[HTML][HTML] Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

…, MS Gadd, KM Grzes, L Ellis, O Epemolu… - Nature …, 2016 - nature.com
Chemical strategies to using small molecules to stimulate hypoxia inducible factors (HIFs)
activity and trigger a hypoxic response under normoxic conditions, such as iron chelators and …

Reversal of Neuromusclar Blockade and Simultaneous Increase in Plasma Rocuronium Concentration after the Intravenous Infusion of the Novel Reversal Agent Org …

O Epemolu, A Bom, F Hope, R Mason - The Journal of the American …, 2003 - pubs.asahq.org
Background The purpose of this study was to determine the changes in the plasma
concentration of rocuronium and the reversal of its neuromuscular blockade after the intravenous …

[PDF][PDF] Development of a novel lead that targets M. tuberculosis polyketide synthase 13

…, D Matthews, D Floyd, P Scullion, J Riley, O Epemolu… - Cell, 2017 - cell.com
Widespread resistance to first-line TB drugs is a major problem that will likely only be resolved
through the development of new drugs with novel mechanisms of action. We have used …

Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R …

…, J Frost, C Galdeano, L Ellis, O Epemolu… - Journal of medicinal …, 2018 - ACS Publications
The von Hippel–Lindau tumor suppressor protein is the substrate binding subunit of the
VHL E3 ubiquitin ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) …

[PDF][PDF] The first potent and selective inhibitors of the glycine transporter type 2

…, IT Collie, RS Dickins, O Epemolu… - Journal of medicinal …, 2001 - academia.edu
Introduction. Glycine is one of the major inhibitory neurotransmitters in the spinal cord and
brain stem of vertebrates. 1 The inhibitory actions of glycine are mediated by the strychnine-…

Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis

…, SR Jonnala, LE Via, V Mizrahi, O Epemolu… - ACS infectious …, 2017 - ACS Publications
A potent, noncytotoxic indazole sulfonamide was identified by high-throughput screening of
>100,000 synthetic compounds for activity against Mycobacterium tuberculosis (Mtb). This …

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure–Activity Relationships, Mechanism of Action …

…, DF Warner, V Mizrahi, O Epemolu… - ACS infectious …, 2018 - ACS Publications
Mycobacterium tuberculosis (MTb) possesses two nonproton pumping type II NADH
dehydrogenase (NDH-2) enzymes which are predicted to be jointly essential for respiratory …

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

…, M Huggett, P Turner, A Smith, O Epemolu… - Journal of Medicinal …, 2018 - ACS Publications
With the emergence of multidrug-resistant strains of Mycobacterium tuberculosis there is a
pressing need for new oral drugs with novel mechanisms of action. Herein, we describe the …

Optimization of TAM16, a benzofuran that inhibits the thioesterase activity of Pks13; evaluation toward a preclinical candidate for a novel antituberculosis clinical target

…, F Tamaki, P Scullion, O Epemolu… - Journal of Medicinal …, 2021 - ACS Publications
With increasing drug resistance in tuberculosis (TB) patient populations, there is an urgent
need for new drugs. Ideally, new agents should work through novel targets so that they are …

[HTML][HTML] Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs

…, C Jansen, F Zuccotto, IH Gilbert, O Epemolu… - Nature …, 2022 - nature.com
Tuberculosis is a major global cause of both mortality and financial burden mainly in low and
middle-income countries. Given the significant and ongoing rise of drug-resistant strains of …