scholarly journals A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors

2020 ◽  
Vol 12 (36) ◽  
pp. 4418-4421
Author(s):  
Kohei Tsuji ◽  
David Hymel ◽  
Terrence R. Burke

Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 , we determined the IC50 of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay.

2013 ◽  
Vol 797 ◽  
pp. 89-94 ◽  
Author(s):  
Dongli Liao ◽  
Wenying Li ◽  
Jian Chen ◽  
Huping Jiao ◽  
Huipeng Zhou ◽  
...  

2014 ◽  
Vol 182 (3-4) ◽  
pp. 571-578 ◽  
Author(s):  
Zhisong Lu ◽  
Xuejuan Chen ◽  
Ying Wang ◽  
Xinting Zheng ◽  
Chang Ming Li

Author(s):  
Ameeruddin Nusrath Unissa ◽  
Luke Elizabeth Hanna

Protease (PR) is an important enzyme required for the posttranslational processing of the viral gene products of type-1 human immunodeficiency virus (HIV-1). Protease inhibitors (PI) act as competitive inhibitors that bind to the active site of PR. The I84V mutation contributes resistance to multiple PIs, and structurally, this mutation affects both sides of the enzyme active site. In order to get insights about this major resistance site to PR inhibitors using in silico approaches, in this chapter, the wild-type (WT) and mutant (MT) I84V of PR were modeled and docked with all PR inhibitors: Atazanavir, Darunavir, Indinavir, Lopinavir, Nelfinavir, Saquinavir, and Tipranavir. Docking results revealed that in comparison to the WT, the binding score was higher for the MT-I84V. Thus, it can be suggested that the high affinity towards inhibitors in the MT could be due to the presence of energetically favorable interactions, which may lead to tight binding of inhibitors with the MT protein, leading to the development of PR resistance against PIs in HIV-1 eventually.


2008 ◽  
Vol 80 (14) ◽  
pp. 5616-5621 ◽  
Author(s):  
Xiaoyang Xu ◽  
Zhen Zhao ◽  
Lidong Qin ◽  
Wei Wei ◽  
Jon E. Levine ◽  
...  

Author(s):  
Odell T. Minick ◽  
Hidejiro Yokoo

Mitochondrial alterations were studied in 25 liver biopsies from patients with alcoholic liver disease. Of special interest were the morphologic resemblance of certain fine structural variations in mitochondria and crystalloid inclusions. Four types of alterations within mitochondria were found that seemed to relate to cytoplasmic crystalloids.Type 1 alteration consisted of localized groups of cristae, usually oriented in the long direction of the organelle (Fig. 1A). In this plane they appeared serrated at the periphery with blind endings in the matrix. Other sections revealed a system of equally-spaced diagonal lines lengthwise in the mitochondrion with cristae protruding from both ends (Fig. 1B). Profiles of this inclusion were not unlike tangential cuts of a crystalloid structure frequently seen in enlarged mitochondria described below.


Author(s):  
G.J.C. Carpenter

In zirconium-hydrogen alloys, rapid cooling from an elevated temperature causes precipitation of the face-centred tetragonal (fct) phase, γZrH, in the form of needles, parallel to the close-packed <1120>zr directions (1). With low hydrogen concentrations, the hydride solvus is sufficiently low that zirconium atom diffusion cannot occur. For example, with 6 μg/g hydrogen, the solvus temperature is approximately 370 K (2), at which only the hydrogen diffuses readily. Shears are therefore necessary to produce the crystallographic transformation from hexagonal close-packed (hep) zirconium to fct hydride.The simplest mechanism for the transformation is the passage of Shockley partial dislocations having Burgers vectors (b) of the type 1/3<0110> on every second (0001)Zr plane. If the partial dislocations are in the form of loops with the same b, the crosssection of a hydride precipitate will be as shown in fig.1. A consequence of this type of transformation is that a cumulative shear, S, is produced that leads to a strain field in the surrounding zirconium matrix, as illustrated in fig.2a.


Author(s):  
J. C. Barry ◽  
H. Alexander

Dislocations in silicon produced by plastic deformation are generally dissociated into partials. 60° dislocations (Burgers vector type 1/2[101]) are dissociated into 30°(Burgers vector type 1/6[211]) and 90°(Burgers vector type 1/6[112]) dislocations. The 30° partials may be either of “glide” or “shuffle” type. Lattice images of the 30° dislocation have been obtained with a JEM 100B, and with a JEM 200Cx. In the aforementioned experiments a reasonable but imperfect match was obtained with calculated images for the “glide” model. In the present experiment direct structure images of 30° dislocation cores have been obtained with a JEOL 4000EX. It is possible to deduce the 30° dislocation core structure by direct inspection of the images. Dislocations were produced by compression of single crystal Si (sample preparation technique described in Alexander et al.).


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