Publications by authors named "Masayoshi Ohkuro"
Article Synopsis
- Fractalkine (FKN) is a chemokine produced by cells in bone tissue and affects monocytes/macrophages through the CX3CR1 receptor, playing a role in the survival and differentiation of osteoclast precursor cells (OCPs).
- Research indicates that FKN enhances the survival and differentiation of OCPs into osteoclasts when paired with RANKL stimulation, with effects varying based on the presence or absence of the CX3CR1 receptor.
- Targeting the FKN-CX3CR1 pathway may offer new therapeutic options for treating noninflammatory bone loss diseases, as shown by reduced RANKL-induced bone loss in mouse models with anti-FKN antibody treatment.
Article Synopsis
- The study aimed to understand how the fractalkine (FKN)/CX CR1 pathway contributes to joint damage in rheumatoid arthritis.
- Researchers tested the effects of an anti-mouse FKN monoclonal antibody on joint destruction and the migration of osteoclast precursors in a collagen-induced arthritis mouse model.
- Results showed that treatment with this antibody significantly reduced arthritis severity, joint damage, and the migration of bone marrow-derived osteoclast precursors, indicating that targeting the FKN/CX CR1 pathway might offer new treatment options for rheumatoid arthritis.
Article Synopsis
- Inflammatory bowel disease (IBD) includes conditions like ulcerative colitis and Crohn's disease, which are marked by chronic inflammation in the intestines due to leukocyte adhesion facilitated by integrins.
- Calreticulin (CRT) plays a role in this process by activating integrin α subunits, but its exact relationship with IBD is not well understood.
- A new small molecule, ER-464195-01, has been found to inhibit CRT's interaction with integrins, reducing inflammation and leukocyte infiltration in IBD mouse models, suggesting a potential new treatment approach.
E6005, a potent, selective phosphodiesterase (PDE) 4 inhibitor, has been developed as a novel topical agent of atopic dermatitis (AD). It has been shown to inhibit itching in patients with AD as well in mouse models. To study the mechanism underlying the anti-pruritic effect of E6005, we examined its effect on the activation of dorsal root ganglion (DRG) neurons associated with the itch sensation.
View Article and Find Full Text PDFDuring the development of autoimmune and inflammatory diseases, infiltration by multiple leukocyte types is commonly observed at the site of inflammation. These cells are chemotactically recruited via activated integrins expressed on their cell surfaces. However, the detailed mechanism of integrin activation has not been fully elucidated.
View Article and Find Full Text PDFNovel piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4]benzothiazine were prepared and evaluated for their inhibitory activity on the upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1). Replacement of the methanesulfonyl group on the piperidine ring of previously prepared derivatives with a carboxylic acid-containing moiety resulted in a number of potent adhesion molecule inhibitors. Of these, (anti) [3-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-yl)methyl-3-azabicyclo[3.
View Article and Find Full Text PDFDuring a search for novel, orally-active inhibitors of upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1), we found a new series of 10H-pyrazino[2,3-b][1,4]benzothiazine derivatives to be potent ICAM-1 inhibitors. Of these compounds, N-[1-(10H-Pyrazino[2,3-b][1,4]benzothiazin-8-ylmethyl)piperidin-4-yl]-N',N'-dimethylsulfamide 7p showed the potent oral inhibitory activities against neutrophil migration in a murine interleukin-1 (IL-1) induced paw inflammation model. The synthesis and structure-activity relationships of these amide derivatives are described.
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