Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Lisa A, Hasvold"'
Autor:
Jonas A. Nilsson, Ulrich Keller, Viktoriya Nikolova, Martina Rudelius, Philip Merta, Lisa A. Hasvold, Somsundar Veppil Muralidharan, Lisa M. Nilsson, Andreas Höglund
PDF file - 1.2MB
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19fc80b42aa4c6ebb0d7402d304386cc
https://doi.org/10.1158/1078-0432.22444460
https://doi.org/10.1158/1078-0432.22444460
Autor:
Jonas A. Nilsson, Ulrich Keller, Viktoriya Nikolova, Martina Rudelius, Philip Merta, Lisa A. Hasvold, Somsundar Veppil Muralidharan, Lisa M. Nilsson, Andreas Höglund
Purpose: The transcription factor c-Myc (or “Myc”) is a master regulator of pathways driving cell growth and proliferation. MYC is deregulated in many human cancers, making its downstream target genes attractive candidates for drug development. W
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08d10dff437781d8413b6e25e4fcdfc7
https://doi.org/10.1158/1078-0432.c.6520178.v1
https://doi.org/10.1158/1078-0432.c.6520178.v1
Autor:
Jonas A. Nilsson, Ulrich Keller, Viktoriya Nikolova, Martina Rudelius, Philip Merta, Lisa A. Hasvold, Somsundar Veppil Muralidharan, Lisa M. Nilsson, Andreas Höglund
PDF file - 116K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4267dd01be9c87a7cd208c03bc3ed243
https://doi.org/10.1158/1078-0432.22444457
https://doi.org/10.1158/1078-0432.22444457
Autor:
Daniel H. Albert, Wei Qiu, Chang H. Park, Steven D. Fidanze, Lisa A. Hasvold, Maricel Torrent, Ganesh Rajaraman, Xiaoli Huang, Peter Kovar, Keith F. McDaniel, Xiaoyu Lin, George S. Sheppard, Le Wang, John K. Pratt, Lu Zhang, Mai Bui, Yu Shen, Kenton L. Longenecker, Warren M. Kati, Dachun Liu, Denise Wilcox, Terrance J. Magoc, Emily J. Faivre
Publikováno v:
Journal of Medicinal Chemistry. 63:5585-5623
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under clinical development for on...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a13664ab18da232a44d2b0a2ef1e6c65
https://doi.org/10.1021/acs.jmedchem.0c00628
https://doi.org/10.1021/acs.jmedchem.0c00628
Autor:
Denise Wilcox, Vasudha Sehgal, Daniel H. Albert, John K. Pratt, Keith F. McDaniel, Xin Lu, Chaohong Sun, Dachun Liu, Joshua P. Plotnik, Srinivasa R. Mantena, Emily J. Faivre, Lisa A. Hasvold, George S. Sheppard, Xiaoli Huang, Le Wang, Lance J Bigelow, Stacey Fossey, Steve D. Fidanze, Lloyd T. Lam, Chang H. Park, Sanjay C. Panchal, Warren M. Kati, John J. Nicolette, Richard J. Bellin, Gaurav Mehta, Xiaoyu Lin, Mai H. Bui, Lu Zhang, Paul Hessler, Maricel Torrent, Tamar Uziel, Saul H. Rosenberg, Yu Shen, Kenton L. Longenecker
Publikováno v:
Nature. 578:306-310
Proteins of the bromodomain and extra-terminal (BET) domain family are epigenetic readers that bind acetylated histones through their bromodomains to regulate gene transcription. Dual-bromodomain BET inhibitors (DbBi) that bind with similar affinitie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8040bf69aa34810391b9a59139a83026
https://doi.org/10.1038/s41586-020-1930-8
https://doi.org/10.1038/s41586-020-1930-8
Autor:
George S, Sheppard, Le, Wang, Steven D, Fidanze, Lisa A, Hasvold, Dachun, Liu, John K, Pratt, Chang H, Park, Kenton, Longenecker, Wei, Qiu, Maricel, Torrent, Peter J, Kovar, Mai, Bui, Emily, Faivre, Xiaoli, Huang, Xiaoyu, Lin, Denise, Wilcox, Lu, Zhang, Yu, Shen, Daniel H, Albert, Terrance J, Magoc, Ganesh, Rajaraman, Warren M, Kati, Keith F, McDaniel
Publikováno v:
Journal of medicinal chemistry. 63(10)
The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain inhibitors under clinical development for oncology bind to each of the eight bromodomains with si
