B
Bradford Graves
Researcher at Hoffmann-La Roche
Publications - 42
Citations - 8453
Bradford Graves is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Neuraminidase & Nutlin. The author has an hindex of 23, co-authored 40 publications receiving 7685 citations. Previous affiliations of Bradford Graves include University of Hertfordshire.
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Journal ArticleDOI
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Lyubomir T. Vassilev,Binh Thanh Vu,Bradford Graves,Daisy Carvajal,Frank John Podlaski,Zoran Filipovic,Norman Kong,Ursula Kammlott,Christine Lukacs,Christian Klein,Nader Fotouhi,Liu Emily Aijun +11 more
TL;DR: In this article, the authors identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts.
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.
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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.
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Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study.
Isabelle Ray-Coquard,Jean-Yves Blay,Antoine Italiano,Axel Le Cesne,Nicolas Penel,Jianguo Zhi,Florian Heil,Ruediger Rueger,Bradford Graves,Meichun Ding,David Geho,Steven A. Middleton,Lyubomir T. Vassilev,Gwen Nichols,Binh Bui +14 more
TL;DR: In this article, the authors report a proof-of-mechanism study of RG7112, a small-molecule MDM2 antagonist, in patients with chemotherapy-naive primary or relapsed well-differentiated or dedifferentiated liposarcoma who were eligible for resection.
Journal ArticleDOI
Insight into E-selectin/ligand interaction from the crystal structure and mutagenesis of the lec/EGF domains
Bradford Graves,Robert Crowther,Chitra Chandran,John M. Rumberger,John M. Rumberger,Shirley Li,Kuo-Sen Huang,David H. Presky,Philip C. Familletti,Barry A. Wolitzky,Daniel K. Burns,Daniel K. Burns +11 more
TL;DR: The three-dimensional structure of the ligand-binding region of human E-selectin has been determined and reveals limited contact between the two domains and a coordination of Ca2+ not predicted from other C-type lectins.