Tu1864 A Novel Orally Active Phosphatidylinositol 3-Phosphate 5-Kinase (Pikfyve) Inhibitor Ameliorates Mouse Colitis by Inhibition of IL-12 and IL-23 Production From Macrophages

Andou, Ayatoshi; Yamamoto, Takashi; Agung, Eviryanti; Seki, Yukie; Nishio, Hisahide; Shuto, Manami; Noguchi, Misato; Shima, Yoichiro; Takeshita, Sen; Yokoyama, Ryohei; Hayakawa, Nobuhiko; Noguchi, Masatsugu; Kageyama, Shunsuke; Eda, Hiroyuki; Shiozaki, Makoto; Tanabe, Itsuya; Nakagawa, Ryusuke; Sakurai, K.; Miyake, Shoji

doi:10.1016/s0016-5085(12)63351-4

Cited by 2 publications

(1 citation statement)

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“…Although initially promising, a phase 2 trial of apilimod in 220 patients with active Crohn’s disease failed to show benefit over placebo, although was well tolerated ( 278 ). A novel PIKfyve inhibitor, APY0201, administered orally ameliorated intestinal inflammation in the IL10 −/− cell transfer model and showed effects in vitro on IL-12/23 production in macrophages ( 279 ). A more in depth understanding of the PIKfyve pathway may yet yield opportunities for reducing intestinal inflammation.…”

Section: Modification Of Prr Signaling In the Management Of Intestinamentioning

confidence: 99%

Emerging Mechanisms of Innate Immunity and Their Translational Potential in Inflammatory Bowel Disease

et al. 2018

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Activation of the innate immune system through pattern-recognition receptor (PRR) signaling plays a pivotal role in the early induction of host defense following exposure to pathogens. Loss of intestinal innate immune regulation leading aberrant immune responses has been implicated in the pathogenesis of inflammatory bowel disease (IBD). The precise role of PRRs in gut inflammation is not well understood, but considering their role as bacterial sensors and their genetic association with IBD, they likely contribute to dysregulated immune responses to the commensal microbiota. The purpose of this review is to evaluate the emerging functions of PRRs including their functional cross-talk, how they respond to mitochondrial damage, induce mitophagy or autophagy, and influence adaptive immune responses by interacting with the antigen presentation machinery. The review also summarizes some of the recent attempts to harness these pathways for therapeutic approaches in intestinal inflammation.

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Section: Modification Of Prr Signaling In the Management Of Intestinamentioning

confidence: 99%

Emerging Mechanisms of Innate Immunity and Their Translational Potential in Inflammatory Bowel Disease

et al. 2018

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Structure–activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201

Hayakawa

Noguchi

Takeshita

et al. 2014

Bioorganic & Medicinal Chemistry

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Tu1864 A Novel Orally Active Phosphatidylinositol 3-Phosphate 5-Kinase (Pikfyve) Inhibitor Ameliorates Mouse Colitis by Inhibition of IL-12 and IL-23 Production From Macrophages

Cited by 2 publications

References 0 publications

Emerging Mechanisms of Innate Immunity and Their Translational Potential in Inflammatory Bowel Disease

Emerging Mechanisms of Innate Immunity and Their Translational Potential in Inflammatory Bowel Disease

Structure–activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201

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