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Makoto Shiozaki

Explore the profile of Makoto Shiozaki including associated specialties, affiliations and a list of published articles. Areas
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Articles 14
Citations 102
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Recent Articles
1.
Kondo K, Otake K, Kaya T, Miwa S, Ueyama Y, Haruta T, et al.
ACS Med Chem Lett . 2025 Jan; 16(1):167-173. PMID: 39811123
Phosphodiesterases (PDEs) have drawn attention due to their critical roles in physiological and pathological conditions. Many research groups have studied these hydrolytic enzymes to develop new drugs, including apremilast as...
2.
Maeba T, Hirata K, Kotoku M, Seki N, Maeda K, Hirashima S, et al.
J Med Chem . 2024 Jan; 67(2):952-970. PMID: 38170624
A number of RORγ inhibitors have been reported over the past decade. There were also several examples advancing to human clinical trials, however, none of them has reached the market...
3.
Miwa S, Yokota M, Ueyama Y, Maeda K, Ogoshi Y, Seki N, et al.
ACS Med Chem Lett . 2021 May; 12(5):745-751. PMID: 34055221
Historically, modulation of transforming growth factor β (TGF-β) signaling has been deemed a rational strategy to treat many disorders, though few successful examples have been reported to date. This difficulty...
4.
Noji S, Hara Y, Miura T, Yamanaka H, Maeda K, Hori A, et al.
J Med Chem . 2020 Jun; 63(13):7163-7185. PMID: 32511913
Dermatologic disorders such as atopic dermatitis arise from genetic and environmental causes and are complex and multifactorial in nature. Among possible risk factors, aberrant immunological reactions are one of the...
5.
Kotoku M, Maeba T, Fujioka S, Yokota M, Seki N, Ito K, et al.
J Med Chem . 2019 Feb; 62(5):2837-2842. PMID: 30776227
Starting from a previously reported RORγ inhibitor (1), successive efforts to improve in vivo potency were continued. Introduction of metabolically beneficial motifs in conjunction with scaffold hopping was examined, resulting...
6.
Noguchi M, Nomura A, Doi S, Yamaguchi K, Hirata K, Shiozaki M, et al.
Sci Rep . 2018 Nov; 8(1):17374. PMID: 30478402
Retinoic acid-related orphan receptor gamma (RORγ) plays pivotal roles in autoimmune diseases by controlling the lineage of interleukin 17 (IL-17)-producing CD4 T cells (Th17 cells). Structure-based drug design has proven...
7.
Noguchi M, Nomura A, Murase K, Doi S, Yamaguchi K, Hirata K, et al.
Genes Cells . 2017 May; 22(6):535-551. PMID: 28493531
Retinoid-related orphan receptor gamma (RORγ) directly controls the differentiation of Th17 cell and the production of interleukin-17, which plays an integral role in autoimmune diseases. To obtain insight into RORγ,...
8.
Noji S, Seki N, Maeba T, Sakai T, Watanabe E, Maeda K, et al.
ACS Med Chem Lett . 2016 Oct; 7(10):919-923. PMID: 27774129
In typical kinase inhibitor programs, a hinge binder showing best potency with preferential specificity is initially selected, followed by fine-tuning of the accompanying substituents on its core module. A shortcoming...
9.
Hirata K, Kotoku M, Seki N, Maeba T, Maeda K, Hirashima S, et al.
ACS Med Chem Lett . 2016 Jan; 7(1):23-7. PMID: 26819660
A novel series of RORγ inhibitors was identified starting with the HTS hit 1. After SAR investigation based on a prospective consideration of two drug-likeness metrics, ligand efficiency (LE) and...
10.
Tanimoto A, Ogawa Y, Oki C, Kimoto Y, Nozawa K, Amano W, et al.
Inflamm Res . 2014 Nov; 64(1):41-51. PMID: 25387665
Objective: To evaluate the pharmacological properties of JTE-052, a novel Janus kinase (JAK) inhibitor. Methods: The JAK inhibitory activity of JTE-052 was evaluated using recombinant human enzymes. The inhibitory effects...