Results 291 to 300 of about 130,849 (328)

Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials

British Journal of Pharmacology, EarlyView.
Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen, Declan P. McKernan, John P. Kelly   +2 more
wiley   +1 more source

Allosteric regulation by c-di-AMP modulates a complete N-acetylglucosamine signaling cascade in Saccharopolyspora erythraea. [PDF]

Nat Commun
You D, Zhao LC, Fu Y, Peng ZY, Chen ZQ, Ye BC.   +5 more
europepmc   +1 more source

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source

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

British 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, Shane C. Wright, Emilia Gvozdenovic, Kristina Nilsson, Kenneth L. Granberg, Michel Bouvier, Linda C. Johansson   +6 more
wiley   +1 more source

Mechanistic insights into allosteric regulation of the reductase component of p-hydroxyphenylacetate 3-hydroxylase by p-hydroxyphenylacetate: a model for effector-controlled activity of redox enzymes. [PDF]

RSC Chem Biol
Visitsatthawong S, Anuwan P, Lawan N, Chaiyen P, Wongnate T.   +4 more
europepmc   +1 more source

Allosteric Regulation of Ferroptosis Suppressor Protein 1 Revealed by Structure-Based Modeling and Simulations

Carlos Ventura, Xiaowei Bogetti, Ji Young Lee, İvet Bahar   +3 more
openalex   +1 more source

The return of metabolism: biochemistry and physiology of glycolysis

Biological Reviews, EarlyView.
ABSTRACT Glycolysis is a fundamental metabolic pathway central to the bioenergetics and physiology of virtually all living organisms. In this comprehensive review, we explore the intricate biochemical principles and evolutionary origins of glycolytic pathways, from the classical Embden–Meyerhof–Parnas (EMP) pathway in humans to various prokaryotic and ...
Nana‐Maria Grüning, Federica Agostini, Camila Caldana, Johannes Hartl, Matthias Heinemann, Markus A. Keller, Jan Lukas Krüsemann, Costanza Lamperti, Carole L. Linster, Steffen N. Lindner, Julia Muenzner, Jens Nielsen, Zoran Nikoloski, Bettina Siebers, Jacky L. Snoep, Hezi Tenenboim, Bas Teusink, Spencer J. Williams, Mirjam M. C. Wamelink, Markus Ralser   +19 more
wiley   +1 more source

Potassium–chloride cotransporter 2 activity dampens induced ictal‐like activity in neocortical slices containing the seizure propagation zone of temporal lobe epilepsy patients

Epilepsia, EarlyView.
The K⁺/Cl− cotransporter (KCC2) limits induced ictal‐like events and their spread in the supragranular layer of human neocortical slices from the seizure‐propagation zone of temporal lobe epilepsy patients. Cl⁻ extrusion is present in supragranular pyramidal neurons but limited under high somatic Cl⁻ load.
Alice Falck, Janna Lehnhoff, Mahraz Behbood, Egor Byvaltcev, Annette Aigner, Helena Radbruch, Pawel Fidzinski, Jan‐Hendrik Schleimer, Gabriel M. S. Janach, Noah Döhne, Julia Onken, Thilo Kalbhenn, Thomas Sauvigny, Rudolf A. Deisz, Susanne Schreiber, Martin Holtkamp, Ulf Strauss   +16 more
wiley   +1 more source

Cryo-EM structures of the human NaS1 and NaDC1 transporters revealed the elevator transport and allosteric regulation mechanism. [PDF]

Sci Adv
Chi X, Chen Y, Li Y, Dai L, Zhang Y, Shen Y, Chen Y, Shi T, Yang H, Wang Z, Yan R.   +10 more
europepmc   +1 more source

Convergent High O₂ Affinity but Distinct ATP-Mediated Allosteric Regulation of Hemoglobins in Oviparous and Viviparous Eremias Lizards from the Qinghai-Tibet Plateau. [PDF]

Animals (Basel)
Pu P, Niu Z, Ma M, Tang X, Chen Q.
europepmc   +1 more source