Journal ArticleDOI
Natural product derived privileged scaffolds in drug discovery.
TLDR
Recent advances in the exploitation of terpenoid, polyketide, phenylpropanoid and alkaloid natural product scaffolds are reviewed for inspiration in the design and development of important new drug candidates.About:
This article is published in Current Opinion in Chemical Biology.The article was published on 2019-10-01. It has received 133 citations till now. The article focuses on the topics: Drug discovery.read more
Citations
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Herbal Medicine for Cardiovascular Diseases: Efficacy, Mechanisms, and Safety.
Abdullah Shaito,Duong Thi Bich Thuan,Hoa Thi Phu,Thi Hieu Dung Nguyen,Hiba Hasan,Sarah Halabi,Samar Abdelhady,Gheyath K. Nasrallah,Ali H. Eid,Ali H. Eid,Gianfranco Pintus,Gianfranco Pintus +11 more
TL;DR: The employment of these four plants in the context of CVDs, such as myocardial infarction, hypertension, peripheral vascular diseases, coronary heart disease, cardiomyopathies, and dyslipidemias has been reviewed, analyzed, and critically discussed.
Journal ArticleDOI
Directed Evolution of a Cytochrome P450 Carbene Transferase for Selective Functionalization of Cyclic Compounds.
TL;DR: A cytochrome P450 variant with 11 amino acid substitutions and a large deletion of the non-catalytic P450 reductase domain is evolved for highly efficient carbene transfer to indoles, pyrroles, and cyclic alkenes, showcasing the tunability of hemoproteins for highly selective functionalization of cyclic targets and the power of directed evolution to enhance the scope of new-to-nature enzyme catalysts.
Journal ArticleDOI
An overview of drug discovery and development.
TL;DR: The different means of drug discovery are discussed including their advantages and disadvantages, and is drug repurposing a viable alternative?
Journal ArticleDOI
Heterologous production of small molecules in the optimized Streptomyces hosts.
TL;DR: Recently developed genetic control elements (such as promoters, ribosome binding sites, terminators) and their application to achieve successful heterologous expression of biosynthetic gene clusters are discussed.
Journal ArticleDOI
Enzymatic Late-Stage Modifications: Better Late Than Never
Elvira Romero,Bethan S. Jones,Bethany N. Hogg,Arnau Rué Casamajo,Martin A. Hayes,Sabine L. Flitsch,Nicholas J. Turner,Christian Schnepel +7 more
TL;DR: An overview of the strengths and limitations of enzymatic late-stage modifications using native and engineered enzymes in synthesis while focusing on important examples in drug development is given in this paper.
References
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Journal ArticleDOI
Escape from flatland: increasing saturation as an approach to improving clinical success.
TL;DR: It is demonstrated that saturation correlates with solubility, an experimental physical property important to success in the drug discovery setting, and both complexity and the presence of chiral centers correlate with success as compounds transition from discovery, through clinical testing, to drugs.
Journal ArticleDOI
Privileged Scaffolds for Library Design and Drug Discovery
TL;DR: This review explores the concept of using privileged scaffolds to identify biologically active compounds through building chemical libraries by revealing through four selected examples the present state of the art in privileged scaffold library synthesis.
Journal ArticleDOI
Chalcone: A Privileged Structure in Medicinal Chemistry.
TL;DR: This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry and is expected to be a comprehensive, authoritative, and critical review of the chal cone template to the chemistry community.
Journal ArticleDOI
Statistical Investigation into the Structural Complementarity of Natural Products and Synthetic Compounds.
TL;DR: The statistical analysis of the structures of the natural and synthetically derived compounds has shown conspicuous variations in structural types in the natural products derived from different natural sources, which can be utilized in the search for individual active substances.
Journal ArticleDOI
Charting, navigating, and populating natural product chemical space for drug discovery.
TL;DR: It is anticipated that it may be a viable, if not necessary, step for research initiatives based on large high-throughput screening campaigns to make the most out of the recent advances in computational tools in order to leverage and take full advantage of the large data sets generated and available in house.
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