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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 ...
  • 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 ...
  • 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 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 ...
  • Unraveling the complex signaling behavior of neurotransmitters and their receptors in the brain
    Stepniewski, Tomasz Maciej, 1988- (Universitat Pompeu Fabra, 2020-01-09)
    G protein-coupled receptors (GPCRs) are the main acceptors of neurotransmitters, and thus play an important role in communication between neurons. Because of this they are an attractive drug target for multiple neurodegenerative ...