[HTML][HTML] In vivo knockdown of pathogenic proteins via specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs)
…, O Ujikawa, K Shimokawa, O Sano, R Koyama… - Journal of Biological …, 2017 - ASBMB
Many diseases, especially cancers, result from aberrant or overexpression of pathogenic
proteins. Specific inhibitors against these proteins have shown remarkable therapeutic effects, …
proteins. Specific inhibitors against these proteins have shown remarkable therapeutic effects, …
Development of protein degradation inducers of androgen receptor by conjugation of androgen receptor ligands and inhibitor of apoptosis protein ligands
…, O Ujikawa, N Ohoka, T Hattori, R Koyama… - Journal of medicinal …, 2018 - ACS Publications
Targeted protein degradation using small molecules is a novel strategy for drug development.
We have developed hybrid molecules named specific and nongenetic inhibitor of …
We have developed hybrid molecules named specific and nongenetic inhibitor of …
[HTML][HTML] The enzymatic activity of inositol hexakisphosphate kinase controls circulating phosphate in mammals
…, S Abe, H Akiyama, A Kobayashi, R Koyama… - Nature …, 2021 - nature.com
Circulating phosphate levels are tightly controlled within a narrow range in mammals. By
using a novel small-molecule inhibitor, we show that the enzymatic activity of inositol …
using a novel small-molecule inhibitor, we show that the enzymatic activity of inositol …
[HTML][HTML] Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation
…, T Hattori, T Sameshima, O Sano, R Koyama… - Journal of Biological …, 2018 - ASBMB
Aberrant expression of proteins often underlies many diseases, including cancer. A recently
developed approach in drug development is small molecule-mediated, selective …
developed approach in drug development is small molecule-mediated, selective …
A novel L-isoleucine hydroxylating enzyme, L-isoleucine dioxygenase from Bacillus thuringiensis, produces (2S, 3R, 4S)-4-hydroxyisoleucine
…, NN Samsonova, YI Kozlov, R Koyama… - Biochemical and …, 2009 - Elsevier
The unique function of 4-hydroxyisoleucine (4-HIL) is to stimulate glucose-induced insulin
secretion in a glucose-dependent manner. 4-HIL is distributed only in certain kinds of plants …
secretion in a glucose-dependent manner. 4-HIL is distributed only in certain kinds of plants …
Design, synthesis, and biological evaluation of retinoic acid-related orphan receptor γt (RORγt) agonist structure-based functionality switching approach from in house …
…, N Negoro, T Kawamoto, R Koyama… - Journal of Medicinal …, 2019 - ACS Publications
Retinoic acid receptor-related orphan receptor γt (RORγt) agonists are expected to provide
a novel class of immune-activating anticancer drugs via activation of Th17 cells and Tc17 …
a novel class of immune-activating anticancer drugs via activation of Th17 cells and Tc17 …
Novel DOCK2-selective inhibitory peptide that suppresses B-cell line migration
…, Y Adachi, Y Komoike, Y Kamada, R Koyama… - Biochemical and …, 2017 - Elsevier
Dedicator of cytokinesis 2 (DOCK2) is a key molecule for lymphocyte activation and migration.
DOCK2 interacts with Ras-related C3 botulinus toxin substrate 1 (Rac1, GTPase) and …
DOCK2 interacts with Ras-related C3 botulinus toxin substrate 1 (Rac1, GTPase) and …
Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation
Y Shimizu, R Koyama, T Kawamoto - Biochemical pharmacology, 2017 - Elsevier
GPR39, a G-protein-coupled receptor activated by zinc, reportedly activates multiple
intracellular signaling pathways via Gs, Gq, G12/13, and β-arrestin, but little is known about …
intracellular signaling pathways via Gs, Gq, G12/13, and β-arrestin, but little is known about …
Discovery of artificial VIPR2-antagonist peptides possessing receptor-and ligand-selectivity
K Sakamoto, R Koyama, Y Kamada, M Miwa… - … and biophysical research …, 2018 - Elsevier
Vasoactive intestinal peptide receptor 2 (VIPR2, also known as VPAC2) is a class B G-protein
coupled receptor (GPCR) and plays important roles in the physiology of central nervous …
coupled receptor (GPCR) and plays important roles in the physiology of central nervous …
Chronic exposure to SCO-267, an allosteric GPR40 full agonist, is effective in improving glycemic control in rats
R Koyama, M Ookawara, M Watanabe, Y Moritoh - Molecular Pharmacology, 2021 - ASPET
Full agonist-mediated activation of free fatty acid receptor 1 (FFAR1/GPR40) alleviates
diabetes in rodents. Considering that diabetes is a chronic disease, assessment of treatment …
diabetes in rodents. Considering that diabetes is a chronic disease, assessment of treatment …