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Browsing by Author "Stepniewski, Tomasz Maciej, 1988-"

Browsing by Author "Stepniewski, Tomasz Maciej, 1988-"

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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), ...
  • 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 ...
  • Do they make a good match? Molecular dynamics studies on CALB-catalyzed esterification of 3-phenylpropionic and cinnamic acids
    Zieniuk, Bartlomiej; Stepniewski, Tomasz Maciej, 1988-; Fabiszewska, Agata (Elsevier, 2023)
    Lipases are versatile catalysts widely used in industrial biotransformations and laboratory-scale developed reactions with industrial potential. Despite the fact that lipase B from Candida antarctica (CALB) is one of 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 ...
  • 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 ...
  • 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 ...
  • 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 ...
  • Ligand entry pathways control the chemical space recognized by GPR183
    Kjaer, Viktoria Madeline Skovgaard; Stepniewski, Tomasz Maciej, 1988-; Medel Lacruz, Brian; Reinmuth, Lisa; Ciba, Marija; Rexen Ulven, Elisabeth; Bonomi, Massimiliano; Selent, Jana; Rosenkilde, Mette Marie (Royal Society of Chemistry, 2023)
    The G protein-coupled receptor GPR183 is a chemotactic receptor with an important function in the immune system and association with a variety of diseases. It recognizes ligands with diverse physicochemical properties as ...
  • Ligand with two modes of interaction with the dopamine D2 receptor-an induced-fit mechanism of insurmountable antagonism
    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) ...
  • Mechanistic insights into dopaminergic and serotonergic neurotransmission - concerted interactions with helices 5 and 6 drive the functional outcome
    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 ...
  • Oxazoline scaffold in synthesis of benzosiloxaboroles and related ring-expanded heterocycles: diverse reactivity, structural peculiarities and antimicrobial activity
    Krajewska, Joanna; Nowicki, Krzysztof; Durka, Krzysztof; Marek-Urban, Paulina H.; Wińska, Patrycja; Stepniewski, Tomasz Maciej, 1988-; Woźniak, Krzysztof; Laudy, Agnieszka E.; Luliński, Sergiusz (Royal Society of Chemistry, 2022)
    Two isomeric benzosiloxaborole derivatives 3a and 5a bearing fluorine and 4,4-dimethyl-2-oxazolin-2-yl substituents attached to the aromatic rings were obtained. Both compounds were prone to hydrolytic cleavage of the ...
  • Plasma membrane preassociation drives β-arrestin coupling to receptors and activation
    Grimes, Jak; Koszegi, Zsombor; Lanoiselée, Yann; Miljus, Tamara; O'Brien, Shannon L.; Stepniewski, Tomasz Maciej, 1988-; Medel Lacruz, Brian; Baidya, Mithu; Makarova, Maria; Mistry, Ravi; Goulding, Joëlle; Drube, Julia; Hoffmann, Carsten; Owen, Dylan M.; Shukla, Arun K.; Selent, Jana; Hill, Stephen J.; Calebiro, Davide (Elsevier, 2023)
    β-arrestin plays a key role in G protein-coupled receptor (GPCR) signaling and desensitization. Despite recent structural advances, the mechanisms that govern receptor-β-arrestin interactions at the plasma membrane of ...

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