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1 January 2007
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Cover Image
X-ray crystal structures of flavonoids bound to the ATP-binding site of the PIM1 kinase. Two distinct orientations were observed. Quercetagetin orients the B ring inside the pocket (orientation I), whereas both myricetin and 5,7,3′,4′,5′-pentahydroxyflavone flip the B ring out toward solvent (orientation II). Both binding orientations have been observed in the crystal structures of flavonoids bound to other kinases. Quercetin in complex with phosphatidylinositol 3-kinase γ (1E8W) and fisetin in complex with cyclin-dependent kinase 6 (1XO2) represent orientation I, whereas quercetin in complex with hematopoetic cell kinase (2HCK) exemplifies orientation II. For details, see Holder et al. in this issue.Close Modal - PDF Icon PDF LinkTable of Contents
ISSN 1535-7163
EISSN 1538-8514
Drug Development Series: Review
Reviews
Research Articles: Therapeutics, Targets, and Development
Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer cell proliferation
Deborah L. Marrocco; Wayne D. Tilley; Tina Bianco-Miotto; Andreas Evdokiou; Howard I. Scher; Richard A. Rifkind; Paul A. Marks; Victoria M. Richon; Lisa M. Butler
Cell cycle phenotype-based optimization of G2-abrogating peptides yields CBP501 with a unique mechanism of action at the G2 checkpoint
Shi-Ken Sha; Takuji Sato; Hidetaka Kobayashi; Machiyo Ishigaki; Sayaka Yamamoto; Hitoshi Sato; Asako Takada; Sigetosi Nakajyo; Yasuo Mochizuki; Jonathan M. Friedman; Fong-Chi Cheng; Takashi Okura; Ryohei Kimura; Donald W. Kufe; Daniel D. VonHoff; Takumi Kawabe
Pharmacodynamic characterization of chemopreventive triterpenoids as exceptionally potent inducers of Nrf2-regulated genes
Melinda S. Yates; Masafumi Tauchi; Fumiki Katsuoka; Kathleen C. Flanders; Karen T. Liby; Tadashi Honda; Gordon W. Gribble; Delinda A. Johnson; Jeffrey A. Johnson; Neal C. Burton; Tomás R. Guilarte; Masayuki Yamamoto; Michael B. Sporn; Thomas W. Kensler
D-501036, a novel selenophene-based triheterocycle derivative, exhibits potent in vitro and in vivo antitumoral activity which involves DNA damage and ataxia telangiectasia–mutated nuclear protein kinase activation
Shin-Hun Juang; Chia-Chi Lung; Pi-Chen Hsu; Kuo-Shun Hsu; Yu-Chen Li; Pao-Chiung Hong; Her-Shyong Shiah; Ching-Chuan Kuo; Ching-Wei Huang; Yu-Chin Wang; Leeyuan Huang; Tom S. Chen; Shyh-Fong Chen; Kuo-Chu Fu; Cheng-Li Hsu; Meng-Ju Lin; Ching-jer Chang; Curtis L. Ashendel; Thomas C.K. Chan; Kai-Ming Chou; Jang-Yang Chang
A phase I trial of hyperthermia-induced interleukin-12 gene therapy in spontaneously arising feline soft tissue sarcomas
Farzan Siddiqui; Chuan-Yuan Li; Susan M. LaRue; Jean M. Poulson; Paul R. Avery; Amy F. Pruitt; Xiuwu Zhang; Robert L. Ullrich; Donald E. Thrall; Mark W. Dewhirst; Marlene L. Hauck
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