Search Results - "Yonemori, Kazuko"
-
1
Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging
Published in Bioorganic & medicinal chemistry letters (15-06-2017)“…[Display omitted] •K-Ras(G12D) is selectively inhibited by a cyclic peptide, KRpep-2d.•Alanine scanning was used to determine the amino acids critical to this…”
Get full text
Journal Article -
2
Farnesoid X receptor antagonist exacerbates dyslipidemia in mice
Published in Pharmacological reports (01-02-2018)“…The effects of farnesoid X receptor (FXR) antagonists on plasma lipid profile in mice have not been investigated thus far. The aim of this study was to…”
Get more information
Journal Article -
3
Discovery of Novel and Potent Stearoyl Coenzyme A Desaturase 1 (SCD1) Inhibitors as Anticancer Agents
Published in Bioorganic & medicinal chemistry (15-07-2017)“…[Display omitted] A lead compound A was identified previously as an stearoyl coenzyme A desaturase (SCD) inhibitor during research on potential treatments for…”
Get full text
Journal Article -
4
Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole
Published in Structure (London) (04-03-2021)“…The hERG channel is a voltage-gated potassium channel involved in cardiac repolarization. Off-target hERG inhibition by drugs has become a critical issue in…”
Get full text
Journal Article -
5
Discovery of [cis-3-({(5R)‑5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro‑1H‑inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5H)‑yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist
Published in Journal of medicinal chemistry (12-04-2018)“…A series of tetrahydronaphthyridine derivatives as novel RORγt inverse agonists were designed and synthesized. We reduced the lipophilicity of…”
Get full text
Journal Article -
6
Identification of PARP14 inhibitors using novel methods for detecting auto-ribosylation
Published in Biochemical and biophysical research communications (06-05-2017)“…Poly(ADP-ribose) polymerases (PARPs) use nicotinamide adenine dinucleotide (NAD+) as a co-substrate to transfer ADP-ribose when it releases nicotinamide as the…”
Get full text
Journal Article -
7
Crystal Structure of a Human K‑Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d
Published in ACS medicinal chemistry letters (13-07-2017)“…The Ras proteins play roles in cell differentiation, proliferation, and survival. Aberrant signaling through Ras-mediated pathways in tumor cells occurs as a…”
Get full text
Journal Article -
8
Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2
Published in Journal of medicinal chemistry (13-07-2017)“…Brr2 is an RNA helicase belonging to the Ski2-like subfamily and an essential component of spliceosome. Brr2 catalyzes an ATP-dependent unwinding of the U4/U6…”
Get full text
Journal Article -
9
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Published in Bioorganic & medicinal chemistry (01-02-2018)“…[Display omitted] Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for…”
Get full text
Journal Article -
10
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3′,4′:3,4]benzo[1,2-d]isothiazole derivatives
Published in Bioorganic & medicinal chemistry (15-04-2017)“…[Display omitted] To develop a novel series of CDK8/19 dual inhibitors, we employed structure-based drug design using docking models based on a library…”
Get full text
Journal Article -
11
Studies of CDK 8/19 inhibitors: Discovery of novel and selective CDK8/19 dual inhibitors and elimination of their CYP3A4 time-dependent inhibition potential
Published in Bioorganic & medicinal chemistry (15-06-2017)“…[Display omitted] In this article, synthetic studies around a pyridylacrylamide-based hit compound (1), utilizing structure-based drug design guided by CDK8…”
Get full text
Journal Article -
12
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents
Published in Bioorganic & medicinal chemistry (15-05-2018)“…[Display omitted] We pursued serine palmitoyltransferase (SPT) inhibitors as novel cancer therapeutic agents based on a correlation between SPT inhibition and…”
Get full text
Journal Article -
13
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds
Published in Bioorganic & medicinal chemistry (15-01-2018)“…[Display omitted] A series of novel phenylglycinamides as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists were discovered…”
Get full text
Journal Article