Targeting the Androgen Receptor with Steroid Conjugates

被引：32
|
作者：
Levine, Paul M. [1 ]
Garabedian, Michael J. [2 ,3 ]
Kirshenbaum, Kent [1 ]
机构：
[1] NYU, Dept Chem, New York, NY 10003 USA
[2] NYU Langone Sch Med, Dept Biochem & Mol Pharmacol, New York, NY 10016 USA
[3] NYU Langone Sch Med, Dept Urol, New York, NY 10016 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 20期
基金：
美国国家科学基金会; 美国国家卫生研究院;
关键词：
PROSTATE-CANCER CELLS; SMALL-MOLECULE INHIBITORS; NUCLEAR RECEPTOR; STRUCTURAL BASIS; BINDING DOMAIN; CONFORMATIONAL-CHANGE; DEPRIVATION THERAPY; TESTOSTERONE LEVELS; ANTITUMOR-ACTIVITY; AMINO-ACID;
D O I：
10.1021/jm500101h
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The androgen receptor (AR) is a major therapeutic target in prostate cancer pharmacology. Progression of prostate cancer has been linked to elevated expression of AR in malignant tissue, suggesting that AR plays a central role in prostate cancer cell biology. Potent therapeutic agents can be precisely crafted to specifically target AR, potentially averting systemic toxicities associated with nonspecific chemotherapies. In this review, we describe various strategies to generate steroid conjugates that can selectively engage AR with high potency. Analogies to recent developments in nonsteroidal conjugates targeting AR are also evaluated. Particular focus is placed on potential applications in AR pharmacology. The review culminates with a description of future prospects for targeting AR.
引用
收藏
页码：8224 / 8237
页数：14
相关论文
共 50 条
  • [31] Targeting the Androgen receptor: 70 years on and still relevant
    Suder, A.
    Rudman, S.
    Chowdhury, S.
    INTERNATIONAL JOURNAL OF CLINICAL PRACTICE, 2012, 66 (08) : 726 - 727
  • [32] Consideration of breast cancer subtype in targeting the androgen receptor
    Venema, Clasina M.
    Bense, Rico D.
    Steenbruggen, Tessa G.
    Nienhuis, Hilde H.
    Qiu, Si-Qi
    van Kruchten, Michel
    Brown, Myles
    Tamimi, Rulla M.
    Hospers, Geke A. P.
    Schroder, Carolina P.
    Fehrmann, Rudolf S. N.
    de Vries, Elisabeth G. E.
    PHARMACOLOGY & THERAPEUTICS, 2019, 200 : 135 - 147
  • [33] Rational targeting of the Androgen receptor interactome in prostate cancer
    Ravindranathan, Preethi
    Tilley, Wayne
    Raj, Ganesh V.
    CANCER RESEARCH, 2014, 74 (19)
  • [34] Targeting the Androgen Receptor: Remaining questions and future directions
    Ryan, Charles J.
    UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS, 2016, 34 (08) : 339 - 339
  • [35] Developing androgen receptor targeting for salivary gland cancers
    Ho, A. L.
    ANNALS OF ONCOLOGY, 2018, 29 (04) : 792 - 794
  • [36] The evolution of prostate cancer therapy: targeting the androgen receptor
    Aragon-Ching, Jeanny B.
    FRONTIERS IN ONCOLOGY, 2014, 4
  • [37] New Opportunities for Targeting the Androgen Receptor in Prostate Cancer
    Centenera, Margaret M.
    Selth, Luke A.
    Ebrahimie, Esmaeil
    Butler, Lisa M.
    Tilley, Wayne D.
    COLD SPRING HARBOR PERSPECTIVES IN MEDICINE, 2018, 8 (12):
  • [38] Current strategies for targeting the activity of androgen receptor variants
    Armstrong, Cameron M.
    Gao, Allen C.
    ASIAN JOURNAL OF UROLOGY, 2019, 6 (01) : 42 - 49
  • [39] Targeting Continued Androgen Receptor Signaling in Prostate Cancer
    Massard, Christophe
    Fizazi, Karim
    CLINICAL CANCER RESEARCH, 2011, 17 (12) : 3876 - 3883
  • [40] Targeting the androgen receptor and overcoming resistance in prostate cancer
    Einstein, David J.
    Arai, Seiji
    Balk, Steven P.
    CURRENT OPINION IN ONCOLOGY, 2019, 31 (03) : 175 - 182
12345