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Role of Structural Flexibility of HIV-1 Integrase in the Design of Potent Anti-HIV Drugs

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Background: The novel drug discovery of HIV- 1 integrase inhibitors is based on exploring protein flexibility and QSAR studies using the protein structure. In this pursuit, several novel inhibitors are under development. For example, Allosteric inhibitors (ALLINIs) and Multimerization integrase inhibitors (MINIs).

Objective: The objective is to discuss the development process of drug discovery and review the latest developments in HIV-1 integrase inhibitors.

Method: A search of scientific literature and data on recent developments of HIV-1 integrase with an intension of safe and effective drugs which inhibits the HIV-1 integrase. The information was organized with an objective of giving Compressive developments leading to the discovery of integrase inhibitors based on protein flexibility, simulation studies and QSAR.

Results: Identification of structural details and understanding the binding sites as lead to develop new chemical entities which are promising integrase inhibitors. The role of protein flexibility in developing novel inhibitors like ALLINIs and MINIs. For example Cabotegravir, Elvitegravir, Raltegravir and Dolutegravir.

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.
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Keywords: ALLINIs; HIV-1 integrase; MINIs; PFV integrase; cabotegravir; dolutegravir; protein flexibility

Document Type: Review Article

Publication date: April 1, 2018

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  • Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology interface, covering topics relating to Chemical Synthesis, Science at Chemistry-Biology Interface and Chemical Mechanisms of Biological Systems.

    Current Chemical Biology covers the following areas: Chemical Synthesis (Syntheses of biologically important macromolecules including proteins, polypeptides, oligonucleotides, oligosaccharides etc.; Asymmetric synthesis; Combinatorial synthesis; Diversity-oriented synthesis; Template-directed synthesis; Biomimetic synthesis; Solid phase biomolecular synthesis; Synthesis of small biomolecules: amino acids, peptides, lipids, carbohydrates and nucleosides; and Natural product synthesis).

    Science at Chemistry-Biology Interface (Chemical informatics; Macromolecular catalysts and receptors; Enzymatic synthesis; Biosynthetic engineering; Combinatorial biosynthesis; Plant cell based chemistry; Bacterial and viral cell based chemistry; Chemistry of cellular processes in plants/animals; Receptor chemistry; Cell signaling chemistry; Drug design through understanding of disease processes; Synthetic biology; New high throughput screening techniques; Small molecular array fabrication; Chemical genomics; Chemical and biological approaches to carbohydrates proteins and nucleic acids design; Chemical and biological regulation of biosynthetic pathways; and Unnatural biomolecular analogs).
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