Evidence map›Paper›PMID 16528410›Full record

ArticleThe Journal of clinical investigation2006

Identification and characterization of noncalcemic, tissue-selective, nonsecosteroidal vitamin D receptor modulators.

Yanfei Ma, Berket Khalifa, Ying K Yee, Jianfen Lu, Ai Memezawa, Rajesh S Savkur, Yoko Yamamoto, Subba R Chintalacharuvu, Kazuyoshi Yamaoka, Keith R Stayrook and 10 more

Open access · bronzeAbstract read
In one paragraph

Article in The Journal of clinical investigation, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed
8.2field-weighted citation impact, top 2% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

29 citing papers in PubMed, 118 citations in OpenAlex.

  1. Trial
  2. Article
  3. Article
  4. Article
  5. Article
  6. Is There a Role of Vitamin D in Alzheimer's Disease?CNS & neurological disorders drug targets · 2024
    Review
  7. Article
  8. Review
  9. Vitamin D in Neurological Diseases.International journal of molecular sciences · 2022
    Review
  10. Review
  11. Review
  12. Update on pharmacologically-relevant vitamin D analogues.British journal of clinical pharmacology · 2019
    Review
  13. Article
  14. Article
  15. Review
  16. Article
  17. Review
  18. Review
  19. Natural compounds as anticancer agents: Experimental evidence.World journal of experimental medicine · 2012
    Review
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

20 authors at 1 institution in 1 country.

Yanfei MaLilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
Berket Khalifa
Ying K Yee
Jianfen Lu
Ai Memezawa
Rajesh S Savkur
Yoko Yamamoto
Subba R Chintalacharuvu
Kazuyoshi Yamaoka
Keith R Stayrook
Kelli S Bramlett
Qing Q Zeng
Srinivasan Chandrasekhar
Xiao-Peng Yu
Jared H Linebarger
Stephen J Iturria
Thomas P Burris
Shigeaki Kato
William W Chin
Sunil Nagpal
Eli Lilly (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of skin, prostate, colon, and breast as well as leukemia. However, the major side effect of VDR ligands that limits their expanded use and clinical development is hypercalcemia that develops as a result of the action of these compounds mainly on intestine. In order to discover VDR ligands with less hypercalcemia liability, we sought to identify tissue-selective VDR modulators (VDRMs) that act as agonists in some cell types and lack activity in others. Here, we describe LY2108491 and LY2109866 as nonsecosteroidal VDRMs that function as potent agonists in keratinocytes, osteoblasts, and peripheral blood mononuclear cells but show poor activity in intestinal cells. Finally, these nonsecosteroidal VDRMs were less calcemic in vivo, and LY2108491 exhibited more than 270-fold improved therapeutic index over the naturally occurring VDR ligand 1,25-dihydroxyvitamin D3 [1,25-(OH)2D3] in an in vivo preclinical surrogate model of psoriasis.

Indexed as

AcetatesAnimalsArylsulfonatesCaco-2 CellsCalcitriolCell ProliferationCells, CulturedColonic NeoplasmsDose-Response Relationship, DrugDrug Evaluation, PreclinicalFemaleHumansHypercalcemiaIntestinesKeratinocytesLigandsAcetatesArylsulfonatesCalcitrioldihydroxy-vitamin D3LigandsLY 2108491LY 2109866Receptors, CalcitriolThiophenesVitamin D

Identifiers

PMID16528410
PMCPMC1395481
OpenAlexW2161765602

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.