scholarly journals Enzyme transformation to modulate the ligand–receptor interactions between small molecules

2015 ◽  
Vol 51 (23) ◽  
pp. 4899-4901 ◽  
Author(s):  
Junfeng Shi ◽  
Xuewen Du ◽  
Dan Yuan ◽  
Richard Haburcak ◽  
Dongdong Wu ◽  
...  

The use of enzymatic transformation to regulate ligand–receptor interactions between small molecules represents a new approach to mimic the essence of living systems.

2019 ◽  
Vol 9 (17) ◽  
pp. 3519
Author(s):  
Bartolomeu S. Souza ◽  
Henrique R. Marcelino ◽  
Francisco Alexandrino ◽  
Silvana C. C. Urtiga ◽  
Karen C. H. Silva ◽  
...  

The water-in-water emulsion method has been reported as a technique able to prepare microparticles without using harmful solvents. However, there are few reports showing the encapsulation of small molecules into microparticles produced within this technique. The probable reason relays on the rapid diffusion of these molecules from the discontinuous phase to the continuous phase. In the present study, xylan microparticles containing mesalamine were produced and the doubled crosslinking approach, used to promote higher encapsulation rates, was disclosed. To achieve this goal, a 23 full factorial design was carried out. The results revealed that all formulations presented spherical-shaped microparticles. However, at specific conditions, only few formulations reached up to 50% of drug loading. In addition, the new xylan-based microparticles formulation retained almost 40% of its drug content after 12 h of a dissolution assay likely due to the degree of crosslinking. Thus, the doubled crosslinking approach used was effective on the encapsulation of mesalamine and may pave the way to successfully produce other polysaccharide-based carriers for clinical use.


1967 ◽  
Vol 50 (11) ◽  
pp. 2565-2578 ◽  
Author(s):  
Andrew H. Soll

A cylindrical treatment of the configuration of small molecules in solution has been proposed. Cylindrical dimensions were obtained from Fisher-Hirschfelder molecular models, and these dimensions were used in an analysis of three sets of reflection coefficient values from the literature. The correlation between solute dimensions and the reflection coefficient was subjected to both statistical analyses and graphical examination, with particular emphasis given to parameter interdependence. The results consistently indicated a significant relation between the reflection coefficient and solute diameter. The dependence on diameter suggests a lengthwise orientation of solute within the membrane. Furthermore it is shown that this orientation is occurring within the aqueous region of the membrane, and thus this region has a structural characteristic which is responsible for the lengthwise orientation of solute.


2021 ◽  
Author(s):  
Galina Pavlova ◽  
Varvara Kolesnikova ◽  
Nadezhda Samoylenkova ◽  
Sergey Drozd ◽  
Alexander Revishchin ◽  
...  

Abstract Cancer cell reprogramming based on aptamers with antiproliferative properties in combination with small molecules that are used for conversion iPSCs into neurons represents a new approach to reduce the probability of glioblastoma recurrence and tumor resistance to therapy. In this research we tested several combinations of factors on whole cell cultures, derived from tumor tissue after surgical resection, and on cell cultures divided in CD133 enriched and depleted populations, as CD133 marker is believed to be characteristic for glioblastoma stem cells. We showed that CD133+ and CD133- cells have a different response to tested combinations of factors and CD133-positive cells are more stable and possess stemness properties. Thus, affecting these cells will lead to decrease of therapy resistance. Moreover, we found a combination of factors that is able to inhibit proliferation of both CD133+ and CD133- cells. Our results reveal a promising strategy to improve treatment of patients with glioblastoma.


2012 ◽  
Vol 74 (7) ◽  
pp. 521-524
Author(s):  
Andrew Brinker

Terrariums have decorated the shelves and counters of biology offices and classrooms for centuries. Living organisms inspire students and teachers alike. These wonderful ecosystems allow for both experimentation and observation of living systems. Here, I outline a new approach to building classroom terrariums. Historically, terrariums have been made using rocks, gravel, soil, wood, leaves, and organic props. This process often creates an immovable terrarium that weighs several hundred pounds. Although this approach will continue to produce beautiful terrariums, new technology has given us the opportunity to create more intricate terrariums that are a fraction of the weight and, therefore, mobile. The step-by-step protocol given here will allow biology professionals with little experience building terrariums an opportunity to explore this rewarding practice.


