Results 261 to 270 of about 130,472 (328)

Profiling of HCAR1 signalling reveals Gαi/o and Gαs activation without β‐arrestin recruitment and the discovery of an allosteric agonist

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind   +6 more
wiley   +1 more source

Structural basis of frizzled 7 activation and allosteric regulation. [PDF]

open access: yesNat Commun
Bous J   +7 more
europepmc   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown   +2 more
wiley   +1 more source

A short intrinsically disordered region at KtrB's N-terminus facilitates allosteric regulation of K<sup>+</sup> channel KtrAB. [PDF]

open access: yesNat Commun
Stautz J   +11 more
europepmc   +1 more source

Schaftoside Improves Hfpef Through Regulation the Autophagy-Lysosome Pathway by Allosterically Targeting Camkii-Δ

open access: green
haiying Zhang   +9 more
openalex   +1 more source

The relationship between the cannabinoids and cardiac remodelling: A comprehensive review of pivotal mechanisms and emerging evidence

open access: yesBritish Journal of Pharmacology, EarlyView.
Cardiac remodelling and fibrosis after myocardial infarction or during chronic diseases, such as arterial and pulmonary hypertension or diabetes mellitus, continue to be the more important prognostic factors in determining survival, and so the search for effective anti‐fibrotic interventions is an important target for research and therapy in cardiology.
Anna Krzyżewska   +2 more
wiley   +1 more source

What is allosteric regulation? Exploring the exceptions that prove the rule! [PDF]

open access: yesJ Biol Chem
McCullagh M   +7 more
europepmc   +1 more source

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