Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents
J. Med. Chem., DOI: 10.1021/acs.jmedchem.8b00106
- These appear to be the first man-made chemicals which increase the Vitamin D receptor, which in-turn increases the amount of Vitamin D which actually gets to cells.
- A great many diseases are associated with poor vitamin D receptors
- You can test the Vitamin D receptor in your mouth as very low cost
- So far there are 7 known ways to increase the Vitamin D receptor (see below)
I am doing 6 of them
- I do not know if the same chemical can increase Vitamin D Receptors for other than breast cancers
- I do not know if the same chemical can increase Vitamin D Receptors for other health problems
- I wonder if people with poor vitamin D receptors could have a good or better benefit from using some of the 7 ways to increase VDR, taking more Vitamin D, and reducing Calcium supplementation
- Henry Lahore, founder of VitaminDWiki
Vitamin D Receptor category has the following
Vitamin D tests cannot detect Vitamin D Receptor (VDR) problems
A poor VDR restricts Vitamin D from getting in the cells
It appears that 30% of the population have a poor VDR (40% of the Obese )
Several diseases protect themselves by deactivating the Vitamin D receptor.Example: Breast Cancer
A poor VDR is associated with the risk of 55 health problems click here for details
The risk of 44 diseases at least double with poor VDR as of Oct 2019 click here for details
Some health problem, such as Breast Cancer reduce the VDR
VDR at-home test $29 - results not easily understood in 2016
There are hints that you may have inherited a poor VDR
Compensate for poor VDR by increasing one or more:
|1) Vitamin D supplement|
Sun, Ultraviolet -B
| Vitamin D in the blood |
and thus in the cells
|2) Magnesium||Vitamin D in the blood |
AND in the cells
|3) Omega-3||Vitamin D in the cells|
|4) Resveratrol||Vitamin D Receptor|
|5) Intense exercise||Vitamin D Receptor|
|6) Get prescription for VDR activator|
|Vitamin D Receptor|
|7) Quercetin (flavonoid)||Vitamin D Receptor|
|8) Zinc is in the VDR||Vitamin D Receptor|
|9) Boron||Vitamin D Receptor ?, |
|10) Essential oils e.g. ginger, curcumin||Vitamin D Receptor|
|11) Progesterone||Vitamin D Receptor|
|12) Infrequent high concentration Vitamin D|
Increases the concentration gradient
|Vitamin D in the cells|
|13) Sulfroaphane and perhaps sulfur||Vitamin D Receptor|
Note: If you are not feeling enough benefit from Vitamin D, you might try increasing VDR activation. You might feel the benefit within days of adding one or more of the above
Far healthier and stronger at age 72 due to supplements Includes 6 supplements that help the VDR
Increased risk associated with a poor Vitamin D Receptor
Meixi Hao† , Siyuan Hou†, Lingjing Xue, Haoliang Yuan , Lulu Zhu, Cong Wang, Bin Wang, Chunming Tang, and Can Zhang, zhangcan at cpu.edu.cn.
- State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Center of Drug Discovery, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China
The vitamin D3 receptor (VDR), which belongs to the nuclear-receptor superfamily, is a potential molecular target for anticancer-drug discovery. In this study, a series of nonsteroidal vitamin D mimics with phenyl-pyrrolyl pentane skeletons with therapeutic potentials in cancer treatment were synthesized.
Among them, 11b and 11g were identified as the most effective agents in reducing the viability of four cancer-cell lines, particularly those of breast-cancer cells, with IC50 values in the submicromolar-concentration range. In addition, 11b and 11g possessed VDR-binding affinities and displayed significant partial VDR-agonistic activities determined by dual-luciferase-reporter assays and human-leukemia-cell-line (HL-60)-differentiation assays.
Furthermore, 11b and 11g inhibited tumor growth in an orthotopic breast-tumor model via inhibition of cell proliferation and induction of cell apoptosis.
More importantly, 11b and 11g exhibited favorable pharmacokinetic behavior in vivo and did not increase serum calcium levels or cause any other apparent side effects.
In summary, 11b and 11g act as novel VDR modulators and may be promising candidates for cancer chemotherapy.
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