A5060650182- Hormonal and reproductive studies
- Computational Drug Discovery Methods
- Sports Performance and Training
- Exercise and Physiological Responses
- Protein Structure and Dynamics
- Estrogen and related hormone effects
- Sports injuries and prevention
- Receptor Mechanisms and Signaling
- Prostate Cancer Treatment and Research
- Phosphodiesterase function and regulation
- Chemical Synthesis and Analysis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Enzyme Structure and Function
- Axial and Atropisomeric Chirality Synthesis
- Liver Disease Diagnosis and Treatment
- Bone and Joint Diseases
- Synthesis and Catalytic Reactions
- Cholinesterase and Neurodegenerative Diseases
- Organic and Inorganic Chemical Reactions
- Liver Diseases and Immunity
- Cardiac, Anesthesia and Surgical Outcomes
- Steroid Chemistry and Biochemistry
- DNA and Nucleic Acid Chemistry
- Bone Metabolism and Diseases
- Thermoregulation and physiological responses
Keio University
2022-2024
Shirasagi Hospital
2024
Kanazawa University
2018
Kyoto University
2006-2015
Kaken Pharmaceutical (Japan)
2011-2014
Hakodate National Hospital
2009
Kyoto Pharmaceutical University
2006
Gifu Pharmaceutical University
1996
Miyazaki Welfare Medical College
1989-1994
This paper describes a similarity-driven simple evolutionary approach to producing candidate molecules of new drugs. The aim the method is explore candidates that are structurally similar reference molecule and yet somewhat different in not only peripheral chains but also their scaffolds. employs known active our interest as which used navigate huge chemical space. obtain seed fragments. An initial set individual structures prepared with fragments additional using several connection rules....
Despite the known beneficial effects of creatine in treating exercise-induced muscle damage (EIMD), its effectiveness remains unclear. This study investigates recovery effect monohydrate (CrM) on EIMD. Twenty healthy men (21-36 years) were subjected to stratified, randomized, double-blind assignments. The (CRE) and placebo (PLA) groups ingested crystalline cellulose, respectively, for 28 days. They subsequently performed dumbbell exercises while emphasizing eccentric contraction elbow...
The objective of the current study was to investigate association between lower body bone fractures occurring during maintenance hemodialysis and prognosis.
The discovery of a new series potent phosphodiesterase 7 (PDE7) inhibitors is described. Novel thieno[3,2-d]pyrimidin-4(3H)-one hit compounds were identified from our chemical library. Preliminary modifications the performed, resulting in fragment-sized compound (10) with highly improved ligand efficiency. Compound design was guided by structure-activity relationships and computational modeling. 6-substituted derivatives thienopyrimidinone showed diminished activity enzyme selectivity....
Selective androgen receptor modulators (SARMs) would provide alternative therapeutic agent for androgen-related diseases. We identified a tetrahydroquinoline (THQ) derivative, 1-(8-nitro-3a, 4, 5, 9b-tetrahydro-3H-cyclopenta[c]quinolin-4-yl) ethane-1, 2-diol (S-40542) as novel SARM antagonist.Affinity nuclear receptors of S-40542 was evaluated in receptor-binding studies. Androgen (AR) transcriptional activity investigated by luciferase reporter assay DU145AR cells. Normal and benign...
Abstract Tetrahydroquinoline (THQ) was deemed to be a suitable scaffold for our nonsteroidal selective androgen receptor modulator (SARM) concept. We adapted the strategy of switching antagonist function cyano‐group‐containing THQ (CN‐THQ) agonist and optimized CN‐THQ as an orally available drug candidate with pharmacological ADME profiles. Based on binding mode analyses synthetic accessibility, we designed synthesized compound that possesses para ‐substituted aromatic ring attached through...
This study aimed to investigate the relationship between muscle shear modulus of biceps brachii, urinary titin N-terminal fragment (UTF), and other damage markers after eccentric exercise. Seventeen healthy males performed five sets ten exercises with dumbbells weighing 50% maximum voluntary contraction (MVC) at elbow joint. Muscle range interest set only brachii measured by ultrasound wave elastography, UTF, MVC, motion (ROM), soreness (SOR) were recorded before, immediately after, 1, 24,...
