Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Francisco Javier Lopez-Tapia"'
Autor:
Weiliang Chen, Kayo Nakamura, Yinsong Zhu, Francisco Javier Lopez-Tapia, Casie Kubota, Wenzhen Fu, James Turkson, Felix Alonso-Valenteen, Lali K. Medina-Kauwe, Christine Brotherton-Pleiss, Jasmine Chen, Peibin Yue, Simoun Mikhael, Marcus A. Tius
Publikováno v:
Journal of Medicinal Chemistry
We optimized our previously reported proline-based STAT3 inhibitors into an exciting new series of (R)-azetidine-2-carboxamide analogues that have sub-micromolar potencies. 5a, 5o, and 8i have STAT3-inhibitory potencies (IC50) of 0.55, 0.38, and 0.34
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03e274d60b9b4117f5dee95ca2720723
https://pubmed.ncbi.nlm.nih.gov/33352047
https://pubmed.ncbi.nlm.nih.gov/33352047
Autor:
Anna Rabkin, Erin Ichinotsubo, Christine Brotherton-Pleiss, Raj Shah, Peibin Yue, Suzie Chen, Ana Carolina Costa Araujo, Megan J. Lantz, Marcus A. Tius, Francisco Javier Lopez-Tapia, Bruna Reis dos Santos, James Turkson, Heide Murakami
Publikováno v:
ACS Medicinal Chemistry Letters. 9:250-255
[Image: see text] The molecular determinants for the activities of the reported benzoic acid (SH4–54), salicylic acid (BP-1–102), and benzohydroxamic acid (SH5–07)-based STAT3 inhibitors were investigated to design optimized analogues. All thre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42dc83b839cb660a325c992dc7e0b879
https://doi.org/10.1021/acsmedchemlett.7b00544
https://doi.org/10.1021/acsmedchemlett.7b00544
Autor:
Felix Alonso-Valenteen, Wenzhen Fu, Yinsong Zhu, Francisco Javier Lopez-Tapia, Lali K. Medina-Kauwe, Christine Brotherton-Pleiss, Marcus A. Tius, James Turkson, Peibin Yue, Simoun Mikhael
Publikováno v:
Cancer Research. 81:1230-1230
Signal Transducer and Activator of Transcription (STAT)3 is a member of the STAT family of transcription factors that is frequently aberrantly-activated in breast cancer and many other cancers. STAT3 represents a valid target for the development of n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d4b0809922cd977eb5e5d1b0df28e708
https://doi.org/10.1158/1538-7445.am2021-1230
https://doi.org/10.1158/1538-7445.am2021-1230
Autor:
Rama K. Kondru, Sung-Sau So, Andreas Kuglstatter, Yan Lou, Francisco Javier Lopez-Tapia, Christine E. Brotherton-Pleiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(9)
A seven-membered cyclic chiral analog of potent lead BTK inhibitor 1 was envisioned by structure-based design to lock the molecule into its bioactive conformation. For the elaboration of the seven-membered ring, compound 1 pyridone 6-position was sub
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0cd98e01670ec9b018467c9ef23adc8
https://pubmed.ncbi.nlm.nih.gov/30857747
https://pubmed.ncbi.nlm.nih.gov/30857747
Autor:
Andrew T. Namanja, David Paladino, Francisco Javier Lopez-Tapia, Yifei Li, Peibin Yue, Chih-Hong Chen, James Turkson, Yuan Chen, Tyvette Hilliard, Marcus A. Tius
Publikováno v:
Cancer Research. 76:652-663
STAT3 offers an attractive target for cancer therapy, but small-molecule inhibitors with appealing pharmacologic properties have been elusive. Here, we report hydroxamic acid–based and benzoic acid–based inhibitors (SH5-07 and SH4-54, respectivel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10ecc9f6a6df195ea13184ca5bc0cbca
https://doi.org/10.1158/0008-5472.can-14-3558
https://doi.org/10.1158/0008-5472.can-14-3558
Autor:
Jasmine Chen, Peibin Yue, Marcus A. Tius, Francisco Javier Lopez-Tapia, Casie Kubota, Christine E. Brotherton-Pleiss, James Turkson
Publikováno v:
Cancer Research. 78:4880-4880
Constitutively-active Signal transducer and activator of transcription (STAT) 3 has been well validated as a significant mechanistic underpinning of many human cancers and a target for anticancer therapy. To date, no small molecule STAT3 inhibitor ha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::611e568120337e17a8fbb77e423d9af4
https://doi.org/10.1158/1538-7445.am2018-4880
https://doi.org/10.1158/1538-7445.am2018-4880
Autor:
Charles Alois Dvorak, Francisco Javier Lopez-Tapia, Xiaojun Huang, Brad Loe, Debra A. Cockayne, William L. Fitch, Scott Broadbent, Berger Jacob, Christine E. Brotherton-Pleiss, Keith A. M. Walker, Rebecca Suttmann, David L. Bourdet, Lee Edwin Lowrie, Shelley K. Gleason, Dov Nitzan, Paul J. Wagner, Jiang Zhu, Zhao Shu-Hai, Fernando Padilla, André Alker, Joanie Caroon, Deborah Phippard, Alam Jahangir, Pankaj D. Rege
Publikováno v:
Journal of medicinal chemistry. 58(21)
Identification of singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clinical candidates 17 and 19. During development, a number of issues were successfully addressed, such as metabolic stability, plasma st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e880f027ef8eadeaef6f8cc77b4f99c
https://pubmed.ncbi.nlm.nih.gov/26460788
https://pubmed.ncbi.nlm.nih.gov/26460788
Autor:
Mohammad R. Masjedizadeh, Lee Edwin Lowrie, Dov Nitzan, Pamela W. Berry, William L. Fitch, Aravamuthan Varadarajan, Ya-Ping Tu, Yanzhou Liu, Ali Tabatabaei, Francisco Javier Lopez-Tapia
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 32(12)
The metabolic fate of three aromatic carboxylic acid analogs under evaluation as prostaglandin I2-preferring receptor antagonists was studied. The initial analog with unsubstituted phenyl groups was subject to a complex set of aromatic oxidative biot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63aecd1ba426409dfb0f641e26819402
https://pubmed.ncbi.nlm.nih.gov/15371298
https://pubmed.ncbi.nlm.nih.gov/15371298