2-Aryladenine Derivatives as a Potent Scaffold for Adenosine Receptor Antagonists: The 6-Morpholino Derivatives

Autor: Filipe Areias, Carla Correia, Ashly Rocha, Sofia Teixeira, Marián Castro, Jose Brea, Huabin Hu, Jens Carlsson, Maria I. Loza, M. Fernanda Proença, M. Alice Carvalho

Publikováno v: Molecules, Vol 29, Iss 11, p 2543 (2024)

A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A1, A2A, A2B, and A3 adenosine receptor subtypes. Eleven purines showed potent antagonism at A1, A3, dual A1/A2A, A1/

Externí odkaz: https://doaj.org/article/7cbea8944ba641e096dee5b96a2e909e

Pharmacology and preclinical validation of a novel anticancer compound targeting PEPCK-M

Autor: Marc Aragó, Juan Moreno-Felici, Sonia Abás, Sergio Rodríguez-Arévalo, Petra Hyroššová, Agnes Figueras, Francesc Viñals, Belén Pérez, Maria I. Loza, Jose Brea, Pedro Latorre, Jose A. Carrodeguas, Pablo M. García-Rovés, Carlos Galdeano, Tiziana Ginex, Francisco J. Luque, Carmen Escolano, Jose C. Perales

Publikováno v: Biomedicine & Pharmacotherapy, Vol 121, Iss , Pp 109601- (2020)

Background: Phosphoenolpyruvate carboxykinase (PEPCK) catalyzes the decarboxylation of oxaloacetate to phosphoenolpyruvate. The mitochondrial isozyme, PEPCK-M is highly expressed in cancer cells, where it plays a role in nutrient stress response. To

Externí odkaz: https://doaj.org/article/4129df432cec43aeb4c51f46efffb0d1

A Novel NMDA Receptor Antagonist Protects against Cognitive Decline Presented by Senescent Mice

Autor: Júlia Companys-Alemany, Andreea L. Turcu, Aina Bellver-Sanchis, Maria I Loza, José M. Brea, Anna M Canudas, Rosana Leiva, Santiago Vázquez, Mercè Pallàs, Christian Griñán-Ferré

Publikováno v: Pharmaceutics, Vol 12, Iss 3, p 284 (2020)

Alzheimer’s disease (AD) is the leading cause of dementia. Non-competitive N-Methyl-D-aspartate (NMDA) receptor antagonist memantine improved cognition and molecular alterations after preclinical treatment. Nevertheless, clinical results are discou

Externí odkaz: https://doaj.org/article/506b5a2b20f3415e94f82e042797ec90

Multitarget Derivatives of D2AAK1 as Potential Antipsychotics: The Effect of Substitution in the Indole Moiety

Autor: Magda Kondej, Tomasz M. Wróbel, Katarzyna M. Targowska‐Duda, Antón Leandro Martínez, Oliwia Koszła, Piotr Stępnicki, Agata Zięba, Alba Paz, Olga Wronikowska‐Denysiuk, Maria I. Loza, Marián Castro, Agnieszka A. Kaczor

Publikováno v: ChemMedChem. 17(15)

Schizophrenia is a complex disease which is best treated with multitarget drugs, such as atypical antipsychotics. Previously, using structure-based virtual screening, we found a virtual hit, D2AAK1, with nanomolar affinity for dopamine and serotonin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::908ffba47a25c42b6a5da41d22c2def5
https://pubmed.ncbi.nlm.nih.gov/35610178

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.

Autor: Wesley C Van Voorhis, John H Adams, Roberto Adelfio, Vida Ahyong, Myles H Akabas, Pietro Alano, Aintzane Alday, Yesmalie Alemán Resto, Aishah Alsibaee, Ainhoa Alzualde, Katherine T Andrews, Simon V Avery, Vicky M Avery, Lawrence Ayong, Mark Baker, Stephen Baker, Choukri Ben Mamoun, Sangeeta Bhatia, Quentin Bickle, Lotfi Bounaadja, Tana Bowling, Jürgen Bosch, Lauren E Boucher, Fabrice F Boyom, Jose Brea, Marian Brennan, Audrey Burton, Conor R Caffrey, Grazia Camarda, Manuela Carrasquilla, Dee Carter, Maria Belen Cassera, Ken Chih-Chien Cheng, Worathad Chindaudomsate, Anthony Chubb, Beatrice L Colon, Daisy D Colón-López, Yolanda Corbett, Gregory J Crowther, Noemi Cowan, Sarah D'Alessandro, Na Le Dang, Michael Delves, Joseph L DeRisi, Alan Y Du, Sandra Duffy, Shimaa Abd El-Salam El-Sayed, Michael T Ferdig, José A Fernández Robledo, David A Fidock, Isabelle Florent, Patrick V T Fokou, Ani Galstian, Francisco Javier Gamo, Suzanne Gokool, Ben Gold, Todd Golub, Gregory M Goldgof, Rajarshi Guha, W Armand Guiguemde, Nil Gural, R Kiplin Guy, Michael A E Hansen, Kirsten K Hanson, Andrew Hemphill, Rob Hooft van Huijsduijnen, Takaaki Horii, Paul Horrocks, Tyler B Hughes, Christopher Huston, Ikuo Igarashi, Katrin Ingram-Sieber, Maurice A Itoe, Ajit Jadhav, Amornrat Naranuntarat Jensen, Laran T Jensen, Rays H Y Jiang, Annette Kaiser, Jennifer Keiser, Thomas Ketas, Sebastien Kicka, Sunyoung Kim, Kiaran Kirk, Vidya P Kumar, Dennis E Kyle, Maria Jose Lafuente, Scott Landfear, Nathan Lee, Sukjun Lee, Adele M Lehane, Fengwu Li, David Little, Liqiong Liu, Manuel Llinás, Maria I Loza, Aristea Lubar, Leonardo Lucantoni, Isabelle Lucet, Louis Maes, Dalu Mancama, Nuha R Mansour, Sandra March, Sheena McGowan, Iset Medina Vera, Stephan Meister, Luke Mercer, Jordi Mestres, Alvine N Mfopa, Raj N Misra, Seunghyun Moon, John P Moore, Francielly Morais Rodrigues da Costa, Joachim Müller, Arantza Muriana, Stephen Nakazawa Hewitt, Bakela Nare, Carl Nathan, Nathalie Narraidoo, Sujeevi Nawaratna, Kayode K Ojo, Diana Ortiz, Gordana Panic, George Papadatos, Silvia Parapini, Kailash Patra, Ngoc Pham, Sarah Prats, David M Plouffe, Sally-Ann Poulsen, Anupam Pradhan, Celia Quevedo, Ronald J Quinn, Christopher A Rice, Mohamed Abdo Rizk, Andrea Ruecker, Robert St Onge, Rafaela Salgado Ferreira, Jasmeet Samra, Natalie G Robinett, Ulrich Schlecht, Marjorie Schmitt, Filipe Silva Villela, Francesco Silvestrini, Robert Sinden, Dennis A Smith, Thierry Soldati, Andreas Spitzmüller, Serge Maximilian Stamm, David J Sullivan, William Sullivan, Sundari Suresh, Brian M Suzuki, Yo Suzuki, S Joshua Swamidass, Donatella Taramelli, Lauve R Y Tchokouaha, Anjo Theron, David Thomas, Kathryn F Tonissen, Simon Townson, Abhai K Tripathi, Valentin Trofimov, Kenneth O Udenze, Imran Ullah, Cindy Vallieres, Edgar Vigil, Joseph M Vinetz, Phat Voong Vinh, Hoan Vu, Nao-Aki Watanabe, Kate Weatherby, Pamela M White, Andrew F Wilks, Elizabeth A Winzeler, Edward Wojcik, Melanie Wree, Wesley Wu, Naoaki Yokoyama, Paul H A Zollo, Nada Abla, Benjamin Blasco, Jeremy Burrows, Benoît Laleu, Didier Leroy, Thomas Spangenberg, Timothy Wells, Paul A Willis

Publikováno v: PLoS Pathogens, Vol 12, Iss 7, p e1005763 (2016)

A major cause of the paucity of new starting points for drug discovery is the lack of interaction between academia and industry. Much of the global resource in biology is present in universities, whereas the focus of medicinal chemistry is still larg

Externí odkaz: https://doaj.org/article/18b88a00726d44659ebd19c6f7c84d1b