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/doi/10.1021/acs…
📣 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/doi/…
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/doi/full/10.102…
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/doi/10.1021/acs…
📣 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/doi/…
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/doi/full/10.102…
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: pubs.acs.org/doi/10.1021/acs… @UCT_news @UCTIDM
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: sciencedirect.com/science/ar…
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/articles/s44386-0…
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/doi/full/10.102…
📣 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/doi/…
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 🧫 pubs.acs.org/doi/10.1021/acs… @UCT_news @UCTIDM
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: febs.onlinelibrary.wiley.com… 🧬 @UCT_news @UCTIDM
Appearing in the European Journal of Medicinal Chemistry, our latest publication by Dziwornu and Attram et al. reports the antischistosomal potential of a new series of compounds derived from the privileged benzimidazole scaffold: doi.org/10.1016/j.ejmech.202… 🌍 @UCT_news @UCTIDM
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
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: pubs.acs.org/doi/10.1021/acs… @UCT_news @UCTIDM 💡
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: nature.com/articles/s41467-0… @UCT_news @UCTIDM 🦟
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: theguardian.com/global-devel…
#Innovation #GuardianNewspaper #RoyalSociety #Africa
