H3D would like to extend a huge congratulations to our Director, Kelly Chibale for being elected as one of the 10 international members of the prestigious United States National Academy of Medicine 👏 Full press release here: nam.edu/national-acade… #NAM #PressRelease #Groundbreakingresearch

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-develop… #Innovation #GuardianNewspaper #RoyalSociety #Africa

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/s4146… UCT UCT IDM 🦟

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/ac… UCT UCT IDM 💡

Exciting Opportunity: Join H3D as a Postdoc Fellow in Medicinal Chemistry H3D is looking for talented postdoctoral fellows to contribute to cutting-edge research Closing Date: 10 Jan 2025 #PostDocOpportunity #MedicinalChemistry

🎉 Wrapping Up 2024 with Gratitude and Joy 🎉 As 2024 ends, we reflect on what a wonderfully busy and fulfilling year it has been for everyone H3. From all of us H3, we wish you a happy and joyous holiday season! Here’s to a bright and inspiring year ahead! ✨

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.ejme… 🌍 UCT UCT IDM

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/doi/full/10.11… 🧬 UCT UCT IDM

Our contributions to a manuscript appearing in Biochemistry 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/ac… UCT UCT IDM

📣 Hot off the press! A Viewpoint article appearing in the esteemed journal Angewandte Chemie written by @DrClintVeale, John Woodland, @Kathryn_Wicht and Kelly Chibale, entitled "Chemistry as a Catalyst for Transforming the Health and Wealth of South Africa" 🇿🇦 onlinelibrary.wiley.com/doi/10.1002/an…

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 💊 ACS Publications Bio & Med Chem Content UCT UCT IDM pubs.acs.org/doi/full/10.10…

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/s4438…

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/articl…

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/ac… UCT UCT IDM

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 🔄 UCT IDM pubs.acs.org/doi/full/10.10…

📣 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 👨‍🔬 UCT IDM UCT onlinelibrary.wiley.com/doi/10.1002/an…

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/ac…

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/10.10…

📣 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" 💊 UCT IDM UCT onlinelibrary.wiley.com/doi/abs/10.100…

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 UCT IDM UCT pubs.acs.org/doi/10.1021/ac…