Faculty Opinions recommendation of Natural products: a continuing source of novel drug leads.

Author(s):  
Jean-Jacques Sanglier
Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2542
Author(s):  
Linda Sukmarini

Natural products (NPs) are evolutionarily optimized as drug-like molecules and remain the most consistently successful source of drugs and drug leads. They offer major opportunities for finding novel lead structures that are active against a broad spectrum of assay targets, particularly those from secondary metabolites of microbial origin. Due to traditional discovery approaches’ limitations relying on untargeted screening methods, there is a growing trend to employ unconventional secondary metabolomics techniques. Aided by the more in-depth understanding of different biosynthetic pathways and the technological advancement in analytical instrumentation, the development of new methodologies provides an alternative that can accelerate discoveries of new lead-structures of natural origin. This present mini-review briefly discusses selected examples regarding advancements in bioinformatics and genomics (focusing on genome mining and metagenomics approaches), as well as bioanalytics (mass-spectrometry) towards the microbial NPs-based drug discovery and development. The selected recent discoveries from 2015 to 2020 are featured herein.


ChemInform ◽  
2011 ◽  
Vol 42 (18) ◽  
pp. no-no ◽  
Author(s):  
Philip Williams ◽  
Analia Sorribas ◽  
Melanie-Jayne R. Howes
Keyword(s):  

Toxins ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 488 ◽  
Author(s):  
Tim Lüddecke ◽  
Andreas Vilcinskas ◽  
Sarah Lemke

Animal venoms are promising sources of novel drug leads, but their translational potential is hampered by the low success rate of earlier biodiscovery programs, in part reflecting the narrow selection of targets for investigation. To increase the number of lead candidates, here we discuss a phylogeny-guided approach for the rational selection of venomous taxa, using tarantulas (family Theraphosidae) as a case study. We found that previous biodiscovery programs have prioritized the three subfamilies Ornithoctoninae, Selenocosmiinae, and Theraphosinae, which provide almost all of the toxin sequences currently available in public databases. The remaining subfamilies are poorly represented, if at all. These overlooked subfamilies include several that form entire clades of the theraphosid life tree, such as the subfamilies Eumenophorinae, Harpactirinae, and Stromatopelminae, indicating that biodiversity space has not been covered effectively for venom biodiscovery in Theraphosidae. Focusing on these underrepresented taxa will increase the likelihood that promising candidates with novel structures and mechanisms of action can be identified in future bioprospecting programs.


Author(s):  
BALABHASKAR R ◽  
RAJENDRA KUMAR A ◽  
SELVARAJAN S ◽  
FARIDHA A ◽  
GAYATHRI GUNALAN

Natural products continue to be a source for the discovery of drugs and drug leads even from ancient period. 80% of drug molecules have been obtained from either natural products or derivatives of the natural product. It has been found that the concept of a single drug for treating single disease may become outdated in the near future and the need of polyherbal formulations, as an alternate remedy is under investigation. Medicinal and aromatic plants contain biologically important phytochemicals, which have known curative properties. They are found as secondary metabolites in plants. Plants also contain certain other compounds that moderate the effects of the active ingredients. Medicinal and aromatic plants have their own contribution toward the treatment of both noncommunicable and communicable diseases. A survey done by the WHO indicates that a majority of the world population tends to use plants for treating diseases. Cancer, the second largest cause of death after cardiovascular disease accounts for about 3500 million people globally. Due to the serious side effects of synthetic chemopreventive agents, research is going onto investigate the nature derived chemopreventive agents. In addition to the plant-derived compounds, marine, and animal resources also play an important role as clinically beneficial anticancer agents with minimal or no toxicity. The best examples for plant-derived compounds include vincristine, vinblastine, irinotecan, etoposide, and paclitaxel; they have a different mode of action against cancer such as interaction with microtubules, inhibition of topoisomerases I or II, alkylation of DNA, and interference with tumor signal transduction. The natural products from marine sources such as bryostatin, squalamine exhibit a significant antimitotic, and anti-angiogenic activities. The benefits of various anticancer drugs derived from natural products are the fact that it can have its effect on cancer cells alone without harming healthy cells, which is unlikely to be the case with other conventional chemotherapeutics. In this review, various natural products and their anticancer properties have been discussed briefly.


Author(s):  
Pedro J Ballester ◽  
W. Graham Richards

Molecular databases are routinely screened for compounds that most closely resemble a molecule of known biological activity to provide novel drug leads. It is widely believed that three-dimensional molecular shape is the most discriminating pattern for biological activity as it is directly related to the steep repulsive part of the interaction potential between the drug-like molecule and its macromolecular target. However, efficient comparison of molecular shape is currently a challenge. Here, we show that a new approach based on moments of distance distributions is able to recognize molecular shape at least three orders of magnitude faster than current methodologies. Such an ultrafast method permits the identification of similarly shaped compounds within the largest molecular databases. In addition, the problematic requirement of aligning molecules for comparison is circumvented, as the proposed distributions are independent of molecular orientation. Our methodology could be also adapted to tackle similar hard problems in other fields, such as designing content-based Internet search engines for three-dimensional geometrical objects or performing fast similarity comparisons between proteins. From a broader perspective, we anticipate that ultrafast pattern recognition will soon become not only useful, but also essential to address the data explosion currently experienced in most scientific disciplines.


2018 ◽  
Vol 19 (6) ◽  
pp. 1578 ◽  
Author(s):  
Nicholas Thomford ◽  
Dimakatso Senthebane ◽  
Arielle Rowe ◽  
Daniella Munro ◽  
Palesa Seele ◽  
...  

MedChemComm ◽  
2019 ◽  
Vol 10 (6) ◽  
pp. 867-879 ◽  
Author(s):  
Urmila Maitra ◽  
Lukasz Ciesla

The review provides an overview of discovery of new drug leads from natural extracts usingDrosophilaas a screening platform to evaluate the therapeutic potential of phytochemicals against Parkinson's disease.


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