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  • ISSN: 2379-089X
    Volume 2, Issue 3
    Review Article
    Zhisong Wang, Nalajam Guravaiah, Chengqing Ning, Yujun He, Lei Yao, Jianming Wang and Niefang Yu
    Abstract: Antibody-drug conjugates (ADCs) are novel targeted chemotherapeutic agents that utilize the specificity of monoclonal antibodies (mAbs) to deliver potent cell-killing agents to cancer cells that express the target antigen, thereby taking advantage of the best characteristics of both components. The experience and/or lessons learned from the first generation of conjugates have guided the development of more effective antitumor agents. Along with the development of the mAbs and cytotoxins, the design of chemical linkers to covalently bind these building blocks is making rapid progress but remains challenging. Encouragingly, the recent successes in these domains show that the next generation of antibody-drug conjugates has come of age.
    Research Article
    Joel José Montalvo-Acosta* and Ricardo Gaitán Ibarra
    Abstract: A series of neocryptolepine derivatives with antimalarial activity were subjected to two-dimensional quantitative structure-activity relationship (2D-QSAR) studies using stepwise multiple linear regressions for variables selection. The results of the study indicate that antimalarial activity of neocryptolepine analogues can be successfully explained in terms of physical (molecular weight and density) and surface properties of the molecules (vsa_don, TPSA and PEOE_VSA-6). The accuracy of the proposed multiple linear regression models was demonstrated using the following evaluation techniques: cross-validation, validation through an external test set and Y-randomization. Furthermore, the domain of applicability which indicates the area of reliable predictions is defined for each model. The results from the 2D-QSAR analysis developed in this study could be used in the design of more potent antimalarial neocryptolepine derivatives.
    Mahmoud M. Sebaiy*, Abdullah A. El-Shanawany, Mohamed M. Baraka, Lobna M. Abdel Aziz and Christa L. Colyer
    A fluorimetric comparison study has been established for the labeling of human serum albumin (HSA) using two new boronic acid functionalized squarylium dyes, one is monofunctional boronic acid dye (SQ-BA4) while the other one is bifunctional boronic acid dye (SQ-DBA2). The spectral properties of these two novel squarylium dyes have been studied under a variety of solutions to explore the optimal conditions for non-covalent protein labeling. Both dyes exhibited very low fluorescence intensity in aqueous solutions presumably due to H-aggregate formation in absence of the protein but showed a significant enhancement in the fluorescence intensity with the addition of HSA in the optimal acidic citrate buffer. Stability constant studies were conducted and SQ-BA4 dye was shown to have much stronger binding affinity with HSA than SQ-DBA2. Also, the stoichiometries of non-covalent complexes were found to be (1:1) for SQ-BA4 and different (1:2) for SQ-DBA2 with HSA. These studies are claimed to be the optimal for CE-LIF work which will be progressed in our continuing project.
    Editorial Perspective
    Jennifer Auer and Khondaker Miraz Rahman*
    Antimicrobial resistance is a growing problem across the world, becoming a major threat to global public health. According to the Centre for Disease Control and prevention (CDC), in the USA alone over 2 million patients are infected with drug resistant bacterial infections and 23,000 of these patients die annually of these infections 1. This not only impacts health care systems but also has a negative impact on the economy as treatments become more expensive due to extended and more complex treatment regimes.
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