Listar por autoría "253767b8-c41c-4581-9cc9-11ab27c0e971"

Mostrando ítems 1-7 de 7

    • closedAccess   Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates 

      Royo, Santiago; Schirmeister, Tanja; Kaiser, Marcel; Jung, Sascha; Rodríguez, Santiago; Bautista, José Manuel; González, Florenci Elsevier (2018-09-01)
      A family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also ...

    • closedAccess   Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action 

      Royo Calvo, Santiago; Rodríguez, Santiago; Schirmeister, Tanja; Kesselring, Jochen; Kaiser, Marcel; González, Florenci Wiley (2015-07-14)
      Dipeptidyl enoates were prepared through a high-yielding two-step synthetic route. They have a dipeptidic structure with a 4-oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened ...

    • closedAccess   Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain 

      Latorre, Antonio; Schirmeister, Tanja; Kesselring, Jochen; Jung, Sascha; Johé, Patrick; Hellmich, Ute A.; Heilos, Anna; Engels, Bernd; Krauth-Siegel, R. Luise; Dirdjaja, Natalie; Bou Iserte, Lledó; Rodríguez, Santiago; González, Florenci American Chemical Society (2016)
      Dipeptidyl nitroalkenes are potent reversible inhibitors of cysteine proteases. Inhibitor 11 resulted to be the most potent one with Ki values of 0.49 and 0.44 nM against rhodesain and cruzain, respectively. According to ...

    • openAccess   Impact of the Recognition Part of Dipeptidyl Nitroalkene Compounds on the Inhibition Mechanism of Cysteine Proteases Cruzain and Cathepsin L 

      Arafet Cruz, Kemel; Royo, Santiago; Schirmeister, Tanja; Barthels, Fabian; González, Florenci; Moliner, Vicent American Chemical Society (2023-05-05)
      Cysteine proteases (CPs) are an important class of enzymes, many of which are responsible for several human diseases. For instance, cruzain of protozoan parasite Trypanosoma cruzi is responsible for the Chagas disease, ...

    • openAccess   Impact of the Warhead of Dipeptidyl Keto Michael Acceptors on the Inhibition Mechanism of Cysteine Protease Cathepsin L 

      Fernández de la Pradilla Ibáñez, Adrián; Royo, Santiago; Schirmeister, Tanja; Barthels, Fabian; Świderek, Katarzyna; González, Florenci; Moliner, Vicent American Chemical Society (2023-10-03)
      Cathepsin L (CatL) is a lysosomal cysteine protease whose activity has been related to several human pathologies. However, although preclinical trials using CatL inhibitors were promising, clinical trials have been ...

    • openAccess   Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors—A Comprehensive Reactivity and Selectivity Study 

      Müller, Patrick; Meta, Mergim; Meidner, Jan Laurenz; Schwickert, Marvin; Meyr, Jessica; Schwickert, Dr. Kevin; Kersten, Christian; Zimmer, Collin; Hammerschmidt, Stefan Josef; Frey, Ariane; Lahu, Albin; de la hoz rodriguez, Sergio; Agost Beltrán, Laura; Rodríguez, Santiago; Diemer, Kira; Neumann, Wilhelm; González, Florenci; Engels, Bernd; Schirmeister, Tanja MDPI (2023-04-13)
      : Covalent peptidomimetic protease inhibitors have gained a lot of attention in drug development in recent years. They are designed to covalently bind the catalytically active amino acids through electrophilic groups ...

    • openAccess   Peptidyl nitroalkene inhibitors of main protease rationalized by computational and crystallographic investigations as antivirals against SARS-CoV-2 

      Medrano Martin, Francisco Javier; de la hoz rodriguez, Sergio; Martí, Sergio; Arafet Cruz, Kemel; Schirmeister, Tanja; Hammerschmidt, Stefan Josef; Müller-Ruttloff, Christin; González-Martínez, Águeda; Santillana Heras, Elena; Ziebuhr, John; Romero Garrido, Antonio; Zimmer, Collin; Weldert, Annabelle Carolin; Zimmermann, Robert; Lodola, Alessio; Świderek, Katarzyna; Moliner, Vicent; González, Florenci Springer Nature (2024-01-18)
      The coronavirus disease 2019 (COVID-19) pandemic continues to represent a global public health issue. The viral main protease (Mpro) represents one of the most attractive targets for the development of antiviral drugs. ...