Journal
TRENDS IN ENDOCRINOLOGY AND METABOLISM
Volume 24, Issue 1, Pages 31-39Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tem.2012.10.003
Keywords
LRP5/6; Wnt/beta-catenin; development; crystal structure; disease
Categories
Funding
- National Institutes of Health [RR024887, AR053293, GM087413]
- NATIONAL CENTER FOR RESEARCH RESOURCES [R21RR024887] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF ARTHRITIS AND MUSCULOSKELETAL AND SKIN DISEASES [R01AR053293] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM087413] Funding Source: NIH RePORTER
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Low-density lipoprotein-related receptors 5 and 6 (LRP5/6) are highly homologous proteins with key functions in canonical Wnt signaling. Alterations in the genes encoding these receptors or their interacting proteins are linked to human diseases, and as such they have been a major focus of drug development efforts to treat several human conditions including osteoporosis, cancer, and metabolic disease. Here, we discuss the links between alterations in LRP5/6 and disease, proteins that interact with them, and insights gained into their function from mouse models. We also highlight current drug development related to LRP5/6 as well as how the recent elucidation of their crystal structures may allow further refinement of our ability to target them for therapeutic benefit.
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