgCl(2) has been demonstrated to date with 17 rhinoviruses. Some rhinoviruses were enhanced either by DEAE-dextran or by dextran sulfate in the overlay. No inhibitors were found in any of 10 bovine sera tested. Rhinovirus type 2 was visualized inside HeLa cells by electron microscopy and there appeared to be a very high ratio of physical particles per infectious unit of virus. 相似文献