The dark sides of the GPCR tree ‐ research progress on understudied GPCRs
British Journal of Pharmacology, EarlyView.Abstract A large portion of the human GPCRome is still in the dark and understudied, consisting even of entire subfamilies of GPCRs such as odorant receptors, class A and C orphans, adhesion GPCRs, Frizzleds and taste receptors. However, it is undeniable that these GPCRs bring an untapped therapeutic potential that should be explored further.
Magdalena M. Scharf +10 more
wiley +1 more source
International Journal of Cardiology: Heart & Vasculature, 2022 Introduction: Microvascular angina is a common cause of ischemia with non-obstructive coronary arteries (INOCA) and limited therapeutic options are available to those affected.
George R. Abraham +7 more
doaj
Astrocytic NMDA Receptors Modulate the Dynamics of Continuous Attractors [PDF]
arXivNeuronal networking supports complex brain functions, with neurotransmitters facilitating communication through chemical synapses. The release probability of neurotransmitters varies and is influenced by pre-synaptic neuronal activity. Recent findings suggest that blocking astrocytic N-Methyl-D-Aspartate (NMDA) receptors reduces this variation. However,
arxiv
Shared determinants of receptor binding for subtype selective, and dual endothelin‐angiotensin antagonists on the AT1 angiotensin II receptor [PDF]
, 1998 David Dascal +5 more
openalex +1 more source
Effect of Dual Endothelin Receptor Antagonist on a Retinal Degeneration Animal Model by Regulating Choroidal Microvascular Morphology. [PDF]
J Ophthalmol, 2021 Zhu X +6 more
europepmc +1 more source
Advancing antihypertensive drug development
British Journal of Pharmacology, EarlyView.Hypertension affects more than a billion individuals worldwide and remains a major cause of cardiovascular morbidity and mortality. Despite advances in therapies, optimal blood pressure control remains elusive for many patients because of treatment resistance, adverse effects, and adherence challenges.
Fay Pu +5 more
wiley +1 more source
Leveraging 13C NMR spectroscopic data derived from SMILES to predict the functionality of small biomolecules by machine learning: a case study on human Dopamine D1 receptor antagonists [PDF]
arXivThis study contributes to ongoing research which aims to predict small biomolecule functionality using Carbon-13 Nuclear Magnetic Resonance ($^{13}$C NMR) spectrum data and machine learning (ML). The approach was demonstrated using a bioassay on human dopamine D1 receptor antagonists.
arxiv
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose TMEM16A Ca2+‐gated Cl− channels mediate depolarisation of contractile vascular cells. The anthelmintic niclosamide was reported to modulate the TMEM16A channel, suggesting possible repurposing for vascular pharmacology. Here, we investigate the mechanism of TMEM16A modulation by niclosamide and explore its effect on the ...
Rachel Kaye +5 more
wiley +1 more source
Comparative analysis of computational approaches for predicting Transthyretin transcription activators and human dopamine D1 receptor antagonists [PDF]
arXivThe study expands the application of scikit-learn-based machine learning (ML) to the prediction of small biomolecule functionalities based on Carbon 13 isotope (13C) NMR spectroscopy data derived from Simplified Molecular Input Line Entry System (SMILES) notations.
arxiv
Role of Histone Deacetylase and Inhibitors in Cardiovascular Diseases
Cell Proliferation, EarlyView.HDACs play an important role in the occurrence and development of cardiovascular diseases, such as myocardial hypertrophy, hypertension, and atherosclerosis. HDAC inhibitors have broad prospects for the treatment of CVD, and different HDAC subtypes can act through different mechanisms.
Li‐Ying Zhang +4 more
wiley +1 more source