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Anti-hormone Therapy: Principles of Endocrine Therapy of Cancer

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Cancer

Part of the book series: Topics in Medicinal Chemistry ((TMC,volume 1))

Abstract

Surgical oophorectomy and orchiectomy, first proposed over a century ago, are effective in thetherapy of breast and prostate cancer, respectively. Later, the discovery of steroid hormones and the steroidhormone receptors led to the concept that inhibition of steroid hormone receptor function by an antagonistprevents tumour growth. While the first anti-hormones, cyproterone acetate (CPA) and tamoxifen, were foundaccidentally, a deeper understanding of steroid hormone receptors as transcription factors enabledmore rational, structure–activity relationship-based drug discovery programmes. This review willprovide both a background on principles and an update on recent developments in the field of endocrinetherapy of cancer.

Results from recent drug-finding programmes on new steroid hormone receptor antagonists will be reviewed.Among these, new steroidal and non-steroidal compounds with increased potency and efficacy, improved tissueselectivity, and without any agonistic activity will be described. New pre-clinical and clinical data ondevelopment candidates will be reported. Advanced breast and prostate cancer is effectively managed byestrogen and androgen ablation, respectively. However, although steroid hormone receptors– estrogenreceptor α (ERα) and androgen receptor (AR) – are still functionally expressed, this therapyfails in a majority of cases. As a novel strategy for the treatment of advanced breast and prostatecancer, the selective down-regulation of the receptor (ER or AR, respectively) has been proposed and thisnew therapeutic concept provides a significant inhibition of tumour growth in vivo.

In addition, it will be our intention to present a deeper insight into the biosynthesis of steroidhormones, which will allow definition of new targets and approaches for the treatment of endocrine-responsivecancer. Enzymes involved in mechanisms of steroid hormone biosynthesis might be novel targets for endocrinetherapy. Moreover, further therapeutic indications for modulators of steroid hormone receptors will bediscussed. In summary, many promising new opportunities for endocrine therapy of breast and prostate cancerare now arising.

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Abbreviations

AACR:

American Association for Cancer Research

AF-1/-2:

Activation function 1 or 2

AI:

Aromatase inhibitor

AR:

Androgen receptor

ARE:

Androgen response element

BPH:

Benign prostate hyperplasia

CIS:

Carcinoma in situ

CPA:

Cyproterone acetate

CR:

Complete response

DBD:

DNA binding domain

DES:

Diethylstilbestrol

DHEA:

Dehydoepiandrostenedione

DHT:

Dihydrotestosterone

E1:

Estrone

E1S:

Estrone sulfate

E2:

17β-Estradiol

EGF:

Epidermal growth factor

EGFR:

Epidermal growth factor receptor

EORTC:

European Organisation for Research and Treatment of Cancer

ER:

Estrogen receptor

ERE:

Estrogen response element

ERKO:

Estrogen receptor knock-out mouse

FSH:

Follicle-stimulating hormone

GnRH:

Gonadotropin-releasing hormone

GR:

Glucocorticoid receptor

HRE:

Hormone response element

HSD:

17β-Hydroxysteroid dehydrogenase

HSP:

Heat shock protein

IEN:

Intraepithelial neoplasia

IGF-1:

Insulin-like growth factor 1

IL-6:

Interleukin 6

KGF:

Keratinocyte growth factor

LBD:

Ligand-binding domain

LH:

Luteinising hormone

LHRH:

Luteinising hormone releasing hormone

MAPK:

Mitogen-activated protein kinase

MGA:

Megestrol acetate

MPA:

Medroxyprogesterone acetate

MMTV:

Murine mammary tumour virus

MR:

Mineralocorticoid receptor

NCI:

National Cancer Institute

4-OHA:

4-Hydroxyandrostendione

4-OHT:

4-Hydroxytamoxifen

OR:

Objective response

PIN:

Prostate intraepithelial neoplasia

PR:

Progesterone receptor

PR:

Partial response

PRE:

Progesterone response element

PRKO:

Progesterone receptor knock-out mouse

PSA:

Prostate-specific antigen

RAR/RXR:

Retinoic acid receptors

USPSTF:

US Preventive Services Task Force

SD:

Stable disease

SERD:

Selective estrogen receptor destabiliser

SERM:

Selective estrogen receptor modulator

SRC:

Steroid receptor co-activator

STS:

Steroid sulfatase

TR:

Thyroid hormone receptor

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    Jens Hoffmann & Anette Sommer

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Hoffmann, J., Sommer, A. (2006). Anti-hormone Therapy: Principles of Endocrine Therapy of Cancer. In: Bradbury, R.H. (eds) Cancer. Topics in Medicinal Chemistry, vol 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/7355_2006_002

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