Recent Advances in Drug Discovery from South African  Marine Invertebrates

Davies‐Coleman, Michael T.; Veale, Clinton G. L.

doi:10.3390/md13106366

Cited by 14 publications

(19 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…[78] Of course, the SAR of hit natural products can be explored using the same methodological approach used for any other hit molecules, such as those discussed above. [79][80][81] However, an alternative is the identification of an SAR and pharmacophore through compound simplification, which has proven to be successful in developing clinical candidates, which are easier to obtain. [78] Halichondrin B ( 59), a marine natural product isolated from the Halichondria okadai Kadota sponge, was found to possess exceptional potency against a range of cancer cell lines in vitro, as well as in vivo antitumor activity in a murine model of cancer.…”

Section: Case Study: Natural Product Sarmentioning

confidence: 99%

“…Importantly, this substitution at position N-5 prevented the formation of a hydrogen bond with the glutamine carbonyl, thus suggesting it was not essential for PDE-1 inhibitory activity. Accordingly, Luo and co-workers hypothesized that by introducing a sterically bulky benzyl group onto the scaffold of compound 79 (81), they could disrupt the hydrogen bond interaction with the binding site glutamine, thereby reducing its affinity for the PDE-9 binding site, whilst maintaining PDE-1 activity. This approach was remarkably successful, resulting in the obliteration of PDE-9 inhibitory, activity, coupled to an impressive improvement in PDE-1 inhibitor activity.…”

Section: Case Study: Structure-based Designmentioning

confidence: 99%

See 1 more Smart Citation

Into the Fray! A Beginner's Guide to Medicinal Chemistry

Veale

2021

ChemMedChem

View full text Add to dashboard Cite

Modern medicinal chemistry is a complex, multidimensional discipline that operates at the interface of the chemical and biological sciences. The medicinal chemistry contribution to drug discovery is typically described in the context of the wellrecited linear progression of the drug discovery pipeline. However, compound optimization is idiosyncratic to each project, and clear definitions of hit and lead molecules and the subsequent progress along the pipeline becomes easily blurred. In addition, this description lacks insight into the entangled relationship between chemical and pharmacological properties, and thus provides limited guidance on how innovative medicinal chemistry strategies can be applied to solve optimization problems, regardless of the stage in the pipeline. Through discussion and illustrative examples, this article seeks to provide insights into the finesse of medicinal chemistry and the subtlety of balancing chemical properties pharmacology. In so doing, it aims to serve as an accessible and simple-to-digest guide for anyone who wishes to learn about the underlying principles of medicinal chemistry, in a context that has been decoupled from the pipeline description.

show abstract

Section: Case Study: Natural Product Sarmentioning

confidence: 99%

Section: Case Study: Structure-based Designmentioning

confidence: 99%

Into the Fray! A Beginner's Guide to Medicinal Chemistry

Veale

2021

ChemMedChem

View full text Add to dashboard Cite

show abstract

“…The resultant information is then utilized to direct efforts to culture antimicrobial-producing bacteria, or to clone and express pathways of interest for compound production in the lab. Using this approach, Dr. Kwan reported progress towards codon-optimized expression of chemical pathways, such as that for mandelalides that have been reported as potential antitumor agents as well as toxic for MRSA [ 79 ].…”

Section: Microbial-ecology Driven Discovery Of Antimicrobials From Thmentioning

confidence: 99%

Microbial-derived products as potential new antimicrobials

Seal

Drider

Oakley

et al. 2018

Vet Res

View full text Add to dashboard Cite

Due to the continuing global concerns involving antibiotic resistance, there is a need for scientific forums to assess advancements in the development of antimicrobials and their alternatives that might reduce development and spread of antibiotic resistance among bacterial pathogens. The objectives of the 2nd International Symposium on Alternatives to Antibiotics were to highlight promising research results and novel technologies that can provide alternatives to antibiotics for use in animal health and production, assess challenges associated with their authorization and commercialization for use, and provide actionable strategies to support their development. The session on microbial-derived products was directed at presenting novel technologies that included exploiting CRISPR-Cas nucleases to produce sequence-specific antimicrobials, probiotics development via fecal microbiome transplants among monogastric production animals such as chickens and mining microbial sources such as bacteria or yeast to identify new antimicrobial compounds. Other research has included continuing development of antimicrobial peptides such as newly discovered bacteriocins as alternatives to antibiotics, use of bacteriophages accompanied by development of unique lytic proteins with specific cell-wall binding domains and novel approaches such as microbial-ecology guided discovery of anti-biofilm compounds discovered in marine environments. The symposium was held at the Headquarters of the World Organisation for Animal Health (OIE) in Paris, France during 12–15 December 2016.

show abstract

“…Knowledge of the diversity of subtidal benthic macrofauna is less extensive and focused research is more sporadic and mostly limited to observational data obtained by SCUBA at depths of less than 30 m during collection of invertebrate specimens (sponges, tunicates, soft corals) for marine natural product chemistry. [31][32][33][34] Recent data collected by a remotely operated vehicle through the African Coelacanth Ecosystem Programme suggest that the Bay may support extraordinary invertebrate diversity including numerous novel, undescribed taxa (Parker-Nance and Dorrington, unpublished data).…”

Section: Algoa Bay As a Case Study For The First South African Marinementioning

confidence: 99%

Working together for our oceans: A marine spatial plan for Algoa Bay, South Africa

Dorrington¹,

Lombard²,

Bornman³

et al. 2018

S. Afr. J. Sci.

View full text Add to dashboard Cite

Southern Africa occupies a critical position within the southern hemisphere for the study of broadscale global change and the three oceans around South Africa (the Atlantic, Indian and Southern Oceans) play a vital role in determining local and regional climate and weather patterns. Oceans and coasts also provide various resources and services (e.g. food and carbon sequestration), but these services are threatened by human activities. Uncertainty of the impact and consequences of these anthropogenic activities makes it problematic to manage marine resources. Given the recent global emphasis on the development of 'ocean economies', the exploitation of living (fisheries, aquaculture and tourism) and non-living (oil and gas, minerals, energy) marine resources should be on a scale that is socially and economically justifiable and ecologically sustainable. In 2014, 'Operation Phakisa' was launched in South Africa as an initiative to accelerate execution of the National Development Plan. 1 The primary focus of Phakisa is to unlock the economic potential of South Africa's oceans. 2 This will be achieved through the 'implementation of an overarching, integrated ocean governance framework for sustainable growth of the ocean economy that will maximise socioeconomic benefits while ensuring adequate ocean environmental protection' by 2019. Marine spatial planning (MSP) is a key component of this integrated governance framework, and the development of MSP legislation during 2016 was prioritised as 'critical' to achieving the Operation Phakisa objectives. Accordingly, the Department of Environmental Affairs (DEA) published the Marine Spatial Planning Bill (2017) 3 'to provide a framework for marine spatial planning in South Africa's waters; to provide for the development of the marine spatial plan; to provide for institutional arrangements for the implementation of the marine spatial plan and governance of the use of the ocean by multiple sectors; and to provide for matters connected therewith'.

show abstract

Recent Advances in Drug Discovery from South African Marine Invertebrates

Cited by 14 publications

References 37 publications

Into the Fray! A Beginner's Guide to Medicinal Chemistry

Into the Fray! A Beginner's Guide to Medicinal Chemistry

Microbial-derived products as potential new antimicrobials

Working together for our oceans: A marine spatial plan for Algoa Bay, South Africa

Contact Info

Product

Resources

About