2012 ◽  
Vol 535-537 ◽  
pp. 1197-1200
Author(s):  
Xin Bo Ding ◽  
Tao Liu ◽  
Yan Hui Zhang ◽  
Jian Han

A theoretical study on damping properties of multi-layered hybrid materials was presented with the aim to obtain good damping materials with a broad and high damping range. The value of the multi-layered organic hybrid materials consisting of polarized polymers and small molecules was evaluated via the correspondence principle. Similarly, the damping properties of the multi-layered organic hybrid materials were predicted according to our previous work. With increasing the number of the layers of multi-layered hybrids, the temperature dependence of could be improved and it was almost rectangular transition range with values for the area under the linear curve. Therefore, it could be considered to be a new approach to improve the temperature dependence of the damping materials and obtain good damping materials with a broad and high damping range.


RSC Advances ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 3092-3104 ◽  
Author(s):  
Xi-wu Zhang ◽  
Qiu-han Li ◽  
Zuo-di Xu ◽  
Jin-jin Dou

Metabolomics is the study of the investigation of small molecules derived from cellular and organism metabolism, which reflects the outcomes of the complex network of biochemical reactions in living systems.


2019 ◽  
Vol 75 (6) ◽  
pp. 667-677 ◽  
Author(s):  
Meiry E. Alvarenga ◽  
Ana Karoline S. M. Valdo ◽  
Leandro Ribeiro ◽  
José Antonio Do Nascimento Neto ◽  
Debora P. De Araujo ◽  
...  

We report here for the first time a cocrystal of the so-called neutral calix[4]tube, which is two tail-to-tail-arranged and partially deprotonated tetrakis(carboxymethoxy)calix[4]arenes, including three sodium ions, with 2-(thiophen-2-yl)-1,3-benzothiazole, namely trisodium bis(carboxymethoxy)bis(carboxylatomethoxy)calix[4]arene tris(carboxymethoxy)(carboxylatomethoxy)calix[4]arene–2-(thiophen-2-yl)-1,3-benzothiazole–dimethyl sulfoxide–water (1/1/2/2), 3Na+·C36H30O12 2−·C36H31O12 −·C11H7NS2·2C2H6OS·2H2O, which provides a new approach into the host–guest chemistry of inclusion complexes. Three packing polymorphs of the same benzothiazole with high Z′ (one with Z′ = 8 and two with Z′ = 4) were also discovered in the course of our desired cocrystallization. The inspection of these polymorphs and a previously known polymorph with Z′ = 2 revealed that Z′ increases as the strength of intermolecular contacts decreases. Also, these results expand the frontier of invoking calixarenes as a host for nonsolvent small molecules, besides providing knowledge on the rare formation of high-Z′ packing polymorphs of simple molecules, such as the target benzothiazole.


2021 ◽  
Author(s):  
Galina Pavlova ◽  
Varvara Kolesnikova ◽  
Nadezhda Samoylenkova ◽  
Sergey Drozd ◽  
Alexander Revishchin ◽  
...  

Abstract Cancer cell reprogramming based on aptamers with antiproliferative properties in combination with small molecules that are used for conversion iPSCs into neurons represents a new approach to reduce the probability of glioblastoma recurrence and tumor resistance to therapy. In this research we tested several combinations of factors on whole cell cultures, derived from tumor tissue after surgical resection, and on cell cultures divided in CD133 enriched and depleted populations, as CD133 marker is believed to be characteristic for glioblastoma stem cells. We showed that CD133+ and CD133- cells have a different response to tested combinations of factors and CD133-positive cells are more stable and possess stemness properties. Thus, affecting these cells will lead to decrease of therapy resistance. Moreover, we found a combination of factors that is able to inhibit proliferation of both CD133+ and CD133- cells. Our results reveal a promising strategy to improve treatment of patients with glioblastoma.


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