Prohibitin-targeting peptide 1

Prohibitin-targeting peptide 1 (also known as prohibitin-TP01 and TP01; trade name Adipotide) is a peptidomimetic with sequence CKGGRAKDC-GG-D(KLAKLAK)2. It is an experimental proapoptotic drug[1] that has been shown to cause rapid weight loss in mice[2] and rhesus monkeys.[3] Its mechanism of action is to target specific blood vessels supplying adipose tissue with blood, cause the vessels to shrink and the fat cells fed by those vessels to undergo apoptosis.[4] TP01 is designed to bind to two receptors, ANXA2 and prohibitin, that are specific to blood vessels supplying white adipose tissue.[5]

Prohibitin-targeting peptide 1
Clinical data
Trade namesAdipotide
Other namesProhibitin-TP01; TP01
Legal status
Legal status
  • Investigational

As of 2019, clinical development has been discontinued.[6]

References
  1. "Prohibitin-targeting peptide 1". NCI Drug Dictionary. National Cancer Institutes.
  2. Kolonin, Mikhail G; Saha, Pradip K; Chan, Lawrence; Pasqualini, Renata; Arap, Wadih (2004). "Reversal of obesity by targeted ablation of adipose tissue". Nature Medicine. Nature Publishing Group. 10 (6): 625–632. doi:10.1038/nm1048. PMID 15133506.
  3. "Blood vessel mapping reveals four new 'ZIP codes'". medicalxpress. 24 October 2011. Retrieved 10 November 2011.
  4. Barnhart, K. F.; Christianson, D. R.; Hanley, P. W.; Driessen, W. H. P.; Bernacky, B. J.; Baze, W. B.; Wen, S.; Tian, M.; Ma, J.; Kolonin, M. G.; Saha, P. K.; Do, K. A.; Hulvat, J. F.; Gelovani, J. G.; Chan, L.; Arap, W.; Pasqualini, R. (2011). "A peptidomimetic targeting white fat causes weight loss and improved insulin resistance in obese monkeys". Science Translational Medicine. 3 (108): 108ra112. doi:10.1126/scitranslmed.3002621. PMC 3666164. PMID 22072637.
  5. Staquicini, Fernanda I.; Cardó-Vila, Marina; Kolonin, Mikhail G.; Trepel, Martin; Edwards, Julianna K.; Nunes, Diana N.; Sergeeva, Anna; Efstathiou, Eleni; Sun, Jessica; Almeida, Nalvo F.; Tu, Shi-Ming; Botz, Gregory H.; Wallace, Michael J.; O’Connell, David J.; Krajewski, Stan; Gershenwald, Jeffrey E.; Molldrem, Jeffrey J.; Flamm, Anne L.; Koivunen, Erkki; Pentz, Rebecca D.; Dias-Neto, Emmanuel; Setubal, João C.; Cahill, Dolores J.; Troncoso, Patricia; Do, Kim-Ahn; Logothetis, Christopher J.; Sidman, Richard L.; Pasqualini, Renata; Arap, Wadih (2011). "Vascular ligand-receptor mapping by direct combinatorial selection in cancer patients". Proceedings of the National Academy of Sciences of the United States of America. 108: 18637–18642. doi:10.1073/pnas.1114503108. PMC 3219136. PMID 22049339. Retrieved 10 November 2011.
  6. "Prohibitin targeting peptide 1". Adis Insight.
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