Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Saul Jaime-Figueroa"'
Autor:
Shanique Alabi, Saul Jaime-Figueroa, Zhan Yao, Yijun Gao, John Hines, Kusal T. G. Samarasinghe, Lea Vogt, Neal Rosen, Craig M. Crews
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without a
Externí odkaz:
https://doaj.org/article/c199e2f0eb92437a873d93ab5b38d197
Autor:
Blake E. Smith, Stephen L. Wang, Saul Jaime-Figueroa, Alicia Harbin, Jing Wang, Brian D. Hamman, Craig M. Crews
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-13 (2019)
PROTACs enable targeted protein degradation by recruiting an E3 ligase to a specific substrate but the determinants of selectivity are not fully understood. Here, the authors show that varying the linker between warhead and E3 ligand and the orientat
Externí odkaz:
https://doaj.org/article/86ec9e4d91cb498bb96bd2e90667c3f4
Autor:
Angela Gong, Elvira An, Ifunanya Okeke, Saul Jaime-Figueroa, Zhenyi Hu, Xuanmeng Luo, Craig M. Crews, Po-Han Chen, Sijin Zheng
Publikováno v:
ACS Chemical Biology. 16:2808-2815
Protein phosphorylation, which regulates many critical aspects of cell biology, is dynamically governed by kinases and phosphatases. Many diseases are associated with dysregulated hyperphosphorylation of critical proteins, such as retinoblastoma prot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aca764cba778dec380dbf914866475a
https://doi.org/10.1021/acschembio.1c00693
https://doi.org/10.1021/acschembio.1c00693
Publikováno v:
The Journal of Organic Chemistry. 86:8479-8488
A novel, facile, and expeditious two-step synthesis of 3,4-unsubstituted isoquinolin-1(2H)-ones from a Suzuki cross-coupling between 2-halobenzonitriles and commercially available vinyl boronates followed by platinum-catalyzed nitrile hydrolysis and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20fe3270fc6b4953c1a7fc3963f733a0
https://doi.org/10.1021/acs.joc.1c00472
https://doi.org/10.1021/acs.joc.1c00472
Autor:
Scott A. Holley, Dhanusha A. Nalawansha, Michael Burgess, Adrian Bebenek, Katherine Dai, Craig M. Crews, Kusal T. G. Samarasinghe, Zhenyi Hu, Saul Jaime-Figueroa
Publikováno v:
Cell chemical biology. 28(5)
Summary Many diseases, including cancer, stem from aberrant activation or overexpression of oncoproteins that are associated with multiple signaling pathways. Although proteins with catalytic activity can be successfully drugged, the majority of othe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa8ae56ee08aeeac035e141b0184c864
https://pubmed.ncbi.nlm.nih.gov/34019844
https://pubmed.ncbi.nlm.nih.gov/34019844
Autor:
Craig M. Crews, Neal Rosen, Yijun Gao, John Hines, Zhan Yao, Kusal T. G. Samarasinghe, Shanique Alabi, Saul Jaime-Figueroa, Lea Vogt
Publikováno v:
Nature Communications
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Nature Communications, Vol 12, Iss 1, Pp 1-11 (2021)
Over 300 BRAF missense mutations have been identified in patients, yet currently approved drugs target V600 mutants alone. Moreover, acquired resistance inevitably emerges, primarily due to RAF lesions that prevent inhibition of BRAF V600 with curren
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1c111d9b909a29cba6e4517c0f5003c
https://doi.org/10.1038/s41467-021-21159-7
https://doi.org/10.1038/s41467-021-21159-7
Many diseases, including cancer, stem from aberrant activation and overexpression of oncoproteins that are associated with multiple signaling pathways. Although proteins with catalytic activity are able to be successfully drugged, the majority of oth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::20ab926ca181a13ab91a03611d480d73
https://doi.org/10.1101/2020.10.12.336529
https://doi.org/10.1101/2020.10.12.336529
Autor:
Haley A Armstrong, Craig M. Crews, Alexandru D. Buhimschi, Saul Jaime-Figueroa, Momar Toure, Timothy L. Chen, Jennifer A. Woyach, Amy Lehman, Amy J. Johnson, John C. Byrd
Publikováno v:
Biochemistry. 57:3564-3575
Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies, yet80% of CLL patients develop
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::591251ba5184e539c5c75d96d5e41bf9
https://doi.org/10.1021/acs.biochem.8b00391
https://doi.org/10.1021/acs.biochem.8b00391
Autor:
Brian D. Hamman, Saul Jaime-Figueroa, Craig M. Crews, Stephen Wang, Alicia Harbin, Blake E. Smith, Jing Wang
Publikováno v:
Nature Communications, Vol 10, Iss 1, Pp 1-13 (2019)
Nature Communications
Nature Communications
PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted degradation. Many potent PROTACs with specificity for dissimilar targets have been d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7e506ced6541a3d88c66773ed98e47f
https://doi.org/10.1038/s41467-018-08027-7
https://doi.org/10.1038/s41467-018-08027-7
Publikováno v:
European Journal of Organic Chemistry. 2016:4171-4175
An innovative and simple expeditious synthesis of 3,4-unsubstituted isoquinolones and isocoumarins starting from safe and easy to handle two-carbon acetylene equivalent was developed. The synthetic potential of this new method was further demonstrate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec8d257f53ff21e0f909b8fb4f17b697
https://doi.org/10.1002/ejoc.201600575
https://doi.org/10.1002/ejoc.201600575