29-06-2016, 04:21 AM
Well my friends, there's a " NEW " estrogen receptor in town named ER-X (estrogen receptor X). Now here's the thing, this ER-X is slightly imperious to anti-estrogens, is that good?? let's find out. A quick note about some alternative research I've meant to follow up on:
1) estrogen and androgens occupy the same receptor (that's a big deal)
2) prediction- a super estrogen receptor type will be discovered, my thought is that the homology of estrogens receptors slip in/out of each receptor type, now what influences this reaction between them I don't know yet, it's certainly intriguing though. (Yup, I've lost my mind lol).
Membrane estrogen receptors - is it an alternative way of estrogen action?
Review article
Soltysik K, et al. J Physiol Pharmacol. 2013.
Show full citation
Abstract
The functions of estrogens are relatively well known, however the molecular mechanism of their action is not clear. The classical pathway of estrogen action is dependent on ERα and ERβ which act as transcription factors. The effects of this pathway occur within hours or days. In addition, so-called, non-classical mechanism of steroid action dependent on membrane estrogen receptors (mER) was described. In this mechanism the effects of estrogen action are observed in a much shorter time. Here we review the structure and cellular localization of mER, molecular basis of non-classical mER action, physiological role of mER as well as implications of mER action for cancer biology. Finally, some concerns about the new estrogen receptor - GPER and candidates for estrogen receptors - ER-X and ERx, are briefly discussed. It seems that mER is a complex containing signal proteins (signalosome), as IGF receptor, EGF receptor, Ras protein, adaptor protein Shc, non-receptor kinase c-Src and PI-3K, what rationalizes production of second messengers. Some features of membrane receptors are almost identical if compared to nuclear receptors. Probably, membrane and nuclear estrogen receptors are not separate units, but rather the components of a complex mechanism in which they both cooperate with each other. We conclude that the image of the estrogen receptor as a simple transcription factor is a far-reaching simplification. A better understanding of the mechanisms of estrogen action will help us to design more effective drugs affecting signal pathways depending on both membrane and nuclear receptors.
PMID 23756388 [PubMed - indexed for MEDLINE]
1) estrogen and androgens occupy the same receptor (that's a big deal)
2) prediction- a super estrogen receptor type will be discovered, my thought is that the homology of estrogens receptors slip in/out of each receptor type, now what influences this reaction between them I don't know yet, it's certainly intriguing though. (Yup, I've lost my mind lol).
Membrane estrogen receptors - is it an alternative way of estrogen action?
Review article
Soltysik K, et al. J Physiol Pharmacol. 2013.
Show full citation
Abstract
The functions of estrogens are relatively well known, however the molecular mechanism of their action is not clear. The classical pathway of estrogen action is dependent on ERα and ERβ which act as transcription factors. The effects of this pathway occur within hours or days. In addition, so-called, non-classical mechanism of steroid action dependent on membrane estrogen receptors (mER) was described. In this mechanism the effects of estrogen action are observed in a much shorter time. Here we review the structure and cellular localization of mER, molecular basis of non-classical mER action, physiological role of mER as well as implications of mER action for cancer biology. Finally, some concerns about the new estrogen receptor - GPER and candidates for estrogen receptors - ER-X and ERx, are briefly discussed. It seems that mER is a complex containing signal proteins (signalosome), as IGF receptor, EGF receptor, Ras protein, adaptor protein Shc, non-receptor kinase c-Src and PI-3K, what rationalizes production of second messengers. Some features of membrane receptors are almost identical if compared to nuclear receptors. Probably, membrane and nuclear estrogen receptors are not separate units, but rather the components of a complex mechanism in which they both cooperate with each other. We conclude that the image of the estrogen receptor as a simple transcription factor is a far-reaching simplification. A better understanding of the mechanisms of estrogen action will help us to design more effective drugs affecting signal pathways depending on both membrane and nuclear receptors.
PMID 23756388 [PubMed - indexed for MEDLINE]