Modulated Estradiol

Dopp E, voLLMER G, HAHNEL c, GREVESMUHL Y and SCHIFFMANN D (1999) Modulation of tile intracellular calcium level in mammalian cells caused by ivp-estradiol, different phytoestrogens and the anti-estrogen ICl 182780. JSteroid Biochem Mol Biol. 68 (1-2) 57-64. 

Another intriguing observation is that the female sex-hormone 17/i-estradiol (28) could dramatically potentiate capsaicin responses, whereas the male hormone testosterone had marginal inhibitory activity. Sex differences in pain responses have long been known, with women being more sensitive to capsaicin-induced pain than men [94]. The differential modulation of capsaicin responses by female and male hormones might provide a rationale to explain this observation. 

Masana, M. I., Soares, J. M. Jr Dubocovich, M. L. (2005). 17beta-Estradiol modulates hMT(l) melatonin receptor function. Neuroendocrinology 81, 87-95. 

Morales A, Diaz M, Ropero AB, Nadal A, Alonso R (2003) Estradiol modulates acetylcholine-induced Ca2+ signals in LHRH-releasing GT1-7 cells through a membrane binding site. Eur J Neurosci 18 2505-2514... 

Nunemaker CS, De Fazio RA, Moenter SM (2002) Estradiol-sensitive afferents modulate long-term episodic firing patterns of GnRH neurons. Endocrinology 143 2284-2292... 

L. Zampieri, P. Bianchi, P. Ruff, and P. Arbuthnot. Differential modulation by estradiol of P-glycoprotein drug resistance protein expression in cultured MCF7 and T47D breast cancer cells. Anticancer Res. 22 2253-2259 (2002). 

Evidence to Implicate Early Modulation of Interleukin-1/3 Expression in the Neuroprotection Afforded by 17/3-Estradiol in Male Rats Undergone Transient Middle Cerebral Artery Occlusion... 

The activation of TRPVl from capsaicin can be modulated by steroid hormones. Thus, the female hormone estradiol (72) augments the activation of TRPVl by capsaicin, rationalizing the long-standing and curious observation that woman are more sensitive to hot food than men [111,112]. On the other hand, dehydroepian-drosterone (DHEA, 73), the most abundant blood steroid, behaves as a vanilloid antagonists [112]. Since the production of DHEA peaks between 20 and 30 years of age and then gradually fades, young people tolerate hot food better that elderly people. 

There also exist a class of ligands referred to as SERMs (selective estrogen receptor modulators) that display tissue-selective pharmacology [13]. Raloxifene and tamoxifen are two clinically used SERMs for which structures are available. Crystal structures of the estrogen receptor bound to different ligands (estradiol, tamoxifen, or raloxifene) reveal that ligands of different sizes and shapes induce a spectrum of receptor conformational states. These states can be interpreted by the cellular complexion of co-regulators and the environment of the local promoter of... 

---