Search Results - "Shiokawa, Zenyu"
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Discovery of a Novel Scaffold as an Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Based on the Pyrrolopiperazinone Alkaloid, Longamide B
Published in ChemMedChem (16-12-2016)“…Indoleamine 2,3‐dioxygenase 1 (IDO1) has emerged as a key target for cancer therapy, as IDO1 plays a critical role in the capacity of tumor cells to evade the…”
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Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: Modification of the core skeleton for improved solubility
Published in Bioorganic & medicinal chemistry (15-09-2012)“…We recently reported the discovery of the novel pyrrolo[3,2-c]quinoline-4-one derivative 1 as a potent inhibitor of Hedgehog (Hh) pathway signaling. However,…”
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Discovery of pyrrolo[3,2-c]quinoline-4-one derivatives as novel hedgehog signaling inhibitors
Published in Bioorganic & medicinal chemistry (15-09-2012)“…The Hedgehog (Hh) signaling pathway plays a significant role in the regulation of cell growth and differentiation during embryonic development. Since…”
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Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2‑a]pyrazine Scaffold as a Novel Proline Mimetic
Published in Journal of medicinal chemistry (14-02-2013)“…To develop novel inhibitor of apoptosis (IAP) proteins antagonists, we designed a bicyclic octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline…”
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Design, stereoselective synthesis, and biological evaluation of novel tri-cyclic compounds as inhibitor of apoptosis proteins (IAP) antagonists
Published in Bioorganic & medicinal chemistry (15-09-2013)“…We recently reported the discovery of octahydropyrrolo[1,2-a]pyrazine A as a lead compound for an inhibitor of apoptosis proteins (IAP) antagonist. To develop…”
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Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist
Published in Journal of medicinal chemistry (14-02-2019)“…Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide a novel class of immune-activating anticancer drugs via activation…”
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Gene Signature-Based Approach Identified MEK1/2 as a Potential Target Associated With Relapse After Anti-TNFα Treatment for Crohn's Disease
Published in Inflammatory bowel diseases (18-05-2018)“…Abstract Background Anti-tumor necrosis factor alpha (anti-TNFα) therapy has become the mainstay of therapy for Crohn's disease (CD). However, post-therapy,…”
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8
Discovery of a Novel Scaffold as an Indoleamine 2,3-Dioxygenase1 (IDO1) Inhibitor Based on the Pyrrolopiperazinone Alkaloid, LongamideB
Published in ChemMedChem (01-12-2016)“…Indoleamine 2,3-dioxygenase1 (IDO1) has emerged as a key target for cancer therapy, as IDO1 plays a critical role in the capacity of tumor cells to evade the…”
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Gene Signature-Based Approach Identified MEK1/2 as a Potential Target Associated With Relapse After Anti-TNF[alpha] Treatment for Crohn's Disease
Published in Inflammatory bowel diseases (01-06-2018)“…Background: Anti-tumor necrosis factor alpha (anti-TNF[alpha]) therapy has become the mainstay of therapy for Crohn's disease (CD). However, post-therapy, the…”
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Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells
Published in Bioorganic & medicinal chemistry (15-12-2013)“…We previously reported octahydropyrrolo[1,2-a]pyrazine derivative 2 (T-3256336) as a potent antagonist for inhibitors of apoptosis (IAP) proteins. Because…”
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Synthesis and evaluation of hedgehog signaling inhibitor with novel core system
Published in Bioorganic & medicinal chemistry (01-08-2015)“…[Display omitted] As we previously reported, N-methylpyrrolo[3,2-c]pyridine derivatives 1 (TAK-441) was discovered as a clinical candidate of hedgehog (Hh)…”
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Synthesis of peptidoglycan fragments and evaluation of their biological activity
Published in Organic & biomolecular chemistry (21-01-2006)“…The peptidoglycan (PG) bacterial cell wall glycoconjugate has been well known as a strong immunopotentiator. Partial structures of PG were chemically…”
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Multimeric bivalent immunogens from recombinant tetanus toxin HC fragment, synthetic hexasaccharides, and a glycopeptide adjuvant
Published in Glycoconjugate journal (2010)“…Using recombinant tetanus toxin HC fragment (rTT-HC) as carrier, we prepared multimeric bivalent immunogens featuring the synthetic hexasaccharide fragment of…”
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Multimeric bivalent immunogens from recombinant tetanus toxin H sub(C) fragment, synthetic hexasaccharides, and a glycopeptide adjuvant
Published in Glycoconjugate journal (01-01-2010)“…Using recombinant tetanus toxin H sub(C) fragment (rTT-H sub(C)) as carrier, we prepared multimeric bivalent immunogens featuring the synthetic hexasaccharide…”
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Chemical synthesis of peptidoglycan fragments for elucidation of the immunostimulating mechanism
Published in Journal of endotoxin research (01-01-2007)“…Partial structures of peptidoglycan were chemically synthesized for elucidation of their precise biological activities. By using an efficient synthetic…”
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