From nature to the laboratory and into the clinic

Nicolaou, K. C.; Chen, Jason S.; Dalby, Stephen M.

doi:10.1016/j.bmc.2008.10.089

Cited by 74 publications

(48 citation statements)

References 291 publications

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“…Such natural products have led to an impressive array of medications, either directly or indirectly, by serving as leads for structural modification and optimization (1)(2)(3)(4). Indeed, it is estimated that the majority of the currently used drugs are derived through one of these two closely related approaches to drug discovery and development.…”

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confidence: 99%

Design, synthesis, and biological evaluation of a biyouyanagin compound library

Nicolaou

Sanchini

Šarlah

et al. 2011

Proc. Natl. Acad. Sci. U.S.A.

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Modern drug discovery efforts rely, to a large extent, on lead compounds from two classes of small organic molecules; namely, natural products (i.e., secondary metabolites) and designed compounds (i.e., synthetic molecules). In this article, we demonstrate how these two domains of lead compounds can be merged through total synthesis and molecular design of analogs patterned after the targeted natural products, whose promising biological properties provide the motivation. Specifically, the present study targeted the naturally occurring biyouyanagins A and B and their analogs through modular chemical synthesis and led to the discovery of small organic molecules possessing anti-HIV and anti-arenavirus properties.

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confidence: 99%

Design, synthesis, and biological evaluation of a biyouyanagin compound library

Nicolaou

Sanchini

Šarlah

et al. 2011

Proc. Natl. Acad. Sci. U.S.A.

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“…The folate pathway is essential in bacteria for the synthesis of aromatic amino acids and purine nucleotides, and plays an essential role in pathogenesis. The pathway is also present in algae, higher plants, fungi and parasites, but absent in mammals, and is thus a potential target for new drug candidates (Coggins et al, 2003;Nicolaou, Chen, & Dalby, 2009). Abyssomicin C shows potent activity against Gram-positive bacteria, including clinical isolates of multiple-resistant and vancomycin-resistant S. aureus .…”

Section: Secondary Metabolites Synthesised By Pks Gene Clustermentioning

confidence: 98%

Marine Microbial Secondary Metabolites

Giordano

Coppola

Russo

et al. 2015

Advances in Microbial Physiology

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“…Biological diversity and its constituent chemical diversity have served as one of the richest sources of bioprospecting thus leading to the discoveries of some of the most important bioactive molecules that mankind have ever known [1][2][3][4][5]. From the antibiotic penicillin (from Penicillium sp.…”

Section: Introductionmentioning

confidence: 99%

Biodiversity and Chemodiversity: Future Perspectives in Bioprospecting

Ramesha¹,

Gertsch²,

Ravikanth³

et al. 2011

CDT

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Biological diversity and its constituent chemical diversity have served as one of the richest sources of bioprospecting leading to the discovery of some of the most important bioactive molecules for mankind. Despite this excellent record, in the recent past, however, bioprospecting of biological resources has met with little success; there has been a perceptible decline in the discovery of novel bioactive compounds. Several arguments have been proposed to explain the current poor success in bioprospecting. Among them, it has been argued that to bioprospect more biodiversity may not necessarily be productive, considering that chemical and functional diversity might not scale with biological diversity. In this paper, we offer a critique on the current perception of biodiversity and chemodiversity and ask to what extent it is relevant in the context of bioprospecting. First, using simple models, we analyze the relation among biodiversity, chemodiversity and functional redundancies in chemical plans of plants and argue that the biological space for exploration might still be wide open. Second, in the context of future bioprospecting, we argue that brute-force high throughput screening approaches alone are insufficient and cost ineffective in realizing bioprospecting success. Therefore, intelligent or non-random approaches to bioprospecting need to be adopted. We review here few examples of such approaches and show how these could be further developed and used in the future to accelerate the pace of discovery.

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From nature to the laboratory and into the clinic

Cited by 74 publications

References 291 publications

Design, synthesis, and biological evaluation of a biyouyanagin compound library

Design, synthesis, and biological evaluation of a biyouyanagin compound library

Marine Microbial Secondary Metabolites

Biodiversity and Chemodiversity: Future Perspectives in Bioprospecting

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