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Two chemicals increase the Vitamin D receptor and decrease the growth of breast cancer cells in the lab - March 2018

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

About 3X less growth of Breast Cancer

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VitaminDWiki
  • 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

300 items in Vitamin D Receptor category

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 has a poor VDR (40% of the Obese )

A poor VDR increases the risk of 53 health problems  click here for details

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:

IncreasingIncreases
1) Vitamin D supplement
  Sun, Ultraviolet -B
Vitamin D in the blood
and thus in the cells
2) MagnesiumVitamin 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
   paricalcitol, maxacalcitol?
Vitamin D Receptor
7) Quercetin (flavonoid) Vitamin D Receptor
8) Zinc is in the VDRVitamin D Receptor
9) BoronVitamin D Receptor ?,
etc
10) Essential oils e.g. ginger, curcuminVitamin D Receptor
11) ProgesteroneVitamin D Receptor
12) Infrequent high concentation Vitamin D
Increases the concentration gradient
Vitamin D in the cells

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 which help the VDR

If poor Vitamin D Receptor

Risk
increase
Health Problem
50Lyme Disease
28Leprosy - another says 3X
15Chronic Heart Failure
13Sepsis
9.6Chronic Periodontitis
   and smoke
8Juvenile Rheumatoid Arthritis
7.6Crohn's disease
7.5Respiratory Tract Infections
5.8Low back pain in athletes
5 Respiratory Distress in preemies
5Ulcerative Colitis
5Coronary Artery Disease
5Asthma Child see also 2.0 and 1.3
4.6Breast Cancer 16.9 X another study
4.1Vitiligo
4Polycystic ovary syndrome
3.6 Pneumonia - children
3.3 Pre-term birth
3.1 Colon Cancer survival
3 Multiple Sclerosis
3Dengue
3 Waist size
3 Ischemic Stroke
3Alzheimer’s
3Gestational Diabetes
2.9Hand, Foot, Mouth Disease
2.8Osteoporosis & COPD
2.7Gastric Cancer
2.6Lupus in children
2.5 Lumbar Disc Degeneration
2.4Lung Cancer
2.3Autism
2.2Juvenile idiopathic arthritis
2.1Adolescent idiopathic scoliosis in Asians
2Diabetic Retinopathy
2Parkinson's
2 Wheezing/Asthma see also 5X
2 Melanoma   Non-melanoma Skin Cancers
2Myopia
2Preeclampsia
1.9Uterine Fibroids
1.9Early tooth decay
1.8Diabetic nephropathy
1.8Sleep Apnea
1.6Diabetes - Type I
1.6Prostate Cancer while black
1.5 Diabetes -Type II
1.5Pertusus
1.5Obesity
1.4Graves Disease
1.4 Rheumatoid arthritis
1.3Childhood asthma see also 5X
1.3Psoriasis in Caucasians
1.3Tuberculosis
?? Rickets - Vitamin D resistant


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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Created by admin. Last Modification: Saturday March 17, 2018 00:46:13 GMT-0000 by admin. (Version 9)

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9529 VDR Cancer.jpg admin 16 Mar, 2018 23:23 24.48 Kb 423
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