C
Christian Tovar
Researcher at Hoffmann-La Roche
Publications - 25
Citations - 4117
Christian Tovar is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Nutlin & Cancer cell. The author has an hindex of 18, co-authored 25 publications receiving 3655 citations.
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Journal ArticleDOI
Selective small-molecule inhibitor reveals critical mitotic functions of human CDK1.
Lyubomir T. Vassilev,Christian Tovar,Shaoqing Chen,Dejan Knezevic,Xiaolan Zhao,Hongmao Sun,David C. Heimbrook,Li Chen +7 more
TL;DR: A selective small-molecule inhibitor of CDK1 is identified that reversibly arrests human cells at the G(2)/M border of the cell cycle and allows for effective cell synchronization in early mitosis.
Journal ArticleDOI
Small-molecule MDM2 antagonists reveal aberrant p53 signaling in cancer: implications for therapy.
Christian Tovar,Jim Rosinski,Zoran Filipovic,Brian Higgins,Kenneth Kolinsky,Holly Hilton,Xiaolan Zhao,Binh Thanh Vu,Weiguo Qing,Packman Kathryn E,Ola Myklebost,David C. Heimbrook,Lyubomir T. Vassilev +12 more
TL;DR: It is found that the cell-cycle arrest function of the p53 pathway is preserved in multiple tumor-derived cell lines expressing wild-type p53, but many have a reduced ability to undergo p53-dependent apoptosis.
Journal ArticleDOI
Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
Yong S. Chang,Bradford Graves,Vincent Guerlavais,Christian Tovar,Packman Kathryn E,Kwong-Him To,Karen A. Olson,Kamala Kesavan,Pranoti Gangurde,Aditi Mukherjee,Theresa Baker,Krzysztof Darlak,Carl Elkin,Zoran Filipovic,Farooq Qureshi,Hongliang Cai,Pamela Berry,Eric Feyfant,Xiangguo E. Shi,James Horstick,D. Allen Annis,Anthony M. Manning,Nader Fotouhi,Huw M. Nash,Lyubomir T. Vassilev,Tomi K. Sawyer +25 more
TL;DR: Overall, ATSP-7041 demonstrates in vitro and in vivo proof-of-concept that stapled peptides can be developed as therapeutically relevant inhibitors of protein–protein interaction and may offer a viable modality for cancer therapy.
Journal ArticleDOI
Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development.
Qingjie Ding,Zhuming Zhang,Jin-Jun Liu,Nan Jiang,Jing Zhang,Tina Morgan Ross,Xin-Jie Chu,David Joseph Bartkovitz,Frank John Podlaski,Cheryl Janson,Christian Tovar,Zoran Filipovic,Brian Higgins,Kelli Glenn,Packman Kathryn E,Lyubomir T. Vassilev,Bradford Graves +16 more
TL;DR: The discovery and characterization of a second generation clinical MDM2 inhibitor, RG7388, with superior potency and selectivity is reported, with a significant challenge for the development of small-molecule inhibitors with desirable pharmacological profiles.
Journal ArticleDOI
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Binh Thanh Vu,Peter Michael Wovkulich,Giacomo Pizzolato,Allen John Lovey,Qingjie Ding,Nan Jiang,Jin-Jun Liu,Chunlin Zhao,Kelli Glenn,Yang Wen,Christian Tovar,Packman Kathryn E,Lyubomir T. Vassilev,Bradford Graves +13 more
TL;DR: RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket ofMDM2, which stabilizes p53 and activates the p 53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.