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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Hemopressin as a breakthrough for the cannabinoid field

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Heimann, Andrea S. [1] ; Dale, Camila S. [2] ; Guimaraes, Francisco S. [3, 4] ; Reis, Ricardo A. M. [5] ; Navon, Ami [6] ; Shmuelov, Michal A. [6] ; Rioli, Vanessa [7] ; Gomes, Ivone [8] ; Devi, Lakshmi L. [8] ; Ferro, Emer S. [9, 6]
Total Authors: 10
[1] Proteimax Israel Biotechnol, IL-7610001 Rehovot - Israel
[2] Univ Sao Paulo, Biomed Sci Inst, Dept Anat, BR-05508000 Sao Paulo, SP - Brazil
[3] Univ Sao Paulo, Ribeirao Preto Med Sch, Dept Pharmacol, BR-14025600 Ribeirao Preto, SP - Brazil
[4] Univ Sao Paulo, Ribeirao Preto Med Sch, Dept Neurosci & Behav, BR-14025600 Ribeirao Preto, SP - Brazil
[5] Rio de Janeiro Fed Univ, Inst Biophys Carlos Chagas Filho, Lab Neurochem, BR-21949900 Rio De Janeiro, RJ - Brazil
[6] Weizmann Inst Sci, Dept Biol Regulat, IL-7610001 Rehovot - Israel
[7] Butantan Inst, Ctr Toxins Immune Response & Cell Signaling CETIC, Special Lab Appl Toxinol LETA, BR-05503900 Sao Paulo - Brazil
[8] Icahn Sch Med Mt Sinai, Dept Pharmacol Sci, New York, NY 10029 - USA
[9] Univ Sao Paulo, Biomed Sci Inst, Dept Pharmacol, BR-05508000 Sao Paulo, SP - Brazil
Total Affiliations: 9
Document type: Review article
Source: Neuropharmacology; v. 183, FEB 1 2021.
Web of Science Citations: 0

Hemopressin (PVNFKFLSH in rats, and PVNFKLLSH in humans and mice), a fragment derived from the alpha-chain of hemoglobin, was the first peptide described to have type 1 cannabinoid receptor activity. While hemopressin was shown to have inverse agonist/antagonistic activity, extended forms of hemopressin (i.e. RVD-hemopressin, also called pepcan-12) exhibit type 1 and type 2 cannabinoid receptor agonistic/allosteric activity, and recent studies suggest that they can activate intracellular mitochondrial cannabinoid receptors. Therefore, hemopressin and hemopressin-related peptides could have location-specific and biased pharmacological action, which would increase the possibilities for fine-tunning and broadening cannabinoid receptor signal transduction. Consistent with this, hemopressins were shown to play a role in a number of physiological processes including antinociceptive and anti-inflammatory activity, regulation of food intake, learning and memory. The shortest active hemopressin fragment, NFKF, delays the first seizure induced by pilocarpine, and prevents neurodegeneration in an experimental model of autoimmune encephalomyelitis. These functions of hemopressins could be due to engagement of both cannabinoid and non-cannabinoid receptor systems. Self-assembled nanofibrils of hemopressin have pH-sensitive switchable surface-active properties, and show potential as inflammation and cancer targeted drug-delivery systems. Upon disruption of the self-assembled hemopressin nanofibril emulsion, the intrinsic analgesic and anti-inflammatory properties of hemopressin could help bolster the therapeutic effect of anti-inflammatory or anti-cancer formulations. In this article, we briefly review the molecular and behavioral pharmacological properties of hemopressins, and summarize studies on the intricate and unique mode of generation and binding of these peptides to cannabinoid receptors. Thus, the review provides a window into the current status of hemopressins in expanding the repertoire of signaling and activity by the endocannabinoid system, in addition to their new potential for pharmaceutic formulations. (AU)

FAPESP's process: 16/04000-3 - Pharmacology of oligopeptidases and intracellular peptides
Grantee:Emer Suavinho Ferro
Support type: Research Projects - Thematic Grants
FAPESP's process: 19/06982-6 - Characterization and development of new modulators of the TrkA and PKMzeta pathways in inflammatory and chronic pain
Grantee:Deborah Schechtman
Support type: Research Projects - Thematic Grants
FAPESP's process: 17/24304-0 - New perspectives in the use of drugs that modify atypical neurotransmitters in the treatment of neuropsychiatric disorders
Grantee:Francisco Silveira Guimaraes
Support type: Research Projects - Thematic Grants