Yasunobu Yamashita (0000-0001-5078-5940)

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Biography

Yasunobu Yamashita graduated from the Faculty of Pharmacy of Keio University in 2012 (Bachelor degree) and obtained his Master degree from the Graduate School of Pharmaceutical Sciences at Keio University in 2014. In 2017 he received his PhD from the Graduate school of Pharmaceutical Sciences, Keio University under the supervision of Prof. Dr. Sugai. From 2017 to 2019 he was a post-doctoral fellow in the research group of Prof. Dr. Gröger at the Bielefeld University. From 2020, he is an assistant professor in the group of Prof. Dr. Takayoshi Suzuki at Osaka University, SANKEN. His research interest includes medicical chemistry and chemical biology.

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Osaka University: Osaka, JP

2020-01-01 to present | Assistant Professor (SANKEN)

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Yasunobu Yamashita

https://orcid.org/0000-0001-5078-5940

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Biography

Activities

Employment (2)

Osaka University: Osaka, JP

Bielefeld University: Bielefeld, DE

Education and qualifications (1)

Keio University: Tokyo, JP

Professional activities (2)

Alexander von Humboldt Foundation: Bonn, DE

Japan Society for the Promotion of Science: Tokyo, JP

Funding (4)

Development of innovative drug candidates by target guided synthesis

深層学習を用いた新規活性予測器の開発とHDAC阻害薬探索への応用

抗炎症作用と気管支拡張作用を併せ持つ既承認薬、メペンゾラートに関する創薬研究

Combinations of chemical oxidations of N-Boc-propargylic and related amines with enzymatic reductions of their corresponding imines in one-pot process

Works (33)

創薬モダリティの高度化と次世代動物評価モデル 4.タンパク質間相互作用阻害を標的とした創薬モダリティ

Epigenetic Inhibitors as Alzheimer’s Disease Therapeutic Agents

Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule

Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells

A Structure–Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1

Identification of a Histone Deacetylase 8 Inhibitor through Drug Screenings Based on Machine Learning

Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity

Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation

HDAC8選択的阻害薬の創製とPROTACへの応用

Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC)

Cancer-Cell-Selective Targeting by Arylcyclopropylamine–Vorinostat Conjugates

Medicinal Chemistry Research on Targeting Epigenetic Complexes

Recent progress on small molecules targeting epigenetic complexes

Identification of Novel Histone Deacetylase 6‐Selective Inhibitors Bearing 3,3,3‐Trifluorolactic Amide (TFLAM) Motif as a Zinc Binding Group

Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach

Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders

Learning about Enzyme Stability against Organic Cosolvents from Structural Insights by Ion Mobility Mass Spectrometry

Metalloprotein-Catalyzed Click Reaction for In Situ Generation of a Potent Inhibitor

Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity

An Asymmetric Organocatalytic Aldol Reaction of a Hydrophobic Aldehyde in Aqueous Medium Running in Flow Mode

Prediction of Protein−compound Binding Energies from Known Activity Data: Docking‐score‐based Method and its Applications

Identification of Mepenzolate Derivatives With Long-Acting Bronchodilatory Activity

Preparation of (R)-3-Hydroxy-N-methylpiperidine, a Synthetic Key Intermediate of (R)-Mepenzolate, Based on the Lipase-Catalyzed Resolution of the Racemic Form

Short-step syntheses of naturally occurring polyoxygenated aromatics based on site-selective transformation

Recent Advances for Synthesis of Scyphostatin and Utilization of Oxabicyclo[2.2.1]Heptene Toward Ethyl Shikimate

Simple Synthesis of Sakuranetin and Selinone &lt;i&gt;via&lt;/i&gt; a Common Intermediate, Utilizing Complementary Regioselectivity in the Deacetylation of Naringenin Triacetate

Ex Situ Enantioconvergent Approaches for the Effective Use of Undesired­ Isomers: Stereochemical Convergence of a Substrate with Multiple Chiral Centers and Recycling of a Decarboxylated Byproduct

Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities

Structure–activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity

Superiority of pulmonary administration of mepenzolate bromide over other routes as treatment for chronic obstructive pulmonary disease

Mepenzolate bromide displays beneficial effects in a mouse model of chronic obstructive pulmonary disease

Chemo-enzymatic enantioconvergent approach toward ethyl shikimate from ethyl 5-hydroxy-3,4-isopropylidenedioxycyclohex-1-enecarboxylate

Prostaglandin E1-containing nanoparticles improve walking activity in an experimental rat model of intermittent claudication

Peer review (5 reviews for 3 publications/grants)

Simple Synthesis of Sakuranetin and Selinone <i>via</i> a Common Intermediate, Utilizing Complementary Regioselectivity in the Deacetylation of Naringenin Triacetate

Ex Situ Enantioconvergent Approaches for the Effective Use of Undesired Isomers: Stereochemical Convergence of a Substrate with Multiple Chiral Centers and Recycling of a Decarboxylated Byproduct