Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

How carvedilol does not activate β2-adrenoceptors

RJ Lefkowitz, HA Rockman, PJ Shim, S Liu… - Nature …, 2023 - nature.com
The introduction of β-adrenergic receptor blockers,“β-blockers”, as a treatment for heart
failure decades ago was a major advance in cardiovascular medicine 1–4. Moreover, it has …

Allosteric regulation of G-protein-coupled receptors: from diversity of molecular mechanisms to multiple allosteric sites and their ligands

AO Shpakov - International Journal of Molecular Sciences, 2023 - mdpi.com
Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs)
and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions …

Pathophysiology and pharmacology of G protein-coupled receptors in the heart

A Grogan, EY Lucero, H Jiang… - Cardiovascular …, 2023 - academic.oup.com
G protein-coupled receptors (GPCRs), comprising the largest superfamily of cell surface
receptors, serve as fundamental modulators of cardiac health and disease owing to their key …

Advances in adrenergic receptors for the treatment of chronic obstructive pulmonary disease: 2023 update

MG Matera, B Rinaldi, L Calzetta… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction Strong scientific evidence and large experience support the use of β2-agonists
for the symptomatic alleviation of COPD. Therefore, there is considerable effort in …

[HTML][HTML] Allosteric crosstalk in modular proteins: Function fine-tuning and drug design

S Abhishek, W Deeksha, KR Nethravathi… - Computational and …, 2023 - Elsevier
Modular proteins are regulatory proteins that carry out more than one function. These
proteins upregulate or downregulate a biochemical cascade to establish homeostasis in …

[HTML][HTML] Status of β1-adrenoceptor signal transduction system in cardiac hypertrophy and heart failure

NS Dhalla, SK Bhullar, A Adameova… - Reviews in …, 2023 - imrpress.com
Although β1-adrenoceptor (β1-AR) signal transduction, which maintains cardiac function, is
downregulated in failing hearts, the mechanisms for such a defect in heart failure are not …

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

Z Vuckovic, J Wang, V Pham, JI Mobbs, MJ Belousoff… - Elife, 2023 - elifesciences.org
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug
discovery. Despite decades of research, a molecular-level understanding of the general …

A 20:1 synergetic mixture of cafedrine/theodrenaline accelerates particle transport velocity in murine tracheal epithelium via IP3 receptor-associated calcium release

G Schmidt, G Rienas, S Müller, F Edinger… - Frontiers in …, 2023 - frontiersin.org
Background: Mucociliary clearance is a pivotal physiological mechanism that protects the
lung by ridding the lower airways of pollution and colonization by pathogens, thereby …

β-adrenergic receptor signaling mediated by β-arrestins and its potential role in heart failure

PC Nibley, SK Shenoy - Current Opinion in Physiology, 2023 - Elsevier
The lethality of heart failure (HF), particularly in the context of post-acute sequelae SARS-
CoV-2 infection (PASC)-related myocarditis, necessitates the discovery of the cellular …