In silico Screening and Molecular Interaction Studies of Tetrahy-drocannabinol and its Derivatives with Acetylcholine Binding Pro-tein
Conclusion: In this study, we propose a novel THC derivative as a potential lead molecule in the drug development strategy for treating AD. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

A New Protocol of Type 2 Diabetes Induction and Hydrocortisone Effects on Beta-Cells Signaling in Mice
Background: There are complex methods to induce type 2 diabetes as multiple low-doses streptozotocin with high fat diet administration and other combined methods which induce modest DNA damage, leading to the incomplete destruction of β cells for insulin-resistant diabetes in mice. Objective: An innovative and simple protocol was investigated to induce type 2 diabetes by only Incre-mental Multiple Low-Doses Streptozotocin (IMLDS) in mice. The effects of hydrocortisone injection on diabetes induction and pancreatic β-cells signaling were also surveyed. Method: IMLDS designed protocol was conducted in 4 consecutive days by...
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

Oxidative Stress and Heavy Metal Levels of Pholiota limonella Mushroom Collected from Different Regions
Conclusion: Study findings demonstrated that the samples collected at Yalova province had higher heavy metal content and OSI value. As a result, the samples collected from Balıkesir (Kaz Mountain National Park) were concluded to be healthier. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

Conformational Changes Induced by P32T Substitution in Human Phosphatase ITPA
Enzyme ITPA participates in purine metabolism and its deficiency plays a role in several human diseases. There is growing evidence that ITPA polymorphism is also an important pharmacogen-ic phenotype, leading to a change in sensitivity to several drugs. ITPA deficiency exists in humans and is observed as elevated levels of ITP. Allele P32T-ITPA has more pronounced effects but the mecha-nism of enzyme inactivation is not known. Based on crystallographic data, Simone et al. assumed that the mutant loop containing P32T substitution led to uncovering of a hydrophobic residue (Phe31) that served as a marker for enzyme degradati...
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

125I-Insulin and 125I-Insulinlike Growth Factor-I in Chicken Hepatocytes Internalization. The Peptides Distribution and Action in Birds
Conclusions: 125I-insulin and 125I-IGF-I distribution is a specific characteristic of internalization, which is capable of changing, despite retaining basic internalization characteristics of both insulin and IGF-I in the cells of different animal species. The differences of 125I-insulin and 125I-IGF-I distribution types in chicken and rat cells, allow us to guess correctly other functional roles of insulin and IGF-I in birds as compared with mammals. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

Microbial Efflux Pump -Specific Determinant to Fight Against the Antimicrobial Resistance in Pathogenic Strains
Conclusion: The structure studies assist to design new drug compound which can efficiently inhibit the efflux pump and provide promising efflux pump inhibitor to cure multidrug resistance caused by the bacterial community. 3D structure of the efflux pump reveals the drug binding site and drug dislodge-ment site. The efflux pump inhibitor reduces the necessity of discovering novel drug molecules and provides a new way to reutilize existing drug with slight modifications. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

MIPs as a Versatile Tool for Micro-Solid-Phase Extraction and Probe Sensing
Conclusion: The current paper also reviews advances in MIPs synthesis onto quantum dots (MIP-QDs) for fluorescenssce sensing of organic compounds, advantages and drawbacks of each methodology, and future expected trends. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

Are There Differences in Catecholamine Levels in Body Fluids of Individuals with and Without Sleep Bruxism? A Systematic Review
Conclusion: There are some methodological flaws in the included studies, thus there is little scientific evidence that adults and children with sleep bruxism have higher catecholamine levels in the urine compared to those without bruxism. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

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(Source: Current Chemical Biology)
Source: Current Chemical Biology - July 17, 2018 Category: Biochemistry Source Type: research

The Regulation of Recombinant Protein S Secretion by Extracellular Factors
Conclusion: Supplementation of the expression medium with 5 mM calcium chloride improves the yield of recombinant PS. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research

Emerging Molecular Targets for Anti-Cancer Drug Design
Conclusion: Molecular mechanism and clinical efficacy of some of the emerging molecular targets for cancer chemotherapy have been briefly reviewed in the present article. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research

Structural Flexibility in HCV NS5B Polymerase and Molecular Modelling of Anti-HCV Drugs
Conclusion: It will help to develop allosteric inhibitors into efficient drugs by understanding their indirect mode of action and complex structure-activity/kinetic relationship. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research

Hsp90 Flexibility and Development of its Inhibitors for the Treatment of Cancer
Hsp90 is a molecular chaperone which is engaged in the repair of diverse oncogenic proteins. Additionally, it is overexpressed in cancer cells along with co-chaperones, whereas normal cell Hsp90 (less than 2 % of cellular proteins) resides in an uncomplexed state. Hence, this chaperone is an encouraging target for the discovery of novel chemical entities against cancer. Proteins execute their functions by interacting with various macromolecules. The conformational flexibility of polypeptides helps them to adopt a shape corresponding to their partner molecules. Hsp90 is a highly flexible polypeptide which can accommodate a ...
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research

Role of Structural Flexibility of HIV-1 Integrase in the Design of Potent Anti-HIV Drugs
Conclusion: Due to nonavailability of HIV-1 integrase in the crystalline form, we have to use the approach of analogue crystal, for example, PFV integrase. Although there are a drastic difference in the structural features in HIV-1 and PFV integrase. Researchers have to depend on PFV integrase for developing HIV-1 integrase inhibitors by trial and error process. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research

Flexibility of Important HIV-1 Targets and in silico Design of anti- HIV Drugs
Conclusion: We have emphasized the importance of incorporating receptor flexibility in molecular docking and QSAR studies. The benefits of allowing receptor flexibility during docking small molecules are vividly evident as the rate of picking false positives is significantly reduced. Similarly, the mechanism of binding and the type of interactions that dominate to exhibit tight binding can be explained by higher dimensional QSAR models, i.e., 4D-QSAR, which includes conformational flexibility. (Source: Current Chemical Biology)
Source: Current Chemical Biology - July 16, 2018 Category: Biochemistry Source Type: research