Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Gilles, Carmel"'
Autor:
Yoshitaka Satoh, Gilles Carmel, Frans Baculi, Peter H. Schafer, Laurie LeBrun, Matt Hickman, Thomas O. Daniel, Brian E. Cathers, James Carmichael, Godrej Khambatta, Hon-Wah Man, Mary E Matyskiela, Philip P Chamberlain, Weihong Zhang, Mariko Riley, George W. Muller, Barbra Pagarigan, Gang Lu, Chin-Chun Lu
Publikováno v:
Journal of Medicinal Chemistry. 61:535-542
The drugs lenalidomide and pomalidomide bind to the protein cereblon, directing the CRL4-CRBN E3 ligase toward the transcription factors Ikaros and Aiolos to cause their ubiquitination and degradation. Here we describe CC-220 (compound 6), a cereblon
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba3ec7b8486c677242241f929022984b
https://doi.org/10.1021/acs.jmedchem.6b01921
https://doi.org/10.1021/acs.jmedchem.6b01921
Autor:
Kevin Ronald Condroski, Matt Hickman, Wei Liu, Laurie LeBrun, Gilles Carmel, Joshua Hansen, Gang Lu, Afshin Mahmoudi, Frans Baculi, Correa Matthew D, Tim Crea, Hon-Wah Man, George W. Muller, Chin-Chun Lu, Alexander L. Ruchelman, Fan Vocanson, Weihong Zhang
Publikováno v:
Journal of Medicinal Chemistry. 61:492-503
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure–activity relationships for analogs of 3 with exploration of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::82b447b68c060eec6fd08bffe825f2a7
https://doi.org/10.1021/acs.jmedchem.6b01911
https://doi.org/10.1021/acs.jmedchem.6b01911
Autor:
Alexander L. Ruchelman, Jack Houston, Nai-Yu Wang, Lyn'Al Nosaka, Antonia Lopez-Girona, Takumi Ito, Gilles Carmel, Mary E Matyskiela, Wei Fang, Derek Nguyen, Philip P Chamberlain, Thomas O. Daniel, Karen Miller, Chin-Chun Lu, Barbra Pagarigan, Svetlana Gaidarova, Gang Lu, Shuichan Xu, James Carmichael, Tam Tran, Gabriel C. Lander, Mariko Riley, Brian E. Cathers, Hiroshi Handa
Publikováno v:
Nature. 535:252-257
Immunomodulatory drugs bind to cereblon (CRBN) to confer differentiated substrate specificity on the CRL4(CRBN) E3 ubiquitin ligase. Here we report the identification of a new cereblon modulator, CC-885, with potent anti-tumour activity. The anti-tum
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91e627c880e58840f87057e76f90aa5d
https://doi.org/10.1038/nature18611
https://doi.org/10.1038/nature18611
Autor:
Joshua D, Hansen, Kevin, Condroski, Matthew, Correa, George, Muller, Hon-Wah, Man, Alexander, Ruchelman, Weihong, Zhang, Fan, Vocanson, Tim, Crea, Wei, Liu, Gang, Lu, Frans, Baculi, Laurie, LeBrun, Afshin, Mahmoudi, Gilles, Carmel, Matt, Hickman, Chin-Chun, Lu
Publikováno v:
Journal of medicinal chemistry. 61(2)
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure-activity relationships for analogs of 3 with exploration of the st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::f8916d455404142030cbeb1a6662660c
https://pubmed.ncbi.nlm.nih.gov/28358507
https://pubmed.ncbi.nlm.nih.gov/28358507
Autor:
Philip P Chamberlain, Maria Wang, Yoshinori Hirano, Brian E. Cathers, Gilles Carmel, Toshio Hakoshima, Hiroshi Handa, Barbra Pagarigan, Emily Rychak, Yan J Ren, Barbara Chie-Leon, Silvia L. Delker, Laura G. Corral, Tomoyuki Mori, Takumi Ito, Thomas O. Daniel, Antonia Lopez-Girona, Karen Miller, Hideki Ando, Mariko Riley
Publikováno v:
Nature Structural & Molecular Biology. 21:803-809
The Cul4-Rbx1-DDB1-Cereblon E3 ubiquitin ligase complex is the target of thalidomide, lenalidomide and pomalidomide, therapeutically important drugs for multiple myeloma and other B-cell malignancies. These drugs directly bind Cereblon (CRBN) and pro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b131abf0f427feaba8ec6b36dad4572
