11-beta-chloromethyl-estradiol (11β-CME) is a synthetic analog of estradiol, a naturally occurring female sex hormone. It's important in research because it possesses a unique combination of properties that makes it a valuable tool for studying estrogen receptors (ERs) and their role in various biological processes.
Here's why 11β-CME is significant for research:
**1. Selective ERα Agonist:** 11β-CME acts as a selective agonist for estrogen receptor alpha (ERα), meaning it preferentially binds to and activates ERα while having minimal or no activity on estrogen receptor beta (ERβ). This selectivity allows researchers to study the specific effects mediated by ERα, excluding the influence of ERβ.
**2. Non-steroidal Structure:** Unlike estradiol, 11β-CME is not a steroid molecule. This non-steroidal structure grants it some advantages:
* **Increased Stability:** It is more stable than estradiol, potentially extending its half-life and allowing for longer-lasting effects.
* **Improved Permeability:** It can potentially cross cell membranes more readily, making it more accessible to target tissues.
**3. Potential Applications in Research:**
* **ERα-mediated Signaling Pathways:** Understanding how 11β-CME interacts with and activates ERα provides insight into the downstream signaling pathways involved in various biological processes, including:
* **Cellular proliferation:** Estrogen is known to influence cell growth and division.
* **Bone metabolism:** Estrogen plays a crucial role in bone health and density.
* **Cardiovascular function:** Estrogen can impact blood vessel function and cardiovascular health.
* **Neurological processes:** Estrogen has been linked to mood regulation, cognition, and neuroprotection.
* **Development of ERα-targeted Therapies:** By understanding the specific actions of 11β-CME, researchers might be able to develop new drugs that target ERα for treating various diseases. This could include conditions related to estrogen deficiency, like osteoporosis, or conditions where ERα is implicated in disease progression, like certain cancers.
**However, it's important to note that 11β-CME is a research tool, not a therapeutic agent.** Its safety and efficacy in humans haven't been established.
In summary, 11β-CME is a valuable tool for research due to its selectivity for ERα, its non-steroidal structure, and its potential applications in investigating ERα-mediated signaling pathways and developing novel therapies.
ID Source | ID |
---|---|
PubMed CID | 67088 |
CHEMBL ID | 175602 |
CHEBI ID | 34142 |
SCHEMBL ID | 8746070 |
MeSH ID | M0116929 |
Synonym |
---|
11beta-chloromethylestradiol |
org 4333 |
71794-60-0 |
(8s,9r,11s,13s,14s,17s)-11-(chloromethyl)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol |
CHEMBL175602 |
chebi:34142 , |
unii-brp4dw4see |
brp4dw4see , |
estra-1,3,5(10)-triene-3,17-diol, 11-(chloromethyl)-, (11beta,17beta)- |
org-4333 |
11-beta-chloromethyl-estradiol |
SCHEMBL8746070 |
11beta-chloromethylestra-1,3,5(10)-trien-3,17beta-diol |
DTXSID40992450 |
Q27115844 |
estra-1,3,5(10)-triene-3,17-diol, 11-(chloromethyl)-, (11.beta.,17.beta.)- |
11.beta.-cme2 |
11.beta.-chloromethylestradiol |
(11.beta.,17.beta.)-11-(chloromethyl)estra-1,3,5(10)-triene-3,17-diol |
Class | Description |
---|---|
3-hydroxy steroid | Any hydroxy steroid carrying a hydroxy group at position 3. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID69391 | Binding affinity against estrogen receptor was determined by using [3H]estradiol as radioligand in competitive radiometric binding assay | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22 | Ligands for the estrogen receptor, containing cyclopentadienyltricarbonylrhenium units. |
AID69390 | Binding affinity against estrogen receptor was determined by using [3H]estradiol as radioligand in competitive radiometric binding assay | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22 | Ligands for the estrogen receptor, containing cyclopentadienyltricarbonylrhenium units. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 4 (66.67) | 18.7374 |
1990's | 1 (16.67) | 18.2507 |
2000's | 1 (16.67) | 29.6817 |
2010's | 0 (0.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.12) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 7 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |