Publications by authors named "Ren-Hua Jheng"
Liposomal PHD2 Inhibitors and the Enhanced Efficacy in Stabilizing HIF-1α.
Nanomaterials (Basel)
January 2022
Article Synopsis
- Inhibition of Prolyl hydroxylase domain-containing protein 2 (PHD2) is a key strategy for boosting hypoxia-inducible factor (HIF)-1α, leading to cellular adaptations to low oxygen levels, making it a critical target for therapy.
- Small-molecule PHD2 inhibitors like IOX2 can benefit from nanoformulations to enhance drug distribution and minimize side effects, especially through liposome delivery systems.
- The study successfully developed a method to encapsulate IOX2 and similar inhibitors into liposomes with high efficiency, showing improved effectiveness in raising HIF-1α levels in cells, particularly with targeting ligands, indicating potential for localized disease treatment.
7-Aminoquinoline (7AQ) and various amino derivatives thereof (-NHR) have been strategically designed and synthesized to study their excited-state proton-transfer (ESPT) properties. Due to the large separation between the proton donor -NHR and the acceptor -N- site, ESPT in 7AQ derivatives, if available, should proceed under protic solvent catalysis. ESPT is found to be influenced by the acidity of -NHR and the basicity of the proton-acceptor -N- in the quinoline moiety.
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