Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Richard Brokx"'
Autor:
David Cescon, Jeffrey Bruce, Lisa-Maria Yonemoto, Philippe L. Bedard, Trisha Denny, Dennis J. Slamon, Mark R. Bray, Tak W. Mak, Zev A. Wainberg, Sze-Wan Li, Graham C. Fletcher, Peter Brent Sampson, Zachary William Neil Veitch, Trevor J. Pugh, Richard Brokx
Publikováno v:
British Journal of Cancer
British journal of cancer, vol 121, iss 4
British journal of cancer, vol 121, iss 4
Background CFI-400945 is a first-in-class oral inhibitor of polo-like kinase 4 (PLK4) that regulates centriole duplication. Primary objectives of this first-in-human phase 1 trial were to establish the safety and tolerability of CFI-400945 in patient
Autor:
Richard Brokx, Graham C. Fletcher, Tak W. Mak, Irina Beletskaya, Xin Wei, Richard Hodgson, Reza Kiarash, Mark R. Bray, Jacqueline M. Mason
Publikováno v:
Proceedings of the National Academy of Sciences. 114:3127-3132
Loss of cell-cycle control is a hallmark of human cancer. Cell-cycle checkpoints are essential for maintaining genome integrity and balanced growth and division. They are specifically deregulated in cancer cells and contain regulators that represent
Autor:
Tak W. Mak, Xin Wei, Guodong Mao, Grace Ng, Richard Brokx, Dan Chi-Chia Lin, Graham C. Fletcher, Miklos Feher, Olga Plotnikova, Richard J. Hodgson, Radoslaw Laufer, Henry W. Pauls, Jacqueline M. Mason, Yunhui Lang, Brian Madeira, Irina Beletskaya, Sze-Wan Li, Yong Liu, Yi Che, Donald E. Awrey, Reza Kiarash, Mark R. Bray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3562-3566
TTK/Mps1 is a key kinase controlling progression of cell division via participation in the mitotic spindle assembly checkpoint and is overexpressed in a number of human cancers. Herein we report the discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazi
Autor:
Mark R. Bray, Wei Qiu, Radoslaw Laufer, Olga Plotnikova, Henry W. Pauls, Richard Brokx, Dan Chi-Chia Lin, Graham C. Fletcher, Richard J. Hodgson, Sze-Wan Li, Narendra Kumar B. Patel, Peter Brent Sampson, Jacqueline M. Mason, Irina Beletskaya, Yunhui Lang, Xin Wei, Yi Che, Reza Kiarash, Tak W. Mak, Miklos Feher, Grace Ng, Donald E. Awrey, Yong Liu, Nickolay Y. Chirgadze
Publikováno v:
ACS Medicinal Chemistry Letters. 7:671-675
This work describes a scaffold hopping exercise that begins with known imidazo[1,2-a]pyrazines, briefly explores pyrazolo[1,5-a][1,3,5]triazines, and ultimately yields pyrazolo[1,5-a]pyrimidines as a novel class of potent TTK inhibitors. An X-ray str
Autor:
Ursula A. Matulonis, Helen Mackay, C. Sidor, Nita K. Lee, Brian Lasonde, Gini F. Fleming, Vincent Castonguay, Julie Lee, Amit M. Oza, Jamie Arnott, Graham C. Fletcher, Daniela Matei, Mark R. Bray, Jill Grothusen, William P. Tew, Richard Brokx, Kian Behbakht, Afra Yehwalashet
Publikováno v:
European Journal of Cancer. 49:121-131
Purpose The purpose was to assess the activity and side effect profile of ENMD-2076, an oral anti-angiogenic and anti-proliferative kinase inhibitor, in platinum-resistant recurrent epithelial ovarian cancer (EOC), fallopian tube or peritoneal cancer
Autor:
Mark R. Bray, Todd A. Hembrough, William E. Fogler, Trisha Denny, C. Sidor, Stacy M. Plum, Graham C. Fletcher, Richard Brokx
Publikováno v:
Molecular Cancer Therapeutics. 10:126-137
ENMD-2076 is a novel orally active, small molecule kinase inhibitor with a mechanism of action involving several pathways key to tumor growth and survival: angiogenesis, proliferation, and the cell cycle. ENMD-2076 has selective activity against the
Autor:
John S. Ward, Dinesh V. Patel, Mark R. Bray, Sampath-Kumar Anandan, Xiao-Xi Xiao, Richard Brokx
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1969-1972
Inhibitors of histone deacetylases (HDAC) are emerging as a promising class of anti-cancer agents. A mercaptoamide functionality was designed as a bidentate zinc chelator and incorporated into the hydroxamic acid based SAHA (1) scaffold in order to i
Autor:
Mark R. Bray, Tak W. Mak, Zev A. Wainberg, Peter Sampson, Philippe L. Bedard, Trish Denny, Dennis J. Slamon, David W. Cescon, Richard Brokx, Graham Fletcher
Publikováno v:
Cancer Research. 76:CT066-CT066
Background: CFI-400945 is a first-in-class, potent, selective, orally active inhibitor of Polo-like kinase 4 (PLK4) (Ki = 0.26 nM), a conserved master regulator of centriole duplication that is important for maintenance of genomic integrity. In precl
Autor:
John S. Ward, Sampath-Kumar Anandan, Dinesh V. Patel, Trisha Denny, Xiao-Yi Xiao, Richard Brokx, Mark R. Bray
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(21)
We have designed and synthesized a series of structurally novel hydroxamic acid-based histone deacetylase (HDAC) inhibitors characterized by a zinc chelating head group attached directly to a thiazole ring. The thiazole ring connects to a piperazine
Publikováno v:
Journal of molecular biology. 365(4)
Tetramerization of the human p53 tumor suppressor protein is required for its biological functions. However, cellular levels of p53 indicate that it exists predominantly in a monomeric state. Since the oligomerization of p53 involves the rate-limitin