https://doi.org/10.1038/nsmb.2874
https://doi.org/10.1038/nsmb.2874
Autor:
Gengxin Chen, Yan Ren, Anita Gandhi, Peter H. Schafer, Michelle Waldman, Emily Rychak, Antonia Lopez-Girona, Mahan Abbasian, Derek Mendy, Rajesh Chopra, Thomas O. Daniel, Pilgrim Jackson, Anjan Thakurta, Michael Breider, Gilles Carmel, Afshin Mahmoudi, Svetlana Gaidarova, Maria Wang, Brian E. Cathers, Karen Miller
Publikováno v:
British Journal of Haematology
Cereblon, a member of the cullin 4 ring ligase complex (CRL4), is the molecular target of the immunomodulatory drugs (IMiDs) lenalidomide and pomalidomide and is required for the antiproliferative activity of these agents in multiple myeloma (MM) and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16d0303030150442401a111f44843f4f
http://europepmc.org/articles/PMC4253085
http://europepmc.org/articles/PMC4253085
Autor:
Peter H. Schafer, Anita Gandhi, Emily Rychak, Svetlana Gaidarova, Brian E. Cathers, Hiroshi Handa, Takumi Ito, Afshin Mahmoudi, Thomas O. Daniel, Antonia Lopez-Girona, Roger Shen-Chu Chen, Jilly F. Evans, Pilgrim Jackson, Mahan Abbasian, Rajesh Chopra, Derek Mendy, Gilles Carmel, Karen Miller, Jian Kang, Satoki Karasawa
Publikováno v:
Leukemia
Thalidomide and the immunomodulatory drug, lenalidomide, are therapeutically active in hematological malignancies. The ubiquitously expressed E3 ligase protein cereblon (CRBN) has been identified as the primary teratogenic target of thalidomide. Our
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c03579afee9c0c69c2956c87ab3cdc19
http://t2r2.star.titech.ac.jp/cgi-bin/publicationinfo.cgi?q_publication_content_number=CTT100691788
http://t2r2.star.titech.ac.jp/cgi-bin/publicationinfo.cgi?q_publication_content_number=CTT100691788
Autor:
Richard A. Alm, Mikael Berg, Bo Xu, Wei Yang, Peter J. Tummino, Daniel J Krosky, Gilles Carmel
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology. 1594:297-306
3-Deoxy- D - manno -2-octulosonate-8-phosphate (KDO-8-P) synthase catalyzes the aldol-type condensation of phosphoenolpyruvate and D -arabinose-5-phosphate (A-5-P) to produce KDO-8-P and inorganic phosphate. All KDO-8-P synthases, as exemplified by t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::650bf86c14c460af916de4942b5e02cf
https://doi.org/10.1016/s0167-4838(01)00319-3
https://doi.org/10.1016/s0167-4838(01)00319-3
Autor:
Tam Tran, Gabriel C. Lander, James Carmichale, Thomas O. Daniel, Svetlana Gaidarova, Mary E Matyskiela, Lyn'Al Nosaka, Antonia Lopez-Girona, Takumi Ito, Alexander L. Ruchelman, Gilles Carmel, Jack Houston, Brian E. Cathers, Philip P Chamberlain, Wei Fang, Hiroshi Handa, Derek Nguyen, Mariko Riley, Karen Miller, Shuichan Xu, Barbra Pagarigan, Gang Lu, Chin-Chu Lu, Nai-Yu Wang
Publikováno v:
Cancer Research. 77:SY37-02
The protein cereblon is part of the CRL4-CRBN E3 ubiquitin ligase complex, and has been shown to be the molecular target for the drugs lenalidomide and pomalidomide. These drugs bind to the surface of cereblon, triggering the recruitment of substrate
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2acec69e19aebcc0985034bd9ab2603b
https://doi.org/10.1158/1538-7445.am2017-sy37-02
https://doi.org/10.1158/1538-7445.am2017-sy37-02
Publikováno v:
Archives of Biochemistry and Biophysics. 387:11-19
The structure of TPK1delta, a truncated variant of the cAMP-dependent protein kinase catalytic subunit from Saccharomyces cerevisiae, was determined in an unliganded state at 2.8 A resolution and refined to a crystallographic R-factor of 19.4%. Compa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3408370f801102519b80b6449a380783
https://doi.org/10.1006/abbi.2000.2241
https://doi.org/10.1006/abbi.2000.2241