Results 61 to 70 of about 1,083,474 (317)

The Vitamin Riboflavin and Its Derivative Lumichrome Activate the LasR Bacterial Quorum-Sensing Receptor

Molecular Plant-Microbe Interactions, 2008
Many bacteria use quorum sensing (QS) as an intercellular signaling mechanism to regulate gene expression in local populations. Plant and algal hosts, in turn, secrete compounds that mimic bacterial QS signals, allowing these hosts to manipulate QS ...
Sathish Rajamani, Wolfgang D. Bauer, Jayne B. Robinson, John M. Farrow, Everett C. Pesci, Max Teplitski, Mengsheng Gao, Richard T. Sayre, Donald A. Phillips   +8 more
doaj   +1 more source

Structural insights into binding specificity, efficacy and bias of a β2AR partial agonist

Nature Chemical Biology, 2018
Salmeterol is a partial agonist for the β2 adrenergic receptor (β2AR) and the first long-acting β2AR agonist to be widely used clinically for the treatment of asthma and chronic obstructive pulmonary disease.
M. Masureel, Y. Zou, Louis-Philippe Picard, E. T. van der Westhuizen, Jacob P. Mahoney, J. Rodrigues, Thomas J. Mildorf, R. Dror, D. Shaw, M. Bouvier, E. Pardon, J. Steyaert, R. Sunahara, W. Weis, Cheng Zhang, B. Kobilka   +15 more
semanticscholar   +1 more source

Agonist binding, agonist affinity and agonist efficacy at G protein‐coupled receptors [PDF]

British Journal of Pharmacology, 2008
Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs).
openaire   +3 more sources

Activation Pathways of Agonists, Partial Agonists and Inverse Agonist in Beta1 and Beta2 Adrenergic Receptors [PDF]

Biophysical Journal, 2010
Modulation of cell signaling by ligands of different efficacies via G-protein coupled receptors (GPCRs), depends intrinsically on the effect of the ligand on the dynamics between the multiple conformational states of these proteins. Ligands with different efficacies can remodel the energy landscape of the receptors, thereby perturbing this ...
Supriyo Bhattacharya, Nagarajan Vaidehi
openaire   +2 more sources

Beta-agonist stimulation ameliorates the phenotype of spinal and bulbar muscular atrophy mice and patient-derived myotubes [PDF]

, 2017
Spinal and bulbar muscular atrophy (SBMA) is a neuromuscular disease characterized by the loss of lower motor neurons. SBMA is caused by expansions of a polyglutamine tract in the gene coding for androgen receptor (AR).
Blaauw, Bert, Borgia, Doriana, Gomes Pereira, Marcelo, Lieberman, Andrew P., Maino, Eleonora, Malena, Adriana, Marchioretti, Caterina, Milioto, Carmelo, Pegoraro, Elena, Pennuto, Maria, Pennuto, Maria, Plebani, Mario, Polanco, Maria J., Sambataro, Fabio, Sambataro, Fabio, Sorar, Gianni, Soraru', Gianni, Venturini, Roberta, Vergani, Lodovica   +18 more
core   +3 more sources

Microfluidic radiosynthesis of [18F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors

Beilstein Journal of Organic Chemistry, 2017
Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers.
Thomas Lee Collier, Steven H. Liang, J. John Mann, Neil Vasdev, J. S. Dileep Kumar   +4 more
doaj   +1 more source

Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives

Frontiers in Chemistry, 2019
Among the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention.
Monica Baiula, Santi Spampinato, Luca Gentilucci, Alessandra Tolomelli   +3 more
doaj   +1 more source

Licraside as novel potent FXR agonist for relieving cholestasis: structure-based drug discovery and biological evaluation studies

Frontiers in Pharmacology, 2023
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi, Axi Shi, Tiantian Shen, Guoxu Wang, Yuhui Wei, Jingjing Guo   +5 more
doaj   +1 more source

The mechanics of agonistic muscles [PDF]

Journal of Biomechanics, 2018
In this study, we tested two assumptions that have been made in experimental studies on muscle mechanics: (i) that the torque-angle properties are similar among agonistic muscles crossing a joint, and (ii) that the sum of the torque capacity of individual muscles adds up to the torque capacity of the agonist group.
Heiliane de Brito Fontana, Heiliane de Brito Fontana, Andrew Sawatsky, Walter Herzog, Seong-won Han   +4 more
openaire   +3 more sources

Conjecturing about Small-Molecule Agonists and Antagonists of α4β1 Integrin: From Mechanistic Insight to Potential Therapeutic Applications

Biomedicines
Integrins are heterodimeric cell-surface receptors that regulate cell–cell adhesion and cellular functions through bidirectional signaling. On the other hand, anomalous trafficking of integrins is also implicated in severe pathologies as cancer ...
Tingting He, Daria Giacomini, Alessandra Tolomelli, Monica Baiula, Luca Gentilucci   +4 more
doaj   +1 more source