Cargando…

Small-Molecule Positive Allosteric Modulators of the β(2)-Adrenoceptor Isolated from DNA-Encoded Libraries

Conventional drug discovery efforts at the β(2)-adrenoceptor (β(2)AR) have led to the development of ligands that bind almost exclusively to the receptor’s hormone-binding orthosteric site. However, targeting the largely unexplored and evolutionarily unique allosteric sites has potential for develop...

Descripción completa

Detalles Bibliográficos
Autores principales:	Ahn, Seungkirl, Pani, Biswaranjan, Kahsai, Alem W., Olsen, Eva K., Husemoen, Gitte, Vestergaard, Mikkel, Jin, Lei, Zhao, Shuai, Wingler, Laura M., Rambarat, Paula K., Simhal, Rishabh K., Xu, Thomas T., Sun, Lillian D., Shim, Paul J., Staus, Dean P., Huang, Li-Yin, Franch, Thomas, Chen, Xin, Lefkowitz, Robert J.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	The American Society for Pharmacology and Experimental Therapeutics 2018
Materias:	Articles
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6022804/ https://www.ncbi.nlm.nih.gov/pubmed/29769246 http://dx.doi.org/10.1124/mol.118.111948

Ejemplares similares

Unique Positive Cooperativity Between the β-Arrestin–Biased β-Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the β2-Adrenergic Receptor
por: Pani, Biswaranjan, et al.
Publicado: (2021)

Conformationally Selective RNA Aptamers Allosterically Modulate the β(2)-Adrenoceptor
por: Kahsai, Alem W., et al.
Publicado: (2016)

Allosteric Nanobodies Reveal the Dynamic Range and Diverse Mechanisms of GPCR Activation
por: Staus, Dean P, et al.
Publicado: (2016)

Allosteric activation of proto-oncogene kinase Src by GPCR–beta-arrestin complexes
por: Pakharukova, Natalia, et al.
Publicado: (2021)

Allosteric modulator potentiates β(2)AR agonist–promoted bronchoprotection in asthma models
por: Ahn, Seungkirl, et al.
Publicado: (2023)

How carvedilol does not activate β(2)-adrenoceptors
por: Lefkowitz, Robert J., et al.
Publicado: (2023)

Signal transduction at GPCRs: Allosteric activation of the ERK MAPK by β-arrestin
por: Kahsai, Alem W., et al.
Publicado: (2023)

The GPCR–β-arrestin complex allosterically activates C-Raf by binding its amino terminus
por: Zang, Yunxiang, et al.
Publicado: (2021)

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor
por: Aristotelous, Tonia, et al.
Publicado: (2013)

Independent β-Arrestin2 and G(q)/Protein Kinase Cζ Pathways for ERK Stimulated by Angiotensin Type 1A Receptors in Vascular Smooth Muscle Cells Converge on Transactivation of the Epidermal Growth Factor Receptor
por: Kim, Jihee, et al.
Publicado: (2009)

Structure of the M2 muscarinic receptor-β-arrestin complex in a lipid nanodisc
por: Staus, Dean P., et al.
Publicado: (2020)

The Glycine Receptor Allosteric Ligands Library (GRALL)
por: Cerdan, Adrien H, et al.
Publicado: (2020)

The Role of Adrenoceptors in Bronchial Asthma
por: Patel, K. R.
Publicado: (1979)

Diazepam is not a direct allosteric modulator of α(1)‐adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase‐4
por: Williams, Lisa M., et al.
Publicado: (2018)

Loss of biased signaling at a G protein-coupled receptor in overexpressed systems
por: Li, Angus, et al.
Publicado: (2023)

Arresting a Transient Receptor Potential (TRP) Channel: β-ARRESTIN 1 MEDIATES UBIQUITINATION AND FUNCTIONAL DOWN-REGULATION OF TRPV4
por: Shukla, Arun K., et al.
Publicado: (2010)

β-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation
por: Ahn, Seungkirl, et al.
Publicado: (2009)

