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Structural basis for antagonism and resistance of bicalutamide in prostate cancer
- Casey E. Bohl, Wenqing Gao, D. Miller, C. Bell, J. Dalton
- Chemistry, Medicine
- Proceedings of the National Academy of Sciences…
- 15 April 2005
Carcinoma of the prostate is the most commonly diagnosed cancer in men. The current pharmacological treatment of choice for progressive androgen-dependent prostate cancer is the nonsteroidal… Expand
FTY720 demonstrates promising preclinical activity for chronic lymphocytic leukemia and lymphoblastic leukemia/lymphoma.
FTY720 is an immunosuppressant developed to prevent organ transplant rejection. Recent studies indicate an additional role for FTY720 in inducing cell apoptosis. We demonstrate here that FTY720… Expand
Chemistry and Structural Biology of Androgen Receptor
The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind,…
- J. Dalton, K. G. Barnette, +5 authors M. Steiner
- Journal of cachexia, sarcopenia and muscle
- 2 August 2011
BackgroundCachexia, also known as muscle wasting, is a complex metabolic condition characterized by loss of skeletal muscle and a decline in physical function. Muscle wasting is associated with… Expand
Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia.
Despite promising preclinical studies with the cyclin-dependent kinase inhibitor flavopiridol in chronic lymphocytic leukemia (CLL) and other diseases, previous clinical trials with this agent have… Expand
Chemistry and structural biology of androgen receptor.
Androgen receptor (AR) is a member of the steroid and nuclear receptor superfamily,1 which is composed of over 100 members and continues to grow. Among this large family of proteins, only five… Expand
Discovery of nonsteroidal androgens.
- J. Dalton, A. Mukherjee, Z. Zhu, L. Kirkovsky, D. Miller
- Medicine, Biology
- Biochemical and biophysical research…
- 6 March 1998
Nonsteroidal androgens have not been reported. During studies to identify affinity ligands for the androgen receptor in our laboratory, we synthesized several electrophilic nonsteroidal ligands for… Expand
Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor*
- Casey E. Bohl, D. Miller, J. Chen, C. Bell, J. Dalton
- Chemistry, Medicine
- Journal of Biological Chemistry
- 11 November 2005
The mechanism by which the androgen receptor (AR) distinguishes between agonist and antagonist ligands is poorly understood. AR antagonists are currently used to treat prostate cancer. However,… Expand
FTY720 Shows Promising In vitro and In vivo Preclinical Activity by Downmodulating Cyclin D1 and Phospho-Akt in Mantle Cell Lymphoma
Purpose: Despite the progress that has been made in the treatment of mantle cell lymphoma (MCL), all patients invariably relapse with the currently available therapies. Because of the absence of… Expand
Drug Insight: testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging
- S. Bhasin, O. M. Calof, +6 authors J. Dalton
- Nature Clinical Practice Endocrinology…
- 1 March 2006
Several regulatory concerns have hindered development of androgens as anabolic therapies, despite unequivocal evidence that testosterone supplementation increases muscle mass and strength in men; it… Expand