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Table of Contents
JOURNAL SCAN
Year : 2019  |  Volume : 8  |  Issue : 2  |  Page : 120-121

Journal scan



Date of Web Publication11-Nov-2019

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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/JCSR.JCSR_55_19

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How to cite this article:
Suresh V, Bitla A R. Journal scan. J Clin Sci Res 2019;8:120-1

How to cite this URL:
Suresh V, Bitla A R. Journal scan. J Clin Sci Res [serial online] 2019 [cited 2019 Dec 16];8:120-1. Available from: http://www.jcsr.co.in/text.asp?2019/8/2/120/270753



Bicyclic RGD peptides with exquisite selectivity for the integrin αvβ3 receptor using a 'random design' approach

The authors describe a 'random design' approach for the identification of bicyclic RGD peptides with high affinity and selectivity for integrin αvβ3. This was achieved through a high-throughput screening of peptide libraries (672 different compounds) comprising the universal integrin-binding sequence Arg-Gly-Asp (RGD) in the first loop and a randomised sequence XXX (X being one of 18 canonical L-amino acids) in the second loop. Lead bicyclic inhibitors displaying sub-micromolar affinities for integrin αvβ3 (e.g., CT3HEQcT3RGDcT3, IC50= 195 nM) were identified following screening of the first-generation libraries. Further, through partial variation in the strongest lead inhibitors, the second- and the third-generation libraries were identified. The authors thus identified three highly selective bicyclic αvβ3 binders with affinities comparable to that of a knottin-RGD-type peptide with better selectivities over integrins αvβ5 and α5β1.


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Integrins, adhesion receptors are potential targets for cancer. In the study, the authors selected integrin αvβ3 from the integrin family to design peptide antagonists based on the random design approach. Generally, disulphide-rich peptides do not bind to the integrins; however, in this study, bicyclic RGD peptides exhibited better binding affinity and selectivity towards αvβ3. This approach may be applied to design more selective and high-affinity peptides to other extracellular matrix protein target involved in various cancers.

Bernhagen D, Jungbluth V, Quilis NG, Dostalek J, White PB, Jalink K, et al. Bicyclic RGD peptides with exquisite selectivity for the integrin αvβ3 receptor using a “Random design” approach. ACS Comb Sci 2019;21:198-206.

Synthesis and anti-HIV profile of a novel tetrahydroindazolylbenzamide derivative obtained by oxazolone chemistry

In this article, the authors report the synthesis, characterisation and evaluation of a new tetrahydroindazolylbenzamide derivative as HIV inhibitor. This agent was able to inhibit HIV proliferation with low cytotoxicity and significant selectivity.In vitro studies showed that the compound did not inhibit the viral integrase. Using quantitative polymerase chain reaction experiments, the authors demonstrated that the block in viral replication occurred in the early steps of replication. The authors also describe the synthesis of the scaffold, consisting of a sequential ring-opening reaction of oxazol-5-(4H)-one with 1,3-diketone using a multistep strategy which also included cyclocondensation with hydrazine and hydrolysis of the nitrile to the desired carboxamide.


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Hsp90, a molecular chaperone involved in protein folding, was identified as a therapeutic target in cancer. Smith et al., 2017 reported that inhibitors of Hsp90 act as potential therapeutics for HIV infection. In this study, the authors selected Hsp90 as a molecular target to design HIV inhibitors. Compound 6 was found to have selective anti-HIV activity with low cytotoxicity and found to be capable of inhibiting late reverse transcription.

Scala A, Piperno A, Micale N, Christ F, Debyser Z. Synthesis and anti-HIV profile of a novel tetrahydroindazolylbenzamide derivative obtained by oxazolone chemistry. ACS Med Chem Lett 2019;10:398-401.

A smartphone-based rapid telemonitoring system for Ebola and Marburg disease surveillance

The authors describe a digital and multiplexed platform for the rapid detection and telemonitoring of infections caused by Ebola and Marburg filoviruses. Using a flow cell assay cartridge for capturing specific antibodies and micro-arrayed recombinant antigens from all six species of filovirus, the authors developed a smartphone fluorescent reader for high-performance interpretation of test results which could be of great help in point-of-care testing of samples. The smartphone reader utilises the computational power of the built-in smartphone and software to guide operation. The method is convenient in terms of the faster processing time (20 min) using a few micro-litres of blood and faster processing and display of test results (15 s). Telemonitoring of test results generated by the smartphone readers can be done through a secure cloud service; this integrated system will be especially useful in resource-poor countries.


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Natesan et al., 2019 established a cost-effective smartphone-based system for the diagnosis of six species of viral Ebola and Marburg diseases with only a drop of blood from symptomatic and asymptomatic patients. The readout assay requires 1–2 μL of serum or plasma and 20 min of time. Disease profiling, data integration and surveillance are fast and reliable with the advent of biosensors, computing power, camera and communication capability of the smartphone. The devices may be extrapolated to resource-limited countries for diagnosis and surveillance of communicable and non-communicable diseases.

Natesan M, Wu SW, Chen CI, Jensen SMR, Karlovac N, Dyas BK, et al. A smartphone-based rapid telemonitoring system for Ebola and Marburg disease surveillance. ACS Sens 2019;4:61-8.

Financial support and sponsorship

Nil.

Conflicts of interest

There are no conflicts of interest.






 

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