H3D

@H3D_UCT

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

162Following

899Followers

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H3D@H3D_UCT · Dec 23

🎉 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 @H3D. From all of us @H3D, we wish you a happy and joyous holiday season! Here’s to a bright and inspiring year ahead! ✨

H3D_UCT's tweet image. 🎉 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 @H3D.
From all of us @H3D, we wish you a happy and joyous holiday season!

Here’s to a bright and inspiring year ahead! ✨

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H3D@H3D_UCT · Jul 16

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…

H3D_UCT's tweet card. 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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H3D@H3D_UCT · May 28

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…

H3D_UCT's tweet card. 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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H3D@H3D_UCT · May 22

📣 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/10.1002/an…

H3D_UCT's tweet card. 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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H3D@H3D_UCT · May 20

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/10.10…

H3D_UCT's tweet card. 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...

H3D@H3D_UCT · Apr 11

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_news @UCTIDM

H3D_UCT's tweet card. 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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H3D@H3D_UCT · Apr 10

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…

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H3D@H3D_UCT · Mar 11

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…

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H3D@H3D_UCT · Feb 21

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/10.10…

H3D_UCT's tweet card. 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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H3D@H3D_UCT · Feb 7

📣 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/10.1002/an…

H3D_UCT's tweet card. 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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H3D@H3D_UCT · Feb 5

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/ac… @UCT_news @UCTIDM

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H3D@H3D_UCT · Jan 27

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_news @UCTIDM

H3D_UCT's tweet card. 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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H3D@H3D_UCT · Jan 14

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_news @UCTIDM

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H3D@H3D_UCT · Dec 12

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

H3D_UCT's tweet image. 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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H3D@H3D_UCT · Dec 6

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_news @UCTIDM 💡

H3D_UCT's tweet card. 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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H3D@H3D_UCT · Dec 5

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_news @UCTIDM 🦟

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H3D@H3D_UCT · Oct 29

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

H3D_UCT's tweet card. 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@H3D_UCT · Oct 24

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.edu/national-acade… #NAM #PressRelease #Groundbreakingresearch

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H3D@H3D_UCT · Oct 21

UPDATE📢 The #DrugDiscoveryAfrica 2025 Abstract submission deadline: 27th October 2024 All the details are on our website 👇: lnkd.in/ebRzu8fe The organising committee is looking forward to receiving your abstract. #AbstractSubmissions #DrugDiscoveryAfrica

H3D_UCT's tweet image. UPDATE📢

The #DrugDiscoveryAfrica 2025 Abstract submission deadline: 27th October 2024

All the details are on our website 👇: lnkd.in/ebRzu8fe

The organising committee is looking forward to receiving your abstract.

#AbstractSubmissions #DrugDiscoveryAfrica

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H3D@H3D_UCT · Oct 16

Reminder to sign up for the #H3D Open Day this week Saturday, 19 October 2024 at 9h00am - 13h00pm! If you're studying science in the Western Cape, don't miss the chance to tour our labs and learn about exciting careers in #DrugDiscovery😀

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