Results 91 to 100 of about 1,156,973 (433)
Functional selectivity of GPCR-directed drug action through location bias. [PDF]
, 2017 G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco +6 more
core +3 more sources
Making tau amyloid models in vitro: a crucial and underestimated challenge
FEBS Letters, EarlyView.This review highlights the challenges of producing in vitro amyloid assemblies of the tau protein. We review how accurately the existing protocols mimic tau deposits found in the brain of patients affected with tauopathies. We discuss the important properties that should be considered when forming amyloids and the benchmarks that should be used to ...
Julien Broc, Clara Piersson, Yann Fichou
wiley +1 more source
Molecular Approaches To Target GPCRs in Cancer Therapy
Pharmaceuticals, 2011 Hundreds of G protein coupled receptor (GPCR) isotypes integrate and coordinate the function of individual cells mediating signaling between different organs in our bodies.
Giulio Innamorati +5 more
doaj +1 more source
Local Clustering and Global Spreading of Receptors for Optimal Spatial Gradient Sensing [PDF]
Phys. Rev. Lett. 134, 158401 (2025)Spatial information from cell-surface receptors is crucial for processes that require signal processing and sensing of the environment. Here, we investigate the optimal placement of such receptors through a theoretical model that minimizes uncertainty in gradient estimation.
arxiv +1 more source
Unraveling Mycobacterium tuberculosis acid resistance and pH homeostasis mechanisms
FEBS Letters, EarlyView.Mycobacterium tuberculosis exhibits a remarkable resilience to acid stress. In this Review, we discuss some of the molecular mechanisms and metabolic pathways used by the tubercle bacilli to adapt and resist host‐mediated acid stress. Mycobacterium tuberculosis (Mtb) is a successful pathogen that has developed a variety of strategies to survive and ...
Janïs Laudouze +3 more
wiley +1 more source
Expression and Role of Gonadotropin-Releasing Hormone 2 and Its Receptor in Mammals
Frontiers in Endocrinology, 2017 Gonadotropin-releasing hormone 1 (GnRH1) and its receptor (GnRHR1) drive mammalian reproduction via regulation of the gonadotropins. Yet, a second form of GnRH (GnRH2) and its receptor (GnRHR2) also exist in mammals.
Amy T. Desaulniers +3 more
doaj +1 more source
The role of dimerisation in the cellular trafficking of G-protein-coupled receptors [PDF]
, 2010 The concept that G-protein-coupled receptors can exist as homomeric and/or heteromeric complexes is now well established. Despite this, how dynamic such interactions are and if this may be modulated during receptor trafficking remain topics of debate ...
Milligan, Graeme
core +1 more source
The power of microRNA regulation—insights into immunity and metabolism
FEBS Letters, EarlyView.MicroRNAs are emerging as crucial regulators at the intersection of metabolism and immunity. This review examines how miRNAs coordinate glucose and lipid metabolism while simultaneously modulating T‐cell development and immune responses. Moreover, it highlights how cutting‐edge artificial intelligence applications can identify miRNA biomarkers ...
Stefania Oliveto +2 more
wiley +1 more source
GPR35 as a novel therapeutic target
Frontiers in Endocrinology, 2011 G protein-coupled receptors (GPCRs) remain the best studied class of cell surface receptors and the most tractable family of proteins for novel small molecule drug discovery. Despite this, a considerable number of GPCRs remain poorly characterised and in
Amanda eMacKenzie +4 more
doaj +1 more source
Crystallization of G Protein-Coupled Receptors [PDF]
, 2013 Oligomerization is one of several mechanisms that can regulate the activity of G protein-coupled receptors (GPCRs), but little is known about the structure of GPCR oligomers. Crystallography and NMR are the only methods able to reveal the details of receptor-receptor interactions at an atomic level, and several GPCR homodimers already have been ...
Pius S. Padayatti +2 more
openaire +3 more sources