Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia
High expression of Mcl-1 promotes tumorigenesis and resistance to anticancer therapies. Here they report a macrocyclic molecule with high selectivity and affinity for Mcl-1 that exhibits potent anti-tumor effects as single agent and in combination with bortezomib or venetoclax in preclinical models...
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Nature Portfolio
2018
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oai:doaj.org-article:814ff3ef6b204d84917e2b025f3e1da92021-12-02T16:49:22ZDiscovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia10.1038/s41467-018-07551-w2041-1723https://doaj.org/article/814ff3ef6b204d84917e2b025f3e1da92018-12-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-07551-whttps://doaj.org/toc/2041-1723High expression of Mcl-1 promotes tumorigenesis and resistance to anticancer therapies. Here they report a macrocyclic molecule with high selectivity and affinity for Mcl-1 that exhibits potent anti-tumor effects as single agent and in combination with bortezomib or venetoclax in preclinical models of multiple myeloma and acute myeloid leukemia.Adriana E. TronMatthew A. BelmonteAmmar AdamBrian M. AquilaLawrence H. BoiseElisabetta ChiarparinJustin CidadoKevin J. EmbreyEric GanglFrancis D. GibbonsGareth P. GregoryDavid HargreavesJ. Adam HendricksJeffrey W. JohannesRicky W. JohnstoneSteven L. KazmirskiJason G. KettleMichelle L. LambShannon M. MatulisAjay K. NookaMartin J. PackerBo PengPhilip B. RawlinsDaniel W. RobbinsAlwin G. SchullerNancy SuWenzhan YangQing YeXiaolan ZhengJ. Paul SecristEdwin A. ClarkDavid M. WilsonStephen E. FawellAlexander W. HirdNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-14 (2018) |
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DOAJ |
| collection |
DOAJ |
| language |
EN |
| topic |
Science Q |
| spellingShingle |
Science Q Adriana E. Tron Matthew A. Belmonte Ammar Adam Brian M. Aquila Lawrence H. Boise Elisabetta Chiarparin Justin Cidado Kevin J. Embrey Eric Gangl Francis D. Gibbons Gareth P. Gregory David Hargreaves J. Adam Hendricks Jeffrey W. Johannes Ricky W. Johnstone Steven L. Kazmirski Jason G. Kettle Michelle L. Lamb Shannon M. Matulis Ajay K. Nooka Martin J. Packer Bo Peng Philip B. Rawlins Daniel W. Robbins Alwin G. Schuller Nancy Su Wenzhan Yang Qing Ye Xiaolan Zheng J. Paul Secrist Edwin A. Clark David M. Wilson Stephen E. Fawell Alexander W. Hird Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| description |
High expression of Mcl-1 promotes tumorigenesis and resistance to anticancer therapies. Here they report a macrocyclic molecule with high selectivity and affinity for Mcl-1 that exhibits potent anti-tumor effects as single agent and in combination with bortezomib or venetoclax in preclinical models of multiple myeloma and acute myeloid leukemia. |
| format |
article |
| author |
Adriana E. Tron Matthew A. Belmonte Ammar Adam Brian M. Aquila Lawrence H. Boise Elisabetta Chiarparin Justin Cidado Kevin J. Embrey Eric Gangl Francis D. Gibbons Gareth P. Gregory David Hargreaves J. Adam Hendricks Jeffrey W. Johannes Ricky W. Johnstone Steven L. Kazmirski Jason G. Kettle Michelle L. Lamb Shannon M. Matulis Ajay K. Nooka Martin J. Packer Bo Peng Philip B. Rawlins Daniel W. Robbins Alwin G. Schuller Nancy Su Wenzhan Yang Qing Ye Xiaolan Zheng J. Paul Secrist Edwin A. Clark David M. Wilson Stephen E. Fawell Alexander W. Hird |
| author_facet |
Adriana E. Tron Matthew A. Belmonte Ammar Adam Brian M. Aquila Lawrence H. Boise Elisabetta Chiarparin Justin Cidado Kevin J. Embrey Eric Gangl Francis D. Gibbons Gareth P. Gregory David Hargreaves J. Adam Hendricks Jeffrey W. Johannes Ricky W. Johnstone Steven L. Kazmirski Jason G. Kettle Michelle L. Lamb Shannon M. Matulis Ajay K. Nooka Martin J. Packer Bo Peng Philip B. Rawlins Daniel W. Robbins Alwin G. Schuller Nancy Su Wenzhan Yang Qing Ye Xiaolan Zheng J. Paul Secrist Edwin A. Clark David M. Wilson Stephen E. Fawell Alexander W. Hird |
| author_sort |
Adriana E. Tron |
| title |
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| title_short |
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| title_full |
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| title_fullStr |
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| title_full_unstemmed |
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| title_sort |
discovery of mcl-1-specific inhibitor azd5991 and preclinical activity in multiple myeloma and acute myeloid leukemia |
| publisher |
Nature Portfolio |
| publishDate |
2018 |
| url |
https://doaj.org/article/814ff3ef6b204d84917e2b025f3e1da9 |
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1718383344974036992 |