Zobrazeno 1 - 10
of 38
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...
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
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
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
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
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
Autor:
Keith F. McDaniel, Carol K. Wada, Terrance J. Magoc, Warren M. Kati, Dachun Liu, Chaohong Sun, Lisa A. Hasvold, Le Wang, Robert A. Mantei, John K. Pratt, Yu Shen, Michael D. Wendt, T. Matthew Hansen, Charles W. Hutchins, Andrew M. Petros, Robin R. Frey, Denise Wilcox, Xiaoyu Lin, Chang H. Park, Rongqi Wang, Xiaoli Huang, Robert D. Hubbard, Peter Kovar, William J. McClellan, James H. Holms, George S. Sheppard, Leiming Li, Ganesh Rajaraman, Daniel H. Albert, Sanjay C. Panchal, Scott E. Warder, Steven D. Fidanze, Todd N. Soltwedel, Steven W. Elmore
Publikováno v:
Journal of medicinal chemistry. 60(9)
Members of the BET family of bromodomain containing proteins have been identified as potential targets for blocking proliferation in a variety of cancer cell lines. A two-dimensional NMR fragment screen for binders to the bromodomains of BRD4 identif