PHA 415 2011 TEST 2 MEMO

1.1. Glucocorticoids regulate carbohydrate, lipid, and protein metabolism

Mineralcorticoids influence salt balance and water retention.

1.2 Steroids consist of four fused rings (A, B, C and D). Chemically, these hydrocarbons are
cyclopean-tanoperhydrophenanthrene; they contain a five-membered cyclopentane (D) ring
plus the three rings of phenanthrene.

A perhydrophenanthrene (rings A, B, and C) is the completely saturated derivative of

phenanthrene.

1.3.Pregnenolone serves as the common precursor in the formation of the adrenocorticoids

and other steroid hormones

1.4. One of the principal actions of estrogens is to promote the development of female
secondary sex characteristics.

These feminizing attributes include hair growth, skin softening, breast growth, and
accumulation of fat in the thighs, hips, and buttocks.

Estrogen also stimulates the growth and development of the female reproductive tract,
including the uterine oviduct, cervix, and vagina.

Estrogens play a significant role in breast tissue as well.

Estrogens serve as “fuel” for hormone-dependant mammary carcinoma and cause

proliferation of breast cells.

They also stimulate gene expression and, therefore, the production of several proteins,
including those intracellular proteins important for breast cell function and growth as well as
those proteins that influence tumor growth and metastasis.

1.5. HRE are particular regions of the cellular DNA, referred to as hormone-responsive
elements
The receptor dimmer interacts with HRE and with various coactivators and nuclear
transcriptional factors.
Binding of the nuclear steroid-receptor complex to DNA (HRE) initiates transcription of the
DNA sequence to produce mRNA.
2.1 The steroid nucleus is not required for estrogenic action

Several derivatives of stilbene (diphenylethylene) that were used therapeutically demonstrate

potent estrogenic activity.

The aromatic A ring and the C3 hydroxyl group are structural features essential for estrogenic
activity.

The 17β-hydroxyl

the distance between the C3 and C17 hydroxyl groups,

and the presence of planar hydrophobic scaffolding also are important structural contributors
and help to optimize estrogenic activity.

Ideally, the distance between the oxygen atoms of the C3 and C17 hydroxyl groups should
range from 10.3 to 12.1 Å.

2.2 An antiprogestin is a substance that competes with progesterone for its receptor

Prevents progesterone from binding to and activating its receptor.

Because progesterone is integral to the continuation of an early pregnancy

Antiprogestins will interfere with pregnancy maintenance

2.3 They exhibit high affinity for the ER.

They prevent translocation of the estrogen-receptor complex in to the nucleus of target cells

Interfere with the binding of the receptor hormone complex to the receptor site of the
chromatin

2.4 Inhibitors of aromatase

Block the conversion of androgens to estrogens

Therapeutic potential to control reproductive functions, aids in treatment of estrogen

dependant breast cancer

Compete with androstenedione for active site of the aromatase enzyme.

3.1 Estradiol

3.2 Ethynyl Estradiol

3.3 Estradiol cypionate or Estradiol valerate

3.4 Budesonide

3.5 Mometasone Furoate

3.6 Fluticasone Propionate

3.7 Prednisone or Prednisolone

3.8 Fludrocortisone

3.9 Methylprednisone

3.10 Betamethasone