Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamine

Histamine Receptors as Potential Therapeutic Targets for Cancer Drug Development

“…Furthermore, the H 3 R was not detected in intestinal tissue (Sander et al, 2006). This data was further confirmed by Boer K et al, that also demonstrated a decreased of H 1 R and H 4 R protein levels in colorectal cancer while the levels of the H 2 R were not modified compared to normal colon mucosa (Boer et al, 2008). It was described that the H 1 R antagonist, loratadine, inhibited proliferation and enhanced radiosensitivity in human colon cancer cells (Soule et al, 2010).…”

“…Furthermore, JNJ7777120 inhibited the cell growth induced by histamine in three different human colon cancer cell lines and also inhibited the histamine-mediated increase in VEGF in two cell lines. Combined treatment with zolantidine (an H 2 R antagonist) and JNJ7777120 determined an additive effect on reducing the histamine-induced VEGF production and histamine-stimulated proliferation , suggesting the involvement of H 4 R in colon carcinogenesis (Boer et al, 2008).…”

Identification of histamine receptors in the canine gastrointestinal tract

“…1,5 H2 receptors have been documented in breast cancer cells and significantly altered populations of H1, H2, and H4 receptors have been detected in colorectal cancers. 66 Decreased expression of the H4 receptor has been noted in colorectal carcinoma. 67 H2 antagonism has been shown to decrease growth of some tumor cell lines.…”

The Histamine H4 Receptor: A Novel Target for Safe Anti-inflammatory Drugs?

“…74 Recent studies have evidenced the presence of H 4 Rs in gastric and colorectal tumor cells and a reduction of H 4 R density has been observed, which parallels the cancer progression. 54,55,56 However, functional data with histamine and H 4 R ligands are contradictory, with both stimulation and/or inhibition of cell proliferation and cell growth being observed.…”

“…39,[55][56] Cell types expressing H 4 R include immune and inflammatory cells, epithelial cells and neurons of the myenteric and submucous plexus. Interestingly, H 4 R expression was found in ghrelin-producing cells of the rat stomach, 37 leading to speculation about a possible role of histamine in the secretion of the orexigenic peptide.…”