Development of novel bosentan analogues as endothelin receptor antagonists for pulmonary arterial hypertension

Panchal, Jigar; Jaiswal, Shivangi; Jain, Sonika; Kumawat, Jyoti; Sharma, Arjun D.; Jain, Pankaj; Jain, Smita; Verma, Kanika; Dwivedi, Jaya; Sharma, Swapnil

doi:10.1016/j.ejmech.2023.115681

Cited by 11 publications

(1 citation statement)

References 55 publications

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“…The latest research has discovered that novel derivatives of bosentan, namely 17d, 16j, and 16h, endothelin receptor antagonists, can dose-dependently decrease HIF-1α levels in PAH rats 114 . A novel lysosomal autophagy inhibitor (ROC-325) can downregulate HIF-1αprotein expression in PASMCs, activate the eNOS-NO signaling pathway, and inhibit autophagy, thus suppressing pulmonary vascular remodeling, inducing pulmonary vasodilation, and alleviating the occurrence and progression of pulmonary arterial hypertension 115 .…”

Section: Hif-1a As a Target For The Treatment Of Hphmentioning

confidence: 99%

Expression and regulation of HIF-1a in hypoxic pulmonary hypertension: Focus on pathological mechanism and Pharmacological Treatment

Wan,

Yi,

Wang

et al. 2024

Int. J. Med. Sci.

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Hypoxia inducible factor-1(HIF-1), a heterodimeric transcription factor, is composed of two subunits (HIF-1α and HIF-1β). It is considered as an important transcription factor for regulating oxygen changes in hypoxic environment, which can regulate the expression of various hypoxia-related target genes and play a role in acute and chronic hypoxia pulmonary vascular reactions. In this paper, the function and mechanism of HIF-1a expression and regulation in hypoxic pulmonary hypertension (HPH) were reviewed, and current candidate schemes for treating pulmonary hypertension by using HIF-1a as the target were introduced, so as to provide reference for studying the pathogenesis of HPH and screening effective treatment methods.

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Section: Hif-1a As a Target For The Treatment Of Hphmentioning

confidence: 99%