Cargando…

Single Stabilizing Point Mutation Enables High‐Resolution Co‐Crystal Structures of the Adenosine A(2A) Receptor with Preladenant Conjugates

The G protein‐coupled adenosine A(2A) receptor (A(2A)AR) is an important new (potential) drug target in immuno‐oncology, and for neurodegenerative diseases. Preladenant and its derivatives belong to the most potent A(2A)AR antagonists displaying exceptional selectivity. While crystal structures of t...

Descripción completa

Detalles Bibliográficos
Autores principales:	Claff, Tobias, Klapschinski, Tim A., Tiruttani Subhramanyam, Udaya K., Vaaßen, Victoria J., Schlegel, Jonathan G., Vielmuth, Christin, Voß, Jan H., Labahn, Jörg, Müller, Christa E.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	John Wiley and Sons Inc. 2022
Materias:	Research Articles
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9310709/ https://www.ncbi.nlm.nih.gov/pubmed/35174942 http://dx.doi.org/10.1002/anie.202115545

Ejemplares similares

Irreversible Antagonists for the Adenosine A(2B) Receptor †
por: Temirak, Ahmed, et al.
Publicado: (2022)

Structural basis for the regulatory interactions of proapoptotic Par-4
por: Tiruttani Subhramanyam, Udaya K, et al.
Publicado: (2017)

Adrenergic Agonists Bind to Adrenergic-Receptor-Like Regions of the Mu Opioid Receptor, Enhancing Morphine and Methionine-Enkephalin Binding: A New Approach to “Biased Opioids”?
por: Root-Bernstein, Robert, et al.
Publicado: (2018)

Mutual Enhancement of Opioid and Adrenergic Receptors by Combinations of Opioids and Adrenergic Ligands Is Reflected in Molecular Complementarity of Ligands: Drug Development Possibilities
por: Root-Bernstein, Robert, et al.
Publicado: (2019)

Crystal structure of adenosine A(2A) receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction
por: Claff, Tobias, et al.
Publicado: (2023)

Fluorinated Adenosine A(2A) Receptor Antagonists Inspired by Preladenant as Potential Cancer Immunotherapeutics
por: Yuan, Gengyang, et al.
Publicado: (2017)

High-throughput stability screening for detergent-solubilized membrane proteins
por: Kotov, Vadim, et al.
Publicado: (2019)

Radiation Dosimetry of a Novel Adenosine A(2A) Receptor Radioligand [(11)C]Preladenant Based on PET/CT Imaging and Ex Vivo Biodistribution in Rats
por: Zhou, Xiaoyun, et al.
Publicado: (2016)

Activated microglia nibbling glycosaminoglycans from spinal cord perineural nets: a new mechanism for neuropathic pain
por: Müller, Christa E., et al.
Publicado: (2022)

Controlled In Meso Phase Crystallization – A Method for the Structural Investigation of Membrane Proteins
por: Kubicek, Jan, et al.
Publicado: (2012)

Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A(2A) and Dual A(1)/A(2A) Receptor Affinity
por: Załuski, Michał, et al.
Publicado: (2023)

A grid-enabled web service for low-resolution crystal structure refinement
por: O’Donovan, Daniel J., et al.
Publicado: (2012)

Expression and Purification of Functional Human Mu Opioid Receptor from E.coli
por: Ma, Yanbin, et al.
Publicado: (2013)

High-efficient production and biophysical characterisation of nicastrin and its interaction with APPC100
por: Yu, Kun, et al.
Publicado: (2017)

Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids
por: Rivière, Solenne, et al.
Publicado: (2020)

The Use of Adenosine to Enable Safe Implantation of Transcatheter Tricuspid Valve
por: Zeniou, Vicki, et al.
Publicado: (2017)

C2‐linked alkynyl poly‐ethylene glycol(PEG) adenosine conjugates as water‐soluble adenosine receptor agonists
por: Ferguson, Lindsay, et al.
Publicado: (2022)

