A clickable photoaffinity probe of betulinic acid identifies tropomyosin as a target

Autor: Pedro Martín-Acosta, Qianli Meng, John Klimek, Ashok P. Reddy, Larry David, Stefanie Kaech Petrie, Bingbing X. Li, Xiangshu Xiao

Publikováno v: Acta Pharmaceutica Sinica B, Vol 12, Iss 5, Pp 2406-2416 (2022)

Target identification of bioactive compounds is important for understanding their mechanisms of action and provides critical insights into their therapeutic utility. While it remains a challenge, unbiased chemoproteomics strategy using clickable phot

Externí odkaz: https://doaj.org/article/094330877cce40b48e305bfa2889fb14

Efficient Multicomponent Synthesis of Diverse Antibacterial Embelin-Privileged Structure Conjugates

Autor: Pedro Martín-Acosta, Rosalyn Peña, Gabriela Feresin, Alejandro Tapia, Isabel Lorenzo-Castrillejo, Félix Machín, Ángel Amesty, Ana Estévez-Braun

Publikováno v: Molecules, Vol 25, Iss 14, p 3290 (2020)

A library of embelin derivatives has been synthesized through a multicomponent reaction from embelin (1), aldehydes and privileged structures such as 4-hydroxycoumarin, 4-hydroxy-2H-pyran-2-one and 2-naphthol, in the presence of InCl3 as catalyst. Th

Externí odkaz: https://doaj.org/article/af48bab38d834f37a2f8b0503e07d072

JKST6, a novel multikinase modulator of the BCR-ABL1/STAT5 signaling pathway that potentiates direct BCR-ABL1 inhibition and overcomes imatinib resistance in chronic myelogenous leukemia

Autor: Juan M. Zapata, Ana Estévez-Braun, Juan Carlos Montero, Vanessa Junco, Yeray Brito-Casillas, Pedro Martín-Acosta, Leandro Fernández-Pérez, Borja Guerra, Ángel Amesty, Grant McNaughton-Smith, Javier León, Rosa M. Blanco, Atanasio Pandiella, Lucía Gandullo-Sánchez, Carlota Recio, Miguel Guerra-Rodríguez, Haidée Aranda-Tavío

Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
instname
Biomedicine & Pharmacotherapy Volume 144, December 2021, 112330
UCrea Repositorio Abierto de la Universidad de Cantabria
Universidad de Cantabria (UC)
Biomedicine & Pharmacotherapy, Vol 144, Iss, Pp 112330-(2021)

© 2021 The Author(s).
Chronic myelogenous leukemia (CML) is a hematological malignancy that highly depends on the BCR-ABL1/STAT5 signaling pathway for cell survival. First-line treatments for CML consist of tyrosine kinase inhibitors that effic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::319ebd870c378695880e0d7f956c7b16
http://hdl.handle.net/10261/261627

Modular Synthesis and Antiproliferative Activity of New Dihydro-1H-pyrazolo[1,3-b]pyridine Embelin Derivatives

Autor: Borja Guerra, Pedro Martín-Acosta, Leandro Fernández-Pérez, Ángel Amesty, Miguel Guerra-Rodríguez, Ana Estévez-Braun

Publikováno v: Pharmaceuticals, Vol 14, Iss 1026, p 1026 (2021)
Pharmaceuticals
Volume 14
Issue 10

A set of new dihydro-1H-pyrazolo[1,3-b]pyridine and pyrazolo[1,3-b]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds were evalu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::171b05aaf06e0179279c05b481a14965
https://doi.org/10.3390/ph14101026

PROTACs to address the challenges facing small molecule inhibitors

Autor: Pedro Martín-Acosta, Xiangshu Xiao

Publikováno v: Eur J Med Chem

Small molecule inhibitors of proteins represent important medicines and critical chemical tools to investigate the biology of the target proteins. Advances in various -omics technologies have fueled the pace of discovery of disease-relevant proteins.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ff32f290b9eb3db41352a7cb7186a0f
https://doi.org/10.1016/j.ejmech.2020.112993