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Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516.
Lagu, Bharat; Kluge, Arthur F; Goddeeris, Matthew M; Tozzo, Effie; Fredenburg, Ross A; Chellur, Shekar; Senaiar, Ramesh S; Jaleel, Mahaboobi; Babu, D Ravi Krishna; Tiwari, Nirbhay K; Takahashi, Taisuke; Patane, Michael A.
Affiliation
  • Lagu B; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States. Electronic address: blagu@mitobridge.com.
  • Kluge AF; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States.
  • Goddeeris MM; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States.
  • Tozzo E; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States.
  • Fredenburg RA; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States.
  • Chellur S; Aurigene Discovery Technologies, Ltd., Bengaluru, Karnataka, India.
  • Senaiar RS; Aurigene Discovery Technologies, Ltd., Bengaluru, Karnataka, India.
  • Jaleel M; Aurigene Discovery Technologies, Ltd., Bengaluru, Karnataka, India.
  • Babu DRK; Aurigene Discovery Technologies, Ltd., Bengaluru, Karnataka, India.
  • Tiwari NK; Aurigene Discovery Technologies, Ltd., Bengaluru, Karnataka, India.
  • Takahashi T; Astellas Pharma, Tsukuba, Japan.
  • Patane MA; Mitobridge, Inc., 1030 Massachusetts Ave., Cambridge, MA 02138, United States.
Bioorg Med Chem Lett ; 28(3): 533-536, 2018 02 01.
Article in En | MEDLINE | ID: mdl-29275935
Compound 1 regulates significantly fewer genes than the PPARδ modulator, GW501516. Both compounds are efficacious in a thermal injury model of muscle regeneration. The restricted gene profile of 1 relative to GW501516 suggests that 1 may be pharmacoequivalent to GW501516 with fewer PPAR-related safety concerns.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiazoles / PPAR delta Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Country of publication: United kingdom
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiazoles / PPAR delta Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Country of publication: United kingdom