Development of orally bioavailable peptides targeting an intracellular protein: from a hit to a clinical KRAS inhibitor
…, H Sase, K Ohara, A Ohta, S Kuramoto… - Journal of the …, 2023 - ACS Publications
Cyclic peptides as a therapeutic modality are attracting a lot of attention due to their potential
for oral absorption and accessibility to intracellular tough targets. Here, starting with a drug-…
for oral absorption and accessibility to intracellular tough targets. Here, starting with a drug-…
The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations
…, Y Tachibana, J Ohwada, H Ebiike, S Kuramoto… - Clinical Cancer …, 2011 - AACR
Purpose: The phosphatidylinositol 3-kinase (PI3K) pathway plays a central role in cell
proliferation and survival in human cancer. PIK3CA mutations, which are found in many cancer …
proliferation and survival in human cancer. PIK3CA mutations, which are found in many cancer …
Stereoselectivity in the oxidation of bufuralol, a chiral substrate, by human cytochrome P450s
S Narimatsu, C Takemi, S Kuramoto… - Chirality: The …, 2003 - Wiley Online Library
Bufuralol (BF), a nonselective β‐adrenoceptor blocking agent, has a chiral center in its
molecule, yielding the enantiomers 1′R‐BF and 1′S‐BF. β‐Adrenoceptor blocking potency is …
molecule, yielding the enantiomers 1′R‐BF and 1′S‐BF. β‐Adrenoceptor blocking potency is …
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799
…, K Yoshinari, M Yoshida, O Kondoh, S Kuramoto… - Bioorganic & medicinal …, 2011 - Elsevier
Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for
cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors …
cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors …
Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets
…, A Chiyoda, S Akai, H Sase, S Kuramoto… - Journal of the …, 2023 - ACS Publications
Establishing a technological platform for creating clinical compounds inhibiting intracellular
protein–protein interactions (PPIs) can open the door to many valuable drugs. Although …
protein–protein interactions (PPIs) can open the door to many valuable drugs. Although …
Discovery of CH7057288 as an orally bioavailable, selective, and potent pan-TRK inhibitor
…, K Hasegawa, H Tanaka, S Kuramoto… - Journal of Medicinal …, 2022 - ACS Publications
Kinase fusions involving tropomyosin receptor kinases (TRKs) have been proven to act as
strong oncogenic drivers and are therefore recognized as attractive therapeutic targets. We …
strong oncogenic drivers and are therefore recognized as attractive therapeutic targets. We …
Angiogenesis inhibitors identified by cell-based high-throughput screening: Synthesis, structure–activity relationships and biological evaluation of 3-[(E)-styryl] …
…, M Hasegawa, Y Sato, K Ogawa, S Kuramoto… - Bioorganic & medicinal …, 2012 - Elsevier
Proliferation of endothelial cells is critical for angiogenesis. We report orally available, in
vivo active antiangiogenic agents which specifically inhibit endothelial cell proliferation. After …
vivo active antiangiogenic agents which specifically inhibit endothelial cell proliferation. After …
Cloning and functional expression of a novel marmoset cytochrome P450 2D enzyme, CYP2D30: comparison with the known marmoset CYP2D19
H Hichiya, S Kuramoto, S Yamamoto, S Shinoda… - Biochemical …, 2004 - Elsevier
Using a primer set designed on the cDNA encoding the known marmoset cytochrome P450
2D19 (CYP2D19), a cDNA encoding a novel CYP2D enzyme (CYP2D30) was cloned from …
2D19 (CYP2D19), a cDNA encoding a novel CYP2D enzyme (CYP2D30) was cloned from …
Simple evaluation method for CYP3A4 induction from human hepatocytes: the relative factor approach with an induction detection limit concentration based on the …
S Kuramoto, M Kato, H Shindoh, A Kaneko… - Drug Metabolism and …, 2017 - ASPET
We investigated the robustness and utility of the relative factor (RF) approach based on the
maximum induction effect (E max ) model, using the mRNA induction data of 10 typical …
maximum induction effect (E max ) model, using the mRNA induction data of 10 typical …
Prediction of drug-induced QT interval prolongation in telemetered common marmosets
…, T Hara, S Sone, N Shishido, S Kuramoto… - The Journal of …, 2008 - jstage.jst.go.jp
Drug-induced QT interval prolongation is a critical issue in development of new chemical
entities, so the pharmaceutical industry needs to evaluate risk as early as possible. Common …
entities, so the pharmaceutical industry needs to evaluate risk as early as possible. Common …