A pair of optically active triptycene derivatives ((R,R)- and (S,S)-8) with a distorted cyclic structure were synthesized via an intramolecular etherification evaluated as novel chiral selector for high-performance liquid chromatography. The (R,R)- (S,S)-8-based stationary phases (CSPs) found to be particularly effective in the resolution axially biaryl compounds. importance present 8 recognition was demonstrated by comparisons corresponding non-cyclic model compound ((R,R)-9), which did not...
Tetrahydroquinolines (THQs), a new class of nonsteroidal selective androgen receptor (AR) modulators, have two indispensable functional groups, that is, hydroxyl group for AR binding and nitro agonistic activity. Interestingly, switching the to cyano group, compound acts as an antagonist. To understand this phenomenon, molecular dynamics simulations were applied dihydrotestosterone (DHT) representative THQs complexes with AR. Upon ligand binding, formed tight hydrogen-bond (H-bond) Asn705 on...
Adrenomedullin (AM), a potent vasodilator peptide, has been shown to act within the central nervous system modulate fluid and electrolyte balance. AM-immunoreactive cells have found in anterior pituitary gland choroid plexus of humans. In addition, AM activity implicated regulation maternal circulation during pregnancy. To determine relationship between concentration cerebrospinal (CSF) plasma, we measured levels CSF plasma pregnant (group P, n = 12) non-pregnant NP, 10) women scheduled...
[Purpose] The purpose of the present study was to investigate effects transcutaneous xenon light irradiation around stellate ganglion on autonomic functions. [Subjects] Thirty healthy volunteers were subjects. [Methods] subjects underwent two experimental sessions: 1) 10-minute bilateral ganglions in a comfortable supine position (Xe-LISG); and 2) rest same as Xe-LISG (control). low frequency (0.04-0.15 Hz) power (LF) ratio LF high (0.15-0.40 (LF/HF) obtained from spectral analysis R-R...
Enantioselective addition of diethylzinc to benzaldehyde in the presence easily available, β-hydroxysulfides 1 was investigated. The use a catalytic amount gave (S)-1-phenylpropanol excellent yield with high enantioselectivity, ranging from 85 88% ee.
Abstract Solvent dipole ordering (SDO), introduced by Higo et al. (Proteins Struct Funct Genet 2000, 40, 193), is an entity that captures aspect of hydration structure. We have studied SDO in the ligand binding site two proteins (FK506 protein and dihydrofolate reductase) found high regions overlap significantly with 3D structures known inhibitors bound to proteins. Thus, region might be used predict preferred molecular shape ligands bind a protein. Based on this finding, we propose novel...
Abstract We previously reported that solvent dipole ordering (SDO) at the ligand binding site of a protein indicates an outline preferred shape and pose ligands. suggested SDO‐mimetic pseudo‐molecules mimic 3D SDO region could be used as molecular queries with similarity matching method in virtual screening. In this work, screening based on SDO, named SDOVS, was proposed. This applied to ligands for four typical drug target proteins performance compared FRED (well‐known rigid docking...
The study aimed to investigate the relationships between shear modulus of biceps brachii (BB) and brachialis muscle (BA) total two (BB+BA), urinary titin N-terminal fragment (UTF), maximum voluntary isometric contraction (MVC), other indirect markers. Fifteen healthy men performed five sets 10 eccentric contractions using a dumbbell corresponding 50% MVC at 90° measured baseline. elbow joint left arm was extended from 180° (180° = full extension) in 5 s exercise, returned with support...
The study aimed to investigate the relationships between shear modulus of biceps brachii (BB) and brachialis muscle (BA) total two (BB+BA), urinary titin N-terminal fragment (UTF), maximum voluntary isometric contraction (MVC), other indirect markers. Fifteen healthy men performed five sets 10 eccentric contractions using a dumbbell corresponding 50% MVC at 90° measured baseline. elbow joint left arm was extended from 180° (180° = full extension) in 5 s exercise, returned with support...