Browsing by Author "Selent, Jana"

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  • A molecular sensor for cholesterol in the human serotonin 1A receptor
    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 ...
  • Allosteric modulation of GPCR-induced β-arrestin trafficking and signaling by a synthetic intrabody
    Baidya, Mithu; Chaturvedi, Madhu; Dwivedi, Hemlata; Ranjan, Ashutosh; Devost, Dominic; Namkung, Yoon; Stepniewski, Tomasz Maciej, 1988-; Pandey, Shubhi; Baruah, Minakshi; Panigrahi, Bhanupriya; Sarma, Parishmita; Yadav, Manish K.; Maharana, Jagannath; Banerjee, Ramanuj; Kawakami, Kouki; Inoue, Asuka; Selent, Jana; Laporte, Stéphane A.; Hébert, Terence E.; Shukla, Arun K. (Nature Research, 2022)
    Agonist-induced phosphorylation of G protein-coupled receptors (GPCRs) is a primary determinant of β-arrestin (βarr) recruitment and trafficking. For several GPCRs such as the vasopressin receptor subtype 2 (V2R), ...
  • C-edge loops of arrestin function as a membrane anchor
    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 ...
  • Can molecular dynamics simulations improve the structural accuracy and virtual screening performance of GPCR models?
    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 ...
  • Characterization of allosteric communication networks in GPCRs
    Morales Pastor, Adrián (Universitat Pompeu Fabra, 2024-04-16)
    G protein-coupled receptors (GPCRs) are central to cellular signaling and pivotal in drug development. This thesis investigates allosteric communication in GPCRs, crucial for their effective modulation in pharmacotherapy. ...
  • Community guidelines for GPCR ligand bias: IUPHAR review 32
    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 ...
  • Conformational sensors and domain swapping reveal structural and functional differences between β-arrestin isoforms
    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 ...
  • Development of fluorescent probes that target serotonin 5-HT2B receptors
    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 ...
  • Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen
    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, ...
  • Distinct phosphorylation sites in a prototypical GPCR differently orchestrate β-arrestin interaction, trafficking, and signaling
    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 ...
  • Dopamine D 2 receptor agonist binding kinetics-role of a conserved serine residue
    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 ...
  • A dynamic view of molecular switch behavior at serotonin receptors: implications for functional selectivity
    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 ...
  • Electron paramagnetic resonance gives evidence for the presence of type 1 gonadotropin-releasing hormone receptor (GnRH-R) in subdomains of lipid rafts
    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 ...
  • Electronic sculpting of ligand-GPCR subtype selectivity: the case of angiotensin II
    Magnani, Francesca; Pappas, Charalampos G.; Crook, Tim; Magafa, Vassiliki; Cordopatis, Paul; Ishiguro, Susumu; Ohta, Naomi; Selent, Jana; Bosnyak, Sanja; Jones, Emma S.; Gerothanassis, Ioannis P.; Tamura, Masaaki; Widdop, Robert E.; Tzakos, Andreas G. (American Chemical Society (ACS), 2014)
    GPCR subtypes possess distinct functional and pharmacological profiles, and thus development of subtype-selective ligands has immense therapeutic potential. This is especially the case for the angiotensin receptor subtypes ...
  • Entrectinib-A SARS-CoV-2 inhibitor in Human Lung Tissue (HLT) cells
    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 ...
  • Fractal dimension as a measure of surface roughness of G protein-coupled receptors: implications for structure and function
    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 ...
  • G protein-specific mechanisms in the serotonin 5-HT2A receptor regulate psychosis-related effects and memory deficits
    Kossatz de Mello, Elk, 1977-; Diez Alarcia, Rebeca; Gaitonde, Supriya A.; Ramon Duaso, Carla, 1987-; Stepniewski, Tomasz Maciej, 1988-; Aranda García, David; Muneta Arrate, Itziar; Tepaz, Elodie; Saen-Oon, Suwipa; Soliva, Robert; Shahraki, Aida; Moreira, David; Brea, José; Loza, María I.; Torre Fornell, Rafael de la; Kolb, Peter; Bouvier, Michel; Meana, J. Javier; Robledo, Patricia, 1958-; Selent, Jana (Nature Research, 2024)
    G protein-coupled receptors (GPCRs) are sophisticated signaling machines able to simultaneously elicit multiple intracellular signaling pathways upon activation. Complete (in)activation of all pathways can be counterproductive ...
  • GPCRmd - A web platform for collection, visualization and analysis of molecular dynamics data for G protein-coupled receptors : Bridging the gap between dynamics and receptor functionality
    Rodríguez Espigares, Ismael (Universitat Pompeu Fabra, 2019-01-09)
    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 ...
  • How do molecular dynamics data complement static structural data of GPCRs
    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 ...
  • In silico study of allosteric communication networks in GPCR signaling bias
    Morales Pastor, Adrián; Nerín-Fonz, Francho; Aranda García, David; Dieguez-Eceolaza, Miguel; Medel Lacruz, Brian; Torrens Fontanals, Mariona; Peralta-Garcia, Alejandro; Selent, Jana (MDPI, 2002)
    Signaling bias is a promising characteristic of G protein-coupled receptors (GPCRs) as it provides the opportunity to develop more efficacious and safer drugs. This is because biased ligands can avoid the activation of ...

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