H3D
@H3D_UCT
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H3D is the first and only centre of its kind on the African continent, an integrated drug discovery and development centre with TB, malaria and AMR platforms
Joined October 2020
Natural products are vital to #drugdiscovery, yet #Africa’s vast #biodiversity remains underutilised 🌍 This perspective in #JNatProd examines opportunities for harnessing natural resources to address local and global health challenges @UCTIDM @UCT_news
pubs.acs.org
Natural products are vital to drug discovery, yet Africa’s vast biodiversity remains underutilized. This perspective examines barriers limiting Africa’s impact─such as weak infrastructure, limited...
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📣 New book chapter! "Multi-Target Antimalarials as a Strategy to Reduce Resistance Risk", written by Lauren B. Coulson and @Kelly_Chibale and appearing in "Polypharmacology: Strategies for Multi‐Target Drug Discovery" 💊 @UCTIDM @UCT_news
onlinelibrary.wiley.com
Malaria remains a serious health concern, and it is critical that the drug development pipeline is constantly replenished with new candidate drugs to ...
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Academic–industry #collaborations are a powerful catalyst for pharmaceutical innovation. Drawing on experiences at H3D, Winks et al. explore the benefits and challenges in the context of #drugdiscovery in this ACS Med. Chem. Lett. Viewpoint 💊
pubs.acs.org
Academic–industry collaborations are increasingly recognized as a catalyst for pharmaceutical innovation. While such partnerships are broadly valued across disciplines, their relevance to drug...
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Now out in #JMedChem! 💊 We report SARs for sapanisertib, identifying analogues with improved safety profiles and dual inhibitory activities against high-value Plasmodium targets PI4Kβ and PKG; a selected compound achieved an in vivo proof-of-concept 🐭
pubs.acs.org
We recently demonstrated that the anticancer human mTOR inhibitor sapanisertib displays antimalarial activity in a malaria mouse model of infection and inhibits multiple Plasmodium kinases, including...
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📣 New in #AngewChemIntEd: Woodland and Coertzen et al. show that the anticancer kinase inhibitor AZD0156 is a potent inhibitor of Plasmodium PI4Kβ and is an attractive candidate for medicinal chemistry optimisation against malaria 👨🔬 @UCTIDM @UCT_news
onlinelibrary.wiley.com
AZD0156, an ATM kinase inhibitor in clinical development, shows promising multistage antiplasmodial activity by targeting Plasmodium falciparum phosphatidylinositol 4-kinase (PfPI4Kβ). With an...
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In #JMedChem, we report a spiroindoline series with high sp3 character and potent activity against drug-resistant #malaria parasites. SAR explorations yielded a novel pyridylspiroindoline frontrunner (50) with promise for further optimisation 🔄 @UCTIDM
pubs.acs.org
In the search for novel chemotypes with high sp3 character and activity against the human malaria parasite Plasmodium falciparum, a spiroindoline series was identified from a phenotypic high-throug...
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Appearing earlier this month in #JMedChem, we report the design, synthesis and evaluation of novel mercapto-3-phenylpropanoyl dipeptides as dual angiotensin-converting enzyme C−domain-selective/neprilysin inhibitors: @UCT_news @UCTIDM.
pubs.acs.org
Dual angiotensin-converting enzyme (ACE) and neprilysin (NEP) inhibitors such as omapatrilat showed promise as potent treatments for hypertension but produced adverse effects due to their high...
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Despite the use of mefloquine in malaria prophylaxis and treatment, its metabolism is not completely understood. In our latest publication in #DrugMetabDispos, Cloete et al. identify CYP1A2 as a key enzyme involved in mefloquine metabolism:
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Identification of novel drug targets is a key component of modern #drugdiscovery 💡 We were part of a team that systematically assessed the P. falciparum genome to identify a list of 27 high-priority antimalarial targets. Read more in npj Drug Discovery!
nature.com
npj Drug Discovery - Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining
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Just out in #ACSMedChemLett: Ishmail et al. report the synthesis and SAR studies of acyl-thiourea platinum(II) complexes, yielding analogues with dual-stage antiplasmodium activity as part of the search for new antimalarials 💊 @ACSBioMed @UCT_news @UCTIDM
pubs.acs.org
Mixed-ligand platinum(II) complexes incorporating bipyridine and acyl-thiourea ligands were synthesized and evaluated for their in vitro growth inhibitory activity against the human malaria parasite...
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📣 Hot off the press! A Viewpoint article appearing in the esteemed journal @angew_chem written by @DrClintVeale, @jgwoodland, @Kathryn_Wicht and @Kelly_Chibale, entitled "Chemistry as a Catalyst for Transforming the Health and Wealth of South Africa" 🇿🇦
onlinelibrary.wiley.com
South Africa's rich natural resources fuelled its industrialisation but are marred by its colonial past. Despite 30 years of democracy, deep inequalities remain, with infectious diseases disproport...
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Our contributions to a manuscript appearing in @BiochemistryACS show that C-terminal amidation of AamAP1-Lys results in an analogue that is significantly more active against Gram-negative pathogens, with improved selectivity 🧫 @UCT_news @UCTIDM.
pubs.acs.org
C-terminal amidation of antimicrobial peptides (AMPs) is a frequent minor modification used to improve antibacterial potency, commonly ascribed to increased positive charge, protection from proteas...
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Our latest article, appearing in #FEBSLett, elucidates the molecular basis of inhibition of human angiotensin-1 converting enzyme (ACE), an important target for hypertension and inflammation, by a series of diprolyl-derived compounds: 🧬 @UCT_news @UCTIDM.
febs.onlinelibrary.wiley.com
Angiotensin-1-converting enzyme (ACE) has two catalytic domains, nACE and cACE. cACE primarily regulates blood pressure, whereas nACE is involved in fibrosis. Current inhibitors lack domain-selecti...
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Exciting Opportunity: Join @H3D_UCT as a Postdoc Fellow in Medicinal Chemistry. @H3D_UCT is looking for talented postdoctoral fellows to contribute to cutting-edge research . Closing Date: 10 Jan 2025. #PostDocOpportunity #MedicinalChemistry
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In our latest #ACSMedChemLett, together with colleagues in Brazil, Sousa et al. describe the integration of virtual screening, synthesis and experimental validation to yield non-covalent inhibitors of SARS-CoV-2 PLpro: @UCT_news @UCTIDM 💡.
pubs.acs.org
The SARS-CoV-2 pandemic has significantly challenged global public health, highlighting the need for effective therapeutic options. This study focuses on the papain-like protease (PLpro) of SARS-Co...
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Recently published in #NatCommun, Naude et al. shine light on how lipoidal uptake of antimalarial compounds influences their asexual blood stage versus transmission-blocking capabilities: @UCT_news @UCTIDM 🦟.
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Prof. @kellychibale, a leading scientist on the continent, believes that Africa, the cradle of humanity, holds keys to groundbreaking scientific advances. See the full article here: #Innovation #GuardianNewspaper #RoyalSociety #Africa.
theguardian.com
Prof Kelly Chibale says the world is failing to take advantage of African genetic diversity, and everyone could be losing out
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H3D would like to extend a huge congratulations to our Director, @KellyChibale for being elected as one of the 10 international members of the prestigious United States @theNAMedicine 👏. Full press release here: #NAM #PressRelease #Groundbreakingresearch.
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