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::283055280d03954bedb827a07dda077b
https://pubmed.ncbi.nlm.nih.gov/32324999
https://pubmed.ncbi.nlm.nih.gov/32324999
Autor:
Keith F. McDaniel, Andrew Bogdan, Lisa A. Hasvold, Ana L. Aguirre, Denise Wilcox, Xiaoyu Lin, Le Wang, Mai H. Bui, Leiming Li, Warren M. Kati, Terrance J. Magoc, James H. Holms, Dachun Liu, Steven D. Fidanze, Justin D. Dietrich, Charles W. Hutchins, Ganesh Rajaraman, Yu Shen, George S. Sheppard, Rongqi Wang, Daniel H. Albert, Chang H. Park, Jasmina Marjanovic, Robert A. Mantei, Xiaoli Huang, Peter Kovar, Yujia Dai, John K. Pratt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1804-1810
Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]py
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec20af598ffa68abcb2f81c612b36b03
https://doi.org/10.1016/j.bmcl.2018.04.020
https://doi.org/10.1016/j.bmcl.2018.04.020
Autor:
Ganesh Rajaraman, Leiming Li, Daniel H. Albert, Ruth L. Martin, Terrance J. Magoc, Todd N. Soltwedel, Denise Wilcox, Xiaoli Huang, Chang H. Park, Steven W. Elmore, George S. Sheppard, Charles W. Hutchins, Dachun Liu, Chaohong C. Sun, Guowei Fang, Le Wang, Wenqing Gao, Robert A. Mantei, Rongqi Wang, Emily J. Faivre, Steven D. Fidanze, John K. Pratt, Xiaoyu Lin, Mai H. Bui, Shekman Wong, Scott E. Warder, Jianwei J. Shen, Rohinton P. Edalji, Lisa A. Hasvold, Warren M. Kati, Keith F. McDaniel, Yu Shen
Publikováno v:
Journal of Medicinal Chemistry. 60:8369-8384
The development of bromodomain and extraterminal domain (BET) bromodomain inhibitors and their examination in clinical studies, particularly in oncology settings, has garnered substantial recent interest. An effort to generate novel BET bromodomain i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e212dfdec3c29433c5f0baac7f9a9a8
https://doi.org/10.1021/acs.jmedchem.7b00746
https://doi.org/10.1021/acs.jmedchem.7b00746
Autor:
Xiaoli Huang, Lisa A. Hasvold, Guowei Fang, Yu Shen, Denise Wilcox, Cherrie K. Donawho, George S. Sheppard, Le Wang, Fred Kohlhapp, Dachun Liu, Tamar Uziel, Leiming Li, Lloyd T. Lam, Daniel H. Albert, Scott E. Warder, Steven W. Elmore, Saul H. Rosenberg, Xiaoyu Lin, Xin Lu, Mai H. Bui, Keith F. McDaniel, Warren M. Kati, Emily J. Faivre, John K. Pratt, Steve D. Fidanze
Publikováno v:
Cancer Research. 77:2976-2989
ABBV-075 is a potent and selective BET family bromodomain inhibitor that recently entered phase I clinical trials. Comprehensive preclinical characterization of ABBV-075 demonstrated broad activity across cell lines and tumor models, representing a v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acae2c64a94df696b6140f0499202c00
https://doi.org/10.1158/0008-5472.can-16-1793
https://doi.org/10.1158/0008-5472.can-16-1793
Autor:
Chang H. Park, Ganesh Rajaraman, George S. Sheppard, Lisa A. Hasvold, Warren M. Kati, Yu Shen, Le Wang, Emily J. Faivre, Terrance J. Magoc, Xiaoyu Lin, Mai-Ha Bui, John K. Pratt, Denise Wilcox, Steven D. Fidanze, Dachun Liu, Keith F. McDaniel, Xiaoli Huang, Daniel H. Albert
Publikováno v:
Cancer Research. 78:931-931
The BET family of proteins consists of BRD2, BRD3, BRD4 and BRDT, with each of these proteins containing two distinct bromodomains (BDI and BDII). ABBV-075, like other first generation BET family bromodomain inhibitors currently under clinical develo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3b962f2650d627d9a223c21bf4a53149
https://doi.org/10.1158/1538-7445.am2018-931
https://doi.org/10.1158/1538-7445.am2018-931