Discovery of Diverse Natural Products from Undeveloped Fungal Gene Resource by Using Epigenetic Regulation
Yakugaku Zasshi. 2022;142(5):439-446. doi: 10.1248/yakushi.21-00218.ABSTRACTDiscovery of natural products that possess novel chemical structures and pharmaceutical activities increases opportunities of drug development. Filamentous fungi have been recognized as an attractive source for pharmaceutically beneficial natural products. Genome sequencing innovation represented by Next-generation sequencer opened fungal genomes one after another, suggesting that one fungal strain has far more biosynthetic gene clusters than that are estimated from the number of previously isolated natural products. In addition, bioinformatics ana...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Teigo Asai Source