Bradford Graves

ScholarGPS® ID: 30670687980018

Affiliation

Roche Holding AG, Basel, Switzerland

Affiliation History

Field

Physical Sciences and Mathematics

Discipline

Chemistry

Top Specialties

Medicinal Chemistry | Crystal Structure | Influenza | Peptide

Metrics Summary

Publication Count

Predicted Citations

10,732

Predicted h-index

Ranking

Publications and Citation History

Publications based on Top Specialties

Types of Publication

Publications
Books
Patents
NIH/NSF

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Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development (journal article) Guerlavais, Vincent \| Sawyer, Tomi K. \| Carvajal, Luis \| Chang, Yong S. \| Graves, Bradford \| Ren, Jian-Guo \| Sutton, David \| Olson, Karen A. \| Packman, Kathryn \| Darlak, Krzysztof \| ... \| Annis, D. Allen Journal of Medicinal Chemistry, volume 66, issue 14, pages 9401-9417 (2023). 10.1021/acs.jmedchem.3c00623 Cited by (23) \| Cite \| Source
Inhibiting CREB binding protein (CBP) (patent) Schiller, Shawn E. R. \| Herbertz, Torsten \| Li, Hongbin \| Graves, Bradford \| Mischke, Steven \| West, Angela \| Downing, Jennifer R. \| Ericsson, Anna Patent Number: 10870648 (2020) Cite \| Source
Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy (journal article) Zhang, Zhuming \| Ding, Qingjie \| Liu, Jin-Jun \| Zhang, Jing \| Jiang, Nan \| Chu, Xin-Jie \| Bartkovitz, David \| Luk, Kin-Chun \| Janson, Cheryl \| Tovar, Christian \| ... \| Graves, Bradford Bioorganic & Medicinal Chemistry, volume 22, issue 15, pages 4001-4009 (2014). 10.1016/j.bmc.2014.05.072 Cited by (46) \| Cite \| Source
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development (journal article) Zhang, Zhuming \| Chu, Xin-Jie \| Liu, Jin-Jun \| Ding, Qingjie \| Zhang, Jing \| Bartkovitz, David \| Jiang, Nan \| Karnachi, Prabha \| So, Sung-Sau \| Tovar, Christian \| ... \| Graves, Bradford ACS Medicinal Chemistry Letters, volume 5, issue 2, pages 124-127 (2014). 10.1021/ml400359z Cited by (76) \| Cite \| Source \| Open Access
Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development (journal article) Ding, Qingjie \| Zhang, Zhuming \| Liu, Jin-Jun \| Jiang, Nan \| Zhang, Jing \| Ross, Tina M. \| Chu, Xin-Jie \| Bartkovitz, David \| Podlaski, Frank \| Janson, Cheryl \| ... \| Graves, Bradford Journal of Medicinal Chemistry, volume 56, issue 14, pages 5979-5983 (2013). 10.1021/jm400487c Cited by (460) \| Cite \| Source
Deconstruction of a Nutlin: Dissecting the Binding Determinants of a Potent Protein–Protein Interaction Inhibitor (journal article) Fry, David C. \| Wartchow, Charles \| Graves, Bradford \| Janson, Cheryl \| Lukacs, Christine \| Kammlott, Ursula \| Belunis, Charles \| Palme, Stefan \| Klein, Christian \| Vu, Binh ACS Medicinal Chemistry Letters, volume 4, issue 7, pages 660-665 (2013). 10.1021/ml400062c Cited by (49) \| Cite \| Source \| Open Access
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development (journal article) Vu, Binh \| Wovkulich, Peter \| Pizzolato, Giacomo \| Lovey, Allen \| Ding, Qingjie \| Jiang, Nan \| Liu, Jin-Jun \| Zhao, Chunlin \| Glenn, Kelli \| Wen, Yang \| ... \| Graves, Bradford ACS Medicinal Chemistry Letters, volume 4, issue 5, pages 466-469 (2013). 10.1021/ml4000657 Cited by (303) \| Cite \| Source \| Open Access
MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models (journal article) Tovar, Christian \| Graves, Bradford \| Packman, Kathryn \| Filipovic, Zoran \| Xia, Brian Higgins Mingxuan \| Tardell, Christine \| Garrido, Rosario \| Lee, Edmund \| Kolinsky, Kenneth \| To, Kwong-Him \| ... \| Vassilev, Lyubomir T. Cancer Research, volume 73, issue 8, pages 2587-2597 (2013). 10.1158/0008-5472.CAN-12-2807 Cited by (246) \| Cite \| Source \| Open Access
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 (journal article) Ray-Coquard, Isabelle \| Blay, Jean-Yves \| Italiano, Antoine \| Le Cesne, Axel \| Penel, Nicolas \| Zhi, Jianguo \| Heil, Florian \| Rueger, Ruediger \| Graves, Bradford \| Ding, Meichun \| ... \| Bui, Binh Nguyen The Lancet Oncology, volume 13, issue 11, pages 1133-1140 (2012). 10.1016/S1470-2045(12)70474-6 Cited by (470) \| Cite \| Source
Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization (journal article) Graves, Bradford \| Thompson, Thelma \| Xia, Mingxuan \| Janson, Cheryl \| Lukacs, Christine \| Deo, Dayanand \| Di Lello, Paola \| Fry, David \| Garvie, Colin \| Huang, Kuo-Sen \| ... \| Vassilev, Lyubomir T. Proceedings of the National Academy of Sciences, volume 109, issue 29, pages 11788-11793 (2012). 10.1073/pnas.1203789109 Cited by (190) \| Cite \| Source \| Open Access
Spiroindolinone pyrrolidines (patent) Bartkovitz, David Joseph \| Chu, Xin-Jie \| Ding, Qingjie \| Graves, Bradford James \| Jiang, Nan \| Zhang, Jing \| Zhang, Zhuming Patent Number: 8088815 (2012) Cited by (28) \| Cite \| Source
4,4,5,5, tetrasubstituted imidazolines (patent) Ding, Qingjie \| Graves, Bradford James \| Kong, Norman \| Liu, Jin-Jun \| Lovey, Allen John \| Pizzolato, Giacomo \| Roberts, John Lawson \| So, Sung-Sau \| Vu, Binh Thanh \| Wovkulich, Peter Michael Patent Number: 7851626 (2010) Cited by (38) \| Cite \| Source
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), A Potent and Selective Cyclin-Dependent Kinase Inhibitor with Significant in Vivo Antitumor Activity (journal article) Chu, Xin-Jie \| DePinto, Wanda \| Bartkovitz, David \| So, Sung-Sau \| Vu, Binh T. \| Packman, Kathryn \| Lukacs, Christine \| Ding, Qingjie \| Jiang, Nan \| Wang, Ka \| ... \| Fotouhi, Nader Journal of Medicinal Chemistry, volume 49, issue 22, pages 6549-6560 (2006). 10.1021/jm0606138 Cited by (125) \| Cite \| Source
Optimization of Small Molecule Drugs Binding to Highly Polar Target Sites: Lessons from the Discovery and Development of Neuraminidase Inhibitors (journal article) Klumpp, Klaus \| Graves, Bradford Current Topics in Medicinal Chemistry, volume 6, issue 5, pages 423-434 (2006). 10.2174/156802606776743138 Cited by (20) \| Cite \| Source
Small Molecule Inhibitors of p53/MDM2 Interaction (journal article) Fotouhi, Nader \| Graves, Bradford Current Topics in Medicinal Chemistry, volume 5, issue 2, pages 159-165 (2005). 10.2174/1568026053507705 Cited by (43) \| Cite \| Source
Development of E3‐Substrate (MDM2‐p53)–Binding Inhibitors: Structural Aspects (book chapter) In Ubiquitin and Protein Degradation, Part B Fry, David C. \| Graves, Bradford \| Vassilev, Lyubomir T. Elsevier (2005) 10.1016/S0076-6879(05)99041-1 Cited by (17) \| Cite \| Source
In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2 (journal article) Vassilev, Lyubomir T. \| Vu, Binh T. \| Graves, Bradford \| Carvajal, Daisy \| Podlaski, Frank \| Filipovic, Zoran \| Kong, Norman \| Kammlott, Ursula \| Lukacs, Christine \| Klein, Christian \| ... \| Liu, Emily A. Science, volume 303, issue 5659, pages 844-848 (2004). 10.1126/science.1092472 Cited by (3,937) \| Cite \| Source
ChemInform Abstract: Carbocyclic Influenza Neuraminidase Inhibitors Possessing a C3 ‐Cyclic Amine Side Chain: Synthesis and Inhibitory Activity. (journal article) Lew, Willard \| Wu, Huiwei \| Chen, Xiaowu \| Graves, Bradford J. \| Escarpe, Paul A. \| MacArthur, Holly L. \| Mendel, Dirk B. \| Kim, Choung U. ChemInform, volume 31, issue 39 (2000). 10.1002/chin.200039227 Cite \| Source
Carbocyclic influenza neuraminidase inhibitors possessing a C 3 -cyclic amine side chain: synthesis and inhibitory activity (journal article) Lew, Willard \| Wu, Huiwei \| Chen, Xiaowu \| Graves, Bradford J \| Escarpe, Paul A \| MacArthur, Holly L \| Mendel, Dirk B \| Kim, Choung U Bioorganic & Medicinal Chemistry Letters, volume 10, issue 11, pages 1257-1260 (2000). 10.1016/S0960-894X(00)00214-6 Cited by (33) \| Cite \| Source
ChemInform Abstract: Synthesis and Evaluation of 1,4,5,6‐Tetrahydropyridazine Derivatives as Influenza Neuraminidase Inhibitors. (journal article) Zhang, Lijun \| Williams, Matthew A. \| Mendel, Dirk B. \| Escarpe, Paul A. \| Chen, Xiaowu \| Wang, Ke‐Yu \| Graves, Bradford J. \| Lawton, Geoff \| Kim, Choung U. ChemInform, volume 30, issue 43 (1999). 10.1002/chin.199943146 Cited by (1) \| Cite \| Source