Abstract:
:Over the last couple of decades, the PPAR family of transcription factors has received much attention from the pharmaceutical industry due to their profound ability to improve glucose and lipid metabolism upon agonist activation. However, more recently the interest in these nuclear receptors has faded because several clinical trials have shown that it is difficult to develop a ligand that significantly ameliorates glucose and lipid metabolism disorders without concomitantly inducing unacceptable side-effects. Nevertheless, the data also suggests that tissue specific targeting could pave the way to renewed interest and clinical use of PPAR ligands. In this review we summarize the results and learnings from the clinical trials on PPAR agonism and discuss the possibilities for tissue targeting of PPAR ligands by using state of the art technology to fuse them to peptides homing selectively to tissues expressing the cognate surface receptor.
journal_name
Biochimiejournal_title
Biochimieauthors
Bugge A,Holst Ddoi
10.1016/j.biochi.2016.10.017subject
Has Abstractpub_date
2017-05-01 00:00:00pages
100-104eissn
0300-9084issn
1638-6183pii
S0300-9084(16)30206-1journal_volume
136pub_type
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