β(2)‐Adrenoceptor agonist activity of higenamine
por: Hudzik, Thomas J., et al.
Publicado: (2021)

In silico identification of a β(2)-adrenoceptor allosteric site that selectively augments canonical β(2)AR-Gs signaling and function
por: Shah, Sushrut D., et al.
Publicado: (2022)

The Role of Adrenoceptors in the Retina
por: Ruan, Yue, et al.
Publicado: (2020)

β-Arrestin–Biased Angiotensin II Receptor Agonists for COVID-19
por: Manglik, Aashish, et al.
Publicado: (2020)

Association of baseline self-reported fatigue with overall survival after stereotactic body radiation therapy for localized prostate cancer
por: Simhal, Rishabh K., et al.
Publicado: (2022)

Social media as a tool to disseminate library contents. Case study of the JFK Library Twitter account
por: Franch, Pere, et al.
Publicado: (2017)

Patient Factors Impacting Perioperative Outcomes for T1b-T2 Localized Renal Cell Carcinoma May Guide Decision for Partial versus Radical Nephrectomy
por: Shah, Yash B., et al.
Publicado: (2022)

A monoclonal antibody raised against a thermo-stabilised β(1)-adrenoceptor interacts with extracellular loop 2 and acts as a negative allosteric modulator of a sub-set of β(1)-adrenoceptors expressed in stable cell lines
por: Soave, Mark, et al.
Publicado: (2018)

Relationships of Adrenoceptor Polymorphisms with Obesity
por: Masuo, Kazuko, et al.
Publicado: (2011)

Adrenal adrenoceptors in heart failure
por: de Lucia, Claudio, et al.
Publicado: (2014)

Affinity selection of double-click triazole libraries for rapid discovery of allosteric modulators for GLP-1 receptor
por: Xin, Ye, et al.
Publicado: (2023)

A Full Pharmacological Analysis of the Three Turkey β-Adrenoceptors and Comparison with the Human β-Adrenoceptors
por: Baker, Jillian G.
Publicado: (2010)

β-Adrenoceptor-mediated Relaxation of Urinary Bladder Muscle in β(2)-Adrenoceptor Knockout Mice
por: Propping, Stefan, et al.
Publicado: (2016)

α (2)-Adrenoceptors: Challenges and Opportunities—Enlightenment from the Kidney
por: Pettinger, William A., et al.
Publicado: (2020)

Biosensor libraries harness large classes of binding domains for construction of allosteric transcriptional regulators
por: Juárez, Javier F., et al.
Publicado: (2018)

The signaling and selectivity of α‐adrenoceptor agonists for the human α2A, α2B and α2C‐adrenoceptors and comparison with human α1 and β‐adrenoceptors
por: Proudman, Richard G. W., et al.
Publicado: (2022)

β(1) Adrenoceptor antagonistic effects of the supposedly selective β(2) adrenoceptor antagonist ICI 118,551 on the positive inotropic effect of adrenaline in murine hearts
por: Pecha, Simon, et al.
Publicado: (2015)

Adrenaline-activated structure of the β(2)-adrenoceptor stabilized by an engineered nanobody
por: Ring, Aaron M., et al.
Publicado: (2013)

Adrenoceptors: ligand-activated molecular dynamics
por: Matijssen, B, et al.
Publicado: (2008)

Beta-Adrenoceptor Blocking Drugs and the Elderly
por: Wilkins, M. R., et al.
Publicado: (1984)

Uses of Beta-Adrenoceptor Blocking Drugs
por: Prichard, B. N. C., et al.
Publicado: (1976)

Alpha(2)‐adrenoceptor agonists inhibit form‐deprivation myopia in the chick
por: Carr, Brittany J, et al.
Publicado: (2019)

The presence of β(2)-adrenoceptors sensitizes α(2A)-adrenoceptors to desensitization after chronic epinephrine treatment
por: Bawa-Khalfe, Tasneem, et al.
Publicado: (2007)

Cannot write session to /tmp/vufind_sessions/sess_6qcvn2cf44i7jsup88kfaql4pq