High-resolution crystal structure of human asparagine synthetase enables analysis of inhibitor binding and selectivity
por: Zhu, Wen, et al.
Publicado: (2019)

Data on solubilization, identification, and thermal stability of human Presenilin-2
por: Yang, Ge, et al.
Publicado: (2018)

Synthesis of Triazole-Linked SAM-Adenosine Conjugates: Functionalization of Adenosine at N-1 or N-6 Position without Protecting Groups
por: Atdjian, Colette, et al.
Publicado: (2020)

Crystal Structure of Schistosoma mansoni Adenosine Phosphorylase/5’-Methylthioadenosine Phosphorylase and Its Importance on Adenosine Salvage Pathway
por: Torini, Juliana Roberta, et al.
Publicado: (2016)

Enhanced A(3 )adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates
por: Klutz, Athena M, et al.
Publicado: (2008)

Synthesis and Properties of a New Water-Soluble Prodrug of the Adenosine A(2A) Receptor Antagonist MSX-2
por: Vollmann, Karl, et al.
Publicado: (2008)

Author Correction: High-resolution crystal structure of human asparagine synthetase enables analysis of inhibitor binding and selectivity
por: Zhu, Wen, et al.
Publicado: (2019)

High-resolution diffusion kurtosis imaging at 3T enabled by advanced post-processing
por: Mohammadi, Siawoosh, et al.
Publicado: (2015)

Influence of solubilization and AD-mutations on stability and structure of human presenilins
por: Yang, Ge, et al.
Publicado: (2017)

Cryogenic Focused Ion Beam Enables Atomic-Resolution Imaging of Local Structures in Highly Sensitive Bulk Crystals and Devices
por: Zhou, Jinfei, et al.
Publicado: (2022)

Adenosine Conjugated Docetaxel Nanoparticles—Proof of Concept Studies for Non-Small Cell Lung Cancer
por: Aldawsari, Hibah M., et al.
Publicado: (2022)

Dual Electrocatalysis Enables Enantioselective Hydrocyanation of Conjugated Alkenes
por: Song, Lu, et al.
Publicado: (2020)

Crystal structures of the A(2A) adenosine receptor and their use in medicinal chemistry
por: Jacobson, Kenneth A
Publicado: (2013)

Liquid Crystals-Enabled AC Electrokinetics
por: Peng, Chenhui, et al.
Publicado: (2019)

Liquid Crystal Enabled Dynamic Nanodevices
por: Ma, Zhenhe, et al.
Publicado: (2018)

Computerized Modeling of Adenosine Triphosphate, Adenosine Triarsenate and Adenosine Trivanadate
por: Nascimento, Valter A., et al.
Publicado: (2012)

Adenosine-Metabolizing Enzymes, Adenosine Kinase and Adenosine Deaminase, in Cancer
por: Zhulai, Galina, et al.
Publicado: (2022)

Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists
por: Claff, Tobias, et al.
Publicado: (2019)

A Cas9-mediated adenosine transient reporter enables enrichment of ABE-targeted cells
por: Brookhouser, Nicholas, et al.
Publicado: (2020)

Purinoceptor Targeted Cytotoxicity of Adenosine Triphosphate-Conjugated Biogenic Selenium Nanoparticles in Human Colon Cancer Cells
por: Saravanakumar, Kandasamy, et al.
Publicado: (2022)

Xanthine–Dopamine Hybrid Molecules as Multitarget Drugs with Potential for the Treatment of Neurodegenerative Diseases
por: Załuski, Michał, et al.
Publicado: (2023)

Crystal structure of a constitutive active mutant of adenosine A(2A) receptor
por: Cui, Min, et al.
Publicado: (2022)

High resolution crystal calorimetry at LHC
por: Schneegans, M, et al.
Publicado: (1992)

Cannot write session to /tmp/vufind_sessions/sess_3nbuh2m9i82bo7a2hf1kqdcoqo