Browsing by Author "Selent, Jana"

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  • Kumar, G Aditya; Sarkar, Parijat; Stepniewski, Tomasz Maciej, 1988-; Jafurulla, Md; Singh, Shishu Pal; Selent, Jana; Chattopadhyay, Amitabha (American Association for the Advancement of Science (AAAS), 2021)
    The function of several G protein-coupled receptors (GPCRs) exhibits cholesterol sensitivity. Cholesterol sensitivity of GPCRs could be attributed to specific sequence and structural features, such as the cholesterol ...
  • Lally, Ciara C.M.; Bauer, Brain; Selent, Jana; Sommer, Martha E. (Nature Publishing Group, 2017)
    G-protein-coupled receptors are membrane proteins that are regulated by a small family of arrestin proteins. During formation of the arrestin–receptor complex, arrestin first interacts with the phosphorylated receptor C ...
  • Kapla, Jon; Rodríguez Espigares, Ismael, 1990-; Ballante, Flavio; Selent, Jana; Carlsson, Jens (Public Library of Science (PLoS), 2021)
    The determination of G protein-coupled receptor (GPCR) structures at atomic resolution has improved understanding of cellular signaling and will accelerate the development of new drug candidates. However, experimental ...
  • Kolb, Peter; Kenakin, Terry; Alexander, Stephen P. H.; Bermudez, Marcel; Bohn, Laura M.; Breinholt, Christian S.; Bouvier, Michel; Hill, Stephen J.; Kostenis, Evi; Martemyanov, Kirill A.; Neubig, Rick R.; Onaran, H. Ongun; Rajagopal, Sudarshan; Roth, Bryan L.; Selent, Jana; Shukla, Arun K.; Sommer, Martha E.; Gloriam, David E. (Wiley, 2022)
    GPCRs modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved drugs. Depending on which ligand activates a receptor, it can engage different intracellular transducers. This 'biased ...
  • Ghosh, Eshan; Dwivedi, Hemlata; Baidya, Mithu; Srivastava, Ashish; Kumari, Punita; Stepniewski, Tomek; Kim, Hee Ryung; Lee, Mi-Hye; van Gastel, Jaana; Chaturvedi, Madhu; Roy, Debarati; Pandey, Shubhi; Maharana, Jagannath; Guixà González, Ramon, 1978-; Luttrell, Louis M.; Chung, Ka Young; Dutta, Somnath; Selent, Jana; Shukla, Arun K. (Elsevier, 2019)
    Desensitization, signaling, and trafficking of G-protein-coupled receptors (GPCRs) are critically regulated by multifunctional adaptor proteins, β-arrestins (βarrs). The two isoforms of βarrs (βarr1 and 2) share a high ...
  • Azuaje, Jhonny; López, Paula; Iglesias, Alba; de la Fuente, Rocío Ailim; Pérez Rubio, José M.; García, Diego; Maciej Stępniewski, Tomasz; García Mera, Xerardo; Brea, José; Selent, Jana; Pérez Sala, Dolores; Castro, Marián; Loza, María I.; Sotelo, Eddy (Nature Publishing Group, 2017)
    Some 5-HT2B fluorescent probes were obtained by tagging 1-(2,5-dimethoxy-4-iodophenyl)-propan-2-amine (DOI) with a subset of fluorescent amines. Some of the resulting fluorescent ligands showed excellent affinity and ...
  • Giubilaro, Jenna; Schuetz, Doris A.; Stepniewski, Tomasz Maciej, 1988-; Namkung, Yoon; Khoury, Etienne; Lara Márquez, Mónica; Campbell, Shirley; Beautrait, Alexandre; Armando, Sylvain; Radresa, Olivier; Duchaine, Jean; Lamarche Vane, Nathalie; Claing, Audrey; Selent, Jana; Bouvier, Michel; Marinier, Anne; Laporte, Stéphane A. (Nature Research, 2021)
    Internalization and intracellular trafficking of G protein-coupled receptors (GPCRs) play pivotal roles in cell responsiveness. Dysregulation in receptor trafficking can lead to aberrant signaling and cell behavior. Here, ...
  • Dwivedi, Hemlata; Chaturvedi, Madhu; Baidya, Mithu; Stepniewski, Tomasz Maciej, 1988-; Pandey, Shubhi; Maharana, Jagannath; Srivastava, Ashish; Caengprasath, Natarin; Hanyaloglu, Aylin C.; Selent, Jana; Shukla, Arun K. (American Association for the Advancement of Science (AAAS), 2020)
    Agonist-induced phosphorylation of G protein-coupled receptors (GPCRs) is a key determinant for their interaction with β-arrestins (βarrs) and subsequent functional responses. Therefore, it is important to decipher the ...
  • Ågren, Richard; Stepniewski, Tomasz Maciej, 1988-; Zeberg, Hugo; Selent, Jana; Sahlholm, Kristoffer (MDPI, 2021)
    The forward (kon) and reverse (koff) rate constants of drug-target interactions have important implications for therapeutic efficacy. Hence, time-resolved assays capable of measuring these binding rate constants may be ...
  • Martí Solano, Maria; Sanz, Ferran; Pastor Maeso, Manuel; Selent, Jana (Public Library of Science (PLoS), 2014)
    Functional selectivity is a property of G protein-coupled receptors that allows them to preferentially couple to particular signaling partners upon binding of biased agonists. Publication of the X-ray crystal structure of ...
  • Koklič, Tilen; Hrovat, Alenka; Guixà González, Ramon, 1978-; Rodríguez Espigares, Ismael, 1990-; Navio, Damaris; Frangež, Robert; Uršič, Matjaž; Kubale, Valentina; Plemenitaš, Ana; Selent, Jana; Šentjurc, Marjeta; Vrecl, Milka (MDPI, 2021)
    This study investigated the effect of type 1 gonadotropin releasing hormone receptor (GnRH-R) localization within lipid rafts on the properties of plasma membrane (PM) nanodomain structure. Confocal microscopy revealed ...
  • Peralta-Garcia, Alejandro; Torrens Fontanals, Mariona; Stepniewski, Tomasz Maciej, 1988-; Grau-Expósito, Judith; Perea, David; Ayinampudi, Vikram; Waldhoer, Maria; Zimmermann, Mirjam; Buzón, María J.; Genescà, Meritxell; Selent, Jana (MDPI, 2021)
    Since the start of the COVID-19 outbreak, pharmaceutical companies and research groups have focused on the development of vaccines and antiviral drugs against SARS-CoV-2. Here, we apply a drug repurposing strategy to ...
  • Kaczor, Agnieszka A.; Guixà González, Ramon, 1978-; Carrió Gaspar, Pau, 1982-; Obiol Pardo, Cristian; Pastor Maeso, Manuel; Selent, Jana (Springer, 2012)
    Protein surface roughness is a structural property associated with ligand-protein and protein-protein binding interfaces. In this work we apply for the first time the concept of surface roughness, expressed as the fractal ...
  • Rodríguez Espigares, Ismael, 1990- (Universitat Pompeu Fabra, 2018-04-04)
    In this thesis, we present GPCRmd, an online repository with a submission system and visualization platform specifically designed for storing and providing easy access to molecular dynamics (MD) data of G protein-coupled ...
  • Torrens Fontanals, Mariona; Stepniewski, Tomasz Maciej, 1988-; Aranda García, David; Morales Pastor, Adrián; Medel Lacruz, Brian; Selent, Jana (MDPI, 2020)
    G protein-coupled receptors (GPCRs) are implicated in nearly every physiological process in the human body and therefore represent an important drug targeting class. Advances in X-ray crystallography and cryo-electron ...
  • Selent, Jana; Sanz, Ferran; Pastor Maeso, Manuel; De Fabritiis, Gianni (Public Library of Science (PLoS), 2010)
    G-protein coupled receptors, the largest family of proteins in the human genome, are involved in many complex signal transduction pathways, typically activated by orthosteric ligand binding and subject to allosteric ...
  • Martí Solano, Maria (Universitat Pompeu Fabra, 2015-02-10)
    La caracterització de diversos fàrmacs capaços d’unir-se a receptors associats a proteïnes G (GPCR)s ha revelat que els seus mecanismes d’acció no eren tan simples com es creia. Primer, l’anàlisi de la seva afinitat d’unió ...
  • Ågren, Richard; Zeberg, Hugo; Stepniewski, Tomasz Maciej, 1988-; Free, R. Benjamin; Reilly, Sean W.; Luedtke, Robert R.; Århem, Peter; Ciruela, Francisco; Sibley, David R.; Mach, Robert H.; Selent, Jana; Nilsson, Johanna; Sahlholm, Kristoffer (American Chemical Society (ACS), 2020)
    A solid understanding of the mechanisms governing ligand binding is crucial for rational design of therapeutics targeting the dopamine D2 receptor (D2R). Here, we use G protein-coupled inward rectifier potassium (GIRK) ...
  • Stepniewski, Tomasz Maciej, 1988-; Mancini, Arturo; Ågren, Richard; Torrens Fontanals, Mariona; Semache, Meriem; Bouvier, Michel; Sahlholm, Kristoffer; Breton, Billy; Selent, Jana (Royal Society of Chemistry, 2021)
    Brain functions rely on neurotransmitters that mediate communication between billions of neurons. Disruption of this communication can result in a plethora of psychiatric and neurological disorders. In this work, we combine ...
  • Guixà González, Ramon, 1978-; Albasanz, José L.; Rodriguez-Espigares, Ismael; Pastor Maeso, Manuel; Sanz, Ferran; Martí Solano, Maria; Manna, Moutusi; Martínez Seara, Hector; Hildebrand, Peter W.; Martín, Mairena; Selent, Jana (Nature Publishing Group, 2017)
    Cholesterol is a key component of cell membranes with a proven modulatory role on the function and ligand-binding properties of G-protein-coupled receptors (GPCRs). Crystal structures of prototypical GPCRs such as the ...