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FTY720 demonstrates promising preclinical activity for chronic lymphocytic leukemia and lymphoblastic leukemia/lymphoma.
FTY720 treatment resulted in significant prolonged survival in a xenograft severe combined immunodeficiency mouse model of disseminated B-cell lymphoma/leukemia, providing the first evidence for the potential use of FTY720 as a therapeutic agent in a variety of B- cell malignancies, including CLL. Expand
Structural basis for antagonism and resistance of bicalutamide in prostate cancer
The three-dimensional structure demonstrates that the B ring of R-bicalutamide in the W741L mutant is accommodated at the location of the indole ring of Trp-741 in the WT AR bound to dihydrotestosterone. 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 fiveExpand
Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia.
Flavopiridol administered using this novel schedule has significant clinical activity in refractory CLL and other diseases, and patients with bulky disease and high-risk genetic features have achieved durable responses, thereby justifying further study of flavopirIDol. Expand
Chemistry and structural biology of androgen receptor.
This review focuses on well-characterized AR ligands that bind to the AR with high affinity and integrates discussion regarding the biology, metabolism, and structure-activity relationships for therapeutic and emerging classes of AR ligand. Expand
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,
GTx-024 showed a dose-dependent improvement in total lean body mass and physical function and was well tolerated and may be useful in the prevention and/or treatment of muscle wasting associated with cancer and other chronic diseases. Expand
FTY720 Shows Promising In vitro and In vivo Preclinical Activity by Downmodulating Cyclin D1 and Phospho-Akt in Mantle Cell Lymphoma
These results provide the first evidence for a potential use of FTY720 in targeting key pathways that are operable in the pathogenesis of MCL and warrant further investigation of F TY720 in clinical trials to treat patients with MCL. Expand
Drug Insight: testosterone and selective androgen receptor modulators as anabolic therapies for chronic illness and aging
Meta-analyses indicate that testosterone supplementation increases fat-free mass and muscle strength in HIV-positive men with weight loss, glucocorticoid-treated men, and older men with low or low-normal testosterone levels, and selective androgen-receptor modulators that are preferentially anabolic hold promise as anabolic therapies. Expand
Structural Basis for Accommodation of Nonsteroidal Ligands in the Androgen Receptor*
These studies provide the first crystallographic evidence of the mechanism by which nonsteroid ligands interact with the wild type AR and provide critical new insight for receptor-based drug design of nonsteroidal AR agonists and antagonists. Expand
Mdr1 limits CYP3A metabolism in vivo.
It is concluded that Pgp, by limiting intracellular substrate availability can be an important determinant of CYP3A metabolism of numerous medications that are substrates for CYP 3A and Pgp. Expand