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Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.
Ortega-Molina A, Lopez-Guadamillas E, Mattison JA, Mitchell SJ, Muñoz-Martin M, Iglesias G, Gutierrez VM, Vaughan KL, Szarowicz MD, González-García I, López M, Cebrián D, Martinez S, Pastor J, de Cabo R, Serrano M. Ortega-Molina A, et al. Among authors: pastor j. Cell Metab. 2015 Apr 7;21(4):558-70. doi: 10.1016/j.cmet.2015.02.017. Epub 2015 Mar 26. Cell Metab. 2015. PMID: 25817535 Free PMC article.
Pten positively regulates brown adipose function, energy expenditure, and longevity.
Ortega-Molina A, Efeyan A, Lopez-Guadamillas E, Muñoz-Martin M, Gómez-López G, Cañamero M, Mulero F, Pastor J, Martinez S, Romanos E, Mar Gonzalez-Barroso M, Rial E, Valverde AM, Bischoff JR, Serrano M. Ortega-Molina A, et al. Among authors: pastor j. Cell Metab. 2012 Mar 7;15(3):382-94. doi: 10.1016/j.cmet.2012.02.001. Cell Metab. 2012. PMID: 22405073 Free article.
PI3Kα inhibition reduces obesity in mice.
Lopez-Guadamillas E, Muñoz-Martin M, Martinez S, Pastor J, Fernandez-Marcos PJ, Serrano M. Lopez-Guadamillas E, et al. Among authors: pastor j. Aging (Albany NY). 2016 Nov 4;8(11):2747-2753. doi: 10.18632/aging.101075. Aging (Albany NY). 2016. PMID: 27816049 Free PMC article.
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.
Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J. Martínez González S, et al. Among authors: pastor j. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. doi: 10.1016/j.bmcl.2012.03.090. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22520259
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.
Martínez González S, Rodríguez-Arístegui S, Hernández AI, Varela C, González Cantalapiedra E, Álvarez RM, Rodríguez Hergueta A, Bischoff JR, Albarrán MI, Cebriá A, Cendón E, Cebrián D, Alfonso P, Pastor J. Martínez González S, et al. Among authors: pastor j. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2536-2543. doi: 10.1016/j.bmcl.2017.03.090. Epub 2017 Apr 2. Bioorg Med Chem Lett. 2017. PMID: 28404374
Identification of novel PI3K inhibitors through a scaffold hopping strategy.
Martínez González S, Hernández AI, Álvarez RM, Rodríguez A, Ramos-Lima F, Bischoff JR, Albarrán MI, Cebriá A, Hernández-Encinas E, García-Arocha J, Cebrián D, Blanco-Aparicio C, Pastor J. Martínez González S, et al. Among authors: pastor j. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4794-4799. doi: 10.1016/j.bmcl.2017.09.059. Epub 2017 Sep 30. Bioorg Med Chem Lett. 2017. PMID: 29017786
Global hyperactivation of enhancers stabilizes human and mouse naive pluripotency through inhibition of CDK8/19 Mediator kinases.
Lynch CJ, Bernad R, Martínez-Val A, Shahbazi MN, Nóbrega-Pereira S, Calvo I, Blanco-Aparicio C, Tarantino C, Garreta E, Richart-Ginés L, Alcazar N, Graña-Castro O, Gómez-Lopez G, Aksoy I, Muñoz-Martín M, Martinez S, Ortega S, Prieto S, Simboeck E, Camasses A, Stephan-Otto Attolini C, Fernandez AF, Sierra MI, Fraga MF, Pastor J, Fisher D, Montserrat N, Savatier P, Muñoz J, Zernicka-Goetz M, Serrano M. Lynch CJ, et al. Among authors: pastor j. Nat Cell Biol. 2020 Oct;22(10):1223-1238. doi: 10.1038/s41556-020-0573-1. Epub 2020 Sep 28. Nat Cell Biol. 2020. PMID: 32989249 Free article.
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.
Martínez González S, Hernández AI, Varela C, Lorenzo M, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán MI, Alfonso P, García-Serelde B, Mateos G, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Blanco-Aparicio C, Pastor J. Martínez González S, et al. Among authors: pastor j. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5208-14. doi: 10.1016/j.bmcl.2012.06.093. Epub 2012 Jul 4. Bioorg Med Chem Lett. 2012. PMID: 22819764
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.
Álvarez RM, García AB, Riesco-Fagundo C, Martín JI, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Oyarzabal J, Di Geronimo B, Lorenzo M, Albarrán MI, Cebriá A, Cebrián D, Martínez-González S, Blanco-Aparicio C, Pastor J. Álvarez RM, et al. Among authors: pastor j. Eur J Med Chem. 2021 Feb 5;211:113109. doi: 10.1016/j.ejmech.2020.113109. Epub 2020 Dec 18. Eur J Med Chem. 2021. PMID: 33360802
923 results