The DOI matches its Crossref record; 118 of the 119 references it cites were found in a registry or an index.
Development of selective androgen receptor modulators (SARMs)
Open accessAbstract
The Androgen Receptor (AR), a member of the steroid hormone receptor family, plays important roles in the physiology and pathology of diverse tissues. AR ligands, which include circulating testosterone and locally synthesized dihydrotestosterone, bind to and activate the AR to elicit their effects. Ubiquitous expression of the AR, metabolism and cross reactivity with other receptors limit broad therapeutic utilization of steroidal androgens. However, the discovery of selective androgen receptor modulators (SARMs) and other tissue-selective nuclear hormone receptor modulators that activate their cognate receptors in a tissue-selective manner provides an opportunity to promote the beneficial effects of androgens and other hormones in target tissues with greatly reduced unwanted side-effects. In the last two decades, significant resources have been dedicated to the discovery and biological characterization of SARMs in an effort to harness the untapped potential of the AR. SARMs have been proposed as treatments of choice for various diseases, including muscle-wasting, breast cancer, and osteoporosis. This review provides insight into the evolution of SARMs from proof-of-concept agents to the cusp of therapeutic use in less than two decades, while covering contemporary views of their mechanisms of action and therapeutic benefits.
Overview
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
In the citing paper
“Steiner introduced Enobosarm, Veru's investigational selective androgen receptor modulator (SARM) [30, 31].”
From Muscle Loss in Obesity Therapy as a Therapeutic Target: Trial Design and Endpoints for Regulatory Discussions (2025) · cites this paper as [30]
In the citing paper
“Putative mechanisms of SARM selectivity include tissue specific enzymes, modulated recruitment of coregulators and activation of unique subcellular signaling cascades are some of the putative mechanisms of SARM selectivity, 249 but more research is required to understand these mechanisms and then leverage these unique features to generative more efficacious therapeutics.”
From The role of the androgen receptor in the pathogenesis of obesity and its utility as a target for obesity treatments (2022) · cites this paper as [249]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Citations
Cites
The Steroid and Thyroid Hormone Receptor Superfamily
Evans, R. M. (1988) · Science · doi:10.1126/science.3283939 · Cited by 7,394
Lehmann, B. D., Bauer, J. A., Chen, X., Sanders, M. E., Chakravarthy, A. B., Shyr, Y., & Pietenpol, J. A. (2011) · Journal of Clinical Investigation · doi:10.1172/jci45014 · Cited by 5,592
MOLECULAR MECHANISMS OF ACTION OF STEROID/THYROID RECEPTOR SUPERFAMILY MEMBERS
Tsai, M., & O’Malley, B. W. (1994) · Annual Review of Biochemistry · doi:10.1146/annurev.bi.63.070194.002315 · Cited by 2,887
Shiau, A. K., Barstad, D., Loria, P. M., Cheng, L., Kushner, P. J., Agard, D. A., & Greene, G. L. (1998) · Cell · doi:10.1016/s0092-8674(00)81717-1 · Cited by 2,759
A signature motif in transcriptional co-activators mediates binding to nuclear receptors
Heery, D. M., Kalkhoven, E., Hoare, S., & Parker, M. G. (1997) · Nature · doi:10.1038/42750 · Cited by 2,128
Activation of the estrogen receptor through phosphorylation by mitogen-activated protein kinase
Kato, S., Endoh, H., Masuhiro, Y., Kitamoto, T., Uchiyama, S., Sasaki, H., Masushige, S., Gotoh, Y., Nishida, E., Kawashima, H., et al. (1995) · Science · doi:10.1126/science.270.5241.1491 · Cited by 1,964
Therapeutic Approaches to Bone Diseases
Rodan, G. A., & Martin, T. J. (2000) · Science · doi:10.1126/science.289.5484.1508 · Cited by 1,767
Population frequencies of inherited neuromuscular diseases—A world survey
Emery, A. E. H. (1991) · Neuromuscular Disorders · doi:10.1016/0960-8966(91)90039-u · Cited by 1,451
The Multifaceted Mechanisms of Estradiol and Estrogen Receptor Signaling
Hall, J. M., Couse, J. F., & Korach, K. S. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.r100029200 · Cited by 1,202
Nongenotropic, Sex-Nonspecific Signaling through the Estrogen or Androgen Receptors
Kousteni, S., Bellido, T., Plotkin, L. I., O’Brien, C. A., Bodenner, D., Li, H., Han, K., Gregorio, G. B. D., Katzenellenbogen, J. A., Katzenellenbogen, B. S., et al. (2001) · Cell · doi:10.1016/s0092-8674(01)00268-9 · Cited by 1,163
Research works printed but not linked: 1
- Ponnusamy, 2016, Tissue selective androgen receptor modulators (SARMs) increase pelvic floor muscle mass in ovariectomized mice, J. Cell Biochem.
Cited by
Sorted by citations
Sarcopenia and type 2 diabetes mellitus: a bidirectional relationship
Mesinovic, J., Zengin, A., de Courten, B. V., Ebeling, P. R., & Scott, D. S. (2019) · Diabetes Metabolic Syndrome and Obesity · doi:10.2147/dmso.s186600 · Cited by 603
Zeng, S., Huang, W., Zheng, X., Cheng, L., Zhang, Z., Wang, J., & Shen, Z. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112981 · Cited by 264
The androgen receptor is a tumor suppressor in estrogen receptor–positive breast cancer
Hickey, T. E., Selth, L. A., Chia, K. M., Laven‐Law, G., Milioli, H. H., Roden, D. L., Jindal, S., Hui, M. N., Finlay-Schultz, J., Ebrahimie, E., et al. (2021) · Nature Medicine · doi:10.1038/s41591-020-01168-7 · Cited by 261
Vignera, S. L., Cannarella, R., Condorelli, R. A., Torre, F., Aversa, A., & Calogero, A. E. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21082948 · Cited by 234
Osteosarcopenia: A case of geroscience
Kirk, B., Saedi, A. A., & Duque, G. (2019) · Aging Medicine · doi:10.1002/agm2.12080 · Cited by 178
Metadata
- Authors
- Narayanan, R., Coss, C. C., & Dalton, J. T.
- Affiliations
- University of Tennessee Health Science Center (US)
- The Ohio State University (US)
- University of Michigan (US)
- Corresponding author
- Dalton, James T.
- Venue
- Molecular and Cellular Endocrinology
- Publisher
- Elsevier BV
- Published
- 2018-04
- Volume
- 465
- Pages
- 134-142
- ISSN
- 0303-7207 (ISSN-L)
- PMC
- PMC5896569
- OpenAlex
- W2625829876
- Cited by
- 251
- References
- 119
- Citations by year
- 2026: 17 · 2025: 22 · 2024: 19 · 2023: 38 · 2022: 42 · 2021: 37 · 2020: 27 · 2019: 24 · 2018: 21
- FWCI
- 3.00
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Molecular and Cellular Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (K12CA133250)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Keywords
- selective androgen receptor modulators, androgen receptor, testosterone, dihydrotestosterone, muscle atrophy, breast cancer, osteoporosis, mechanism of action, drug development
- MeSH terms
- Androgens, Animals, Humans, Models, Biological, Organ Specificity, Receptors, Androgen
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
