Thyroid-binding inhibiting

The steroid hormone 1,25-dihydroxy vitamin D3 (calcitriol) slowly increases both intestinal calcium absorption and bone resorption, and is also stimulated through low calcium levels. In contrast, calcitonin rapidly inhibits osteoclast activity and thus decreases serum calcium levels. Calcitonin is secreted by the clear cells of the thyroid and inhibits osteoclast activity by increasing the intracellular cyclic AMP content via binding to a specific cell surface receptor, thus causing a contraction of the resorbing cell membrane. The biological relevance of calcitonin in human calcium homeostasis is not well established. 

Thyrotropin-releasing factor (TRF) is produced in the hypothalamus and arrives at the pituitary via the hypophyseal portal blood system. TRF mediates the release of thyrotropin from the anterior hypophysis. The thyrotropin release is inhibited by thyroxine, presumably free thyroxine, and the inhibition is dose dependent. Thus excessive levels of thyroxine depress thyrotropin release, and lower thyroxine levels result in increased thyrotropin release from the anterior pituitary. TSH, in turn, stimulates thyroid hormone synthesis and secretion by the thyroid gland. Thyroxine and triiodothyronine are bound to specific binding proteins in the blood. The amounts and binding constants of the specific thyroid-binding proteins, together with the rate of thyroid hormone release from the thyroid, determine the amount of free thyroxine in the blood. Free thyroxine levels are determined not only by the rate of... 

The functional form of thyroxine (T3) is generated by the deiodination of T4, and PCBs can influence the tissue levels of this form by disturbing metabolism, as well as by reducing the binding of T4. PCBs have been shown to inhibit the sulfation of thyroid hormones and the deiodination of T4 to T3. They can also induce the glucuronyl transferase that conjugates T4 (Brouwer et al. 1998). 

A) Thiocyanate inhibits the binding of iodide to thyroid hormone receptors. 

Mechanism of Action A thioimidazole derivative that inhibits synthesis of thyroid hormone by interfering with the incorporation of iodine into tyrosyl residues. Thera-peuticEffect Effectively treats hyperthyroidism by decreasingthyroid hormone levels. Pharmacohinetics Rapid absorption following PO administration. Protein binding Not significant. Widely distributed throughout the body. Metabolized in liver. Excreted in urine. Half-life 5-6 hr. 

Miyamoto, T, Kaneko, A., Kakizawa, T, Yajima, H., Kamijo, K., Sekine, R., Hiramatsu, K., Nishii, Y, Hashimoto, T. Hashizume, K. (1997) Inhibition of peroxisome proliferator signaling pathways by thyroid hormone receptor. Competitive binding to the response element. J. biol. Chem., Ill, 7752-7758... 

Doxorubicin Oxygen free radicals bind to DNA causing single- and double-strand DNA breaks inhibits topoisomerase II intercalates into DNA Breast cancer, Hodgkin s and non-Hodgkin s lymphoma, soft tissue sarcoma, ovarian cancer, non-small cell and small cell lung cancer, thyroid cancer, Wilms tumor, neuroblastoma Nausea, red urine (not hematuria) Cardiotoxicity (see text), alopecia, myelosuppression, stomatitis... 

Thyroid hormone receptors differ from steroid hormone receptors in that they are always bound to DNA. In the absence of thyroid hormones, these receptors inhibit the expression of genes to which they bind the addition of hormone converts them into transcriptional activators. 

Daunorubicin (Daunomycin and Cerubidine) and doxorubicin (Adriamycin) bind to and cause the intercalation of the DNA molecule, thereby inhibiting DNA template function. They also provoke DNA chain scission and chromosomal damage. Daunorubicin is useful in treating patients with acute lymphocytic or acute granulocytic leukemia. Adriamycin is useful in cases of solid tumors such as sarcoma, metastatic breast cancer, and thyroid cancer. These agents cause stomatitis, alopecia, myelosuppression, and cardiac abnormalities ranging from arrhythmias to cardiomyopathy. 

Fig. 7. Model for activation by coactivators (A) and inhibition by corepressors (B) of transcription. Abbreviations CBP/p300, cAMP response element binding protein SRC-1, steroid receptor coactivator 1 TBP, TATA-binding protein TAF, TBP-associated factor pol II, RNA polymerase II N-CoR, nuclear receptor corepressor SMRT, silencing mediator of retinoic and thyroid hormone receptors.

---