Evidence map›Paper›PMID 33609553›Full record

ArticleThe Journal of investigative dermatology2021

Development of hMC1R Selective Small Agonists for Sunless Tanning and Prevention of Genotoxicity of UV in Melanocytes.

Leonid Koikov, Renny J Starner, Viki B Swope, Parth Upadhyay, Yuki Hashimoto, Katie T Freeman, James J Knittel, Carrie Haskell-Luevano, Zalfa A Abdel-Malek

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in The Journal of investigative dermatology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
2.2field-weighted citation impact, top 13% 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

10 citing papers in PubMed, 23 citations in OpenAlex.

  1. Review
  2. Article
  3. An overview of benefits and risks of chronic melanocortin-1 receptor activation.Journal of the European Academy of Dermatology and Venereology : JEADV · 2025
    Review
  4. Review
  5. Article
  6. Article
  7. Review
  8. Article
  9. Review
  10. Pharmacologic manipulation of skin pigmentation.Pigment cell & melanoma research · 2021
    Review
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

9 authors at 4 institutions in 2 countries.

Leonid KoikovDepartment of Dermatology, University of Cincinnati, Cincinnati, Ohio, USA.
Renny J StarnerDepartment of Dermatology, University of Cincinnati, Cincinnati, Ohio, USA.
Viki B SwopeDepartment of Dermatology, University of Cincinnati, Cincinnati, Ohio, USA.
Parth UpadhyayDepartment of Dermatology, University of Cincinnati, Cincinnati, Ohio, USA.
Yuki HashimotoDepartment of Dermatology, Toho University, Tokyo, Japan.
Katie T FreemanDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota, USA.
James J KnittelDepartment of Pharmaceutical and Administrative Sciences, Western New England University, Springfield, Massachusetts, USA.
Carrie Haskell-LuevanoDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota, USA.
Zalfa A Abdel-MalekDepartment of Dermatology, University of Cincinnati, Cincinnati, Ohio, USA. Electronic address: abdelmza@uc.edu.
University of Cincinnati · USUniversity of Minnesota · USToho University · JPWestern New England University · US

Funding

REPRODUCTIVE AND DEVELOPMENTAL TOXICOLOGY RESEARCHP30ES006096 · NIEHS · UNIVERSITY OF CINCINNATI · PI PINNEY, SUSAN MENGEL · 1992 to 2022
$35.4M
Melanocortin Selective LigandsR01DK091906 · NIDDK · UNIVERSITY OF MINNESOTA · PI HASKELL-LUEVANO, CARRIE · 2012 to 2015
$1.8M
Melanoma prevention by MC1R selective small peptide analogs of alpha MSHR21CA191761 · NCI · UNIVERSITY OF CINCINNATI · PI ABDEL-MALEK, ZALFA · 2015 to 2016
$406k
BLRD VA I01 BX003668NCI NIH HHS R21 CA191761NIDDK NIH HHS R01 DK091906NIEHS NIH HHS P30 ES006096
6 · The paper itself

Abstract

Activation of the human melanocortin 1 receptor (hMC1R) expressed on melanocytes by α-melanocortin plays a central role in regulating human pigmentation and reducing the genotoxicity of UV by activating DNA repair and antioxidant defenses. For the development of a hMC1R-targeted photoprotection strategy, we designed tetra- and tripeptide agonists with modifications that provide the necessary lipophilicity and hMC1R selectivity to be effective drugs. These peptides proved to be superior to most of the existing analogs of the physiological tridecapeptide α-melanocortin because of their small size and high hMC1R selectivity. Testing on primary cultures of human melanocytes showed that these peptides are highly potent with prolonged stimulation of melanogenesis, enhanced repair of UV-induced DNA photoproducts, and reduced apoptosis. One of the tripeptides, designated as LK-514 (5), with a molecular weight of 660 Da, has unprecedented (>100,000) hMC1R selectivity when compared with the other melanocortin receptors hMC3R, hMC4R, and hMC5R, and increases pigmentation (sunless tanning) in a cultured, three-dimensional skin model. These new analogs should be efficacious in preventing skin cancer, including melanoma, and treatment of skin disorders, such as vitiligo and polymorphic light eruptions.

Indexed as

alpha-MSHCells, CulturedDermatologic AgentsDNA DamageHumansMelanocytesMelanomaPhotosensitivity DisordersPrimary Cell CultureReceptor, Melanocortin, Type 1SkinSkin Diseases, GeneticSkin NeoplasmsSkin PigmentationUltraviolet RaysVitiligoalpha-MSHDermatologic AgentsMC1R protein, humanReceptor, Melanocortin, Type 1

Identifiers

PMID33609553
PMCPMC9009400
OpenAlexW3133416342

What OpenQuestion holds

Textmetadata
LicenceTDM
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.