Medicinal Chemistry Out of Africa

Chibale, Kelly; Wicht, Kathryn J.; Woodland, John G.

doi:10.1021/acs.jmedchem.1c01183

Cited by 7 publications

(9 citation statements)

References 4 publications

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“…Despite the further clinical development of MMV048 being stopped in Phase II due to some preclinical safety liabilities, which are yet to be understood, the discovery process of MMV048 and UCT943 facilitated not only the advancement of basic and clinical sciences but also infrastructure development which to this day partly anchors the drug discovery capabilities at H3D. 13 MoA studies leading to the identification of Pf PI4K as the novel target of MMV048 ushered the first time in which a chemical proteomics approach was used to identify a malaria drug target. At this juncture, it is noteworthy that MMV048 has set the precedence for the clinical validation of a Plasmodium kinase inhibitor.…”

Section: Tuberculosismentioning

confidence: 99%

“…At this juncture, it is noteworthy that MMV048 has set the precedence for the clinical validation of a Plasmodium kinase inhibitor. 13 …”

Section: Tuberculosismentioning

confidence: 99%

“…Some aspects of our work can also be found in our recent publication: “ Medicinal Chemistry out of Africa ”. 13 …”

mentioning

confidence: 99%

“…Some aspects of our work can also be found in our recent publication: "Medicinal Chemistry out of Af rica". 13 ■ MALARIA Phenotypic whole-cell high throughput screening of a 36,608member SoftFocus 14 Kinase (SFK) library of small molecules, spanning more than 200 chemotypes, against the human malaria parasite Pf drug-sensitive (3D7) and drug-resistant (Dd2) strains led to the identification of more than 200 hits displaying selective antiplasmodium activity. A greater than 80% inhibition of parasite growth at a primary and retest concentration of 1.82 μM and absence of cytotoxicity on a mammalian cell-line at this concentration was defined as hit criteria.…”

mentioning

confidence: 99%

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Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

Singh

Mambwe

Korkor

et al. 2022

ACS Med. Chem. Lett.

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As the so-called “next frontier” in global economic terms, Africa’s disease burden continues to choke and cripple economic growth across the continent. The highest burden is attributable to malaria and tuberculosis (TB), which also remain among the deadliest infectious diseases affecting mankind the world over (Malaria, 627,000 deaths; TB, 1.5 million deaths, in 2020). In achieving self-determination with respect to the health needs of all who live on the continent, Africa must align with global north efforts and be a source of health innovation. This will in part require the creation of an ecosystem of innovative pharmaceutical R&D and expanding it across the continent by scaling up through sustained performance and excellence. To this end, the Holistic Drug Discovery and Development (H3D) Centre at University of Cape Town in South Africa has risen to this challenge. Here, we highlight the innovation experiences gained at H3D, covering the advances made in our quest to contribute to a global pipeline of therapeutic interventions against malaria and TB. We discuss selected chemical series starting from their identification, structure–activity relationships, mode of action, safety, proof-of-concept studies, and lessons learned.

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Section: Tuberculosismentioning

confidence: 99%

“…At this juncture, it is noteworthy that MMV048 has set the precedence for the clinical validation of a Plasmodium kinase inhibitor. 13 …”

Section: Tuberculosismentioning

confidence: 99%

“…Some aspects of our work can also be found in our recent publication: “ Medicinal Chemistry out of Africa ”. 13 …”

mentioning

confidence: 99%

mentioning

confidence: 99%

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Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

Singh

Mambwe

Korkor

et al. 2022

ACS Med. Chem. Lett.

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“…There is limited drug discovery research in sub-Saharan Africa [ 1 ], with the notable exception of Holistic Drug Discovery and Development (H3D), which is based in Cape Town. Hence, we recognized the value in outlining our vision and the progress made in Ghana towards the development of drug discovery research and to highlight some of the challenges that we face.…”

Section: Introductionmentioning

confidence: 99%

Drug discovery research in Ghana, challenges, current efforts, and the way forward

et al. 2022

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We have a long-term vision to develop drug discovery research capacity within Ghana, to tackle unmet medical needs in Ghana and the wider West African region. However, there are several issues and challenges that need to be overcome to enable this vision, including training, human resource, equipment, infrastructure, procurement, and logistics. We discuss these challenges from the context of Ghana in this review. An important development is the universities and research centres within Ghana working together to address some of these challenges. Therefore, while there is a long way to go to fully accomplish our vision, there are encouraging signs.

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Biological and Medicinal Chemistry in Africa

et al. 2023

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The young, fast‐growing population of Africa means that harnessing the economic benefits of scientific research is critical to sustained and equitable growth in the continent. Moreover, the whole world would benefit from the added intellectual contribution that would come from nurturing African science. The high burden of neglected diseases in Africa makes chemical biology a particularly important field. In this editorial, the reconvergence of science conducted at the interface of chemistry and biology is placed in the context of African participation, its importance to global science and the unique blend of supporting and hindering factors that influence African scientific contributions. The new Biological and Medicinal Chemistry in Africa special collection showcases a broad spectrum of African chemical biology.

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Medicinal Chemistry Out of Africa

Cited by 7 publications

References 4 publications

Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre

Drug discovery research in Ghana, challenges, current efforts, and the way forward

Biological and Medicinal Chemistry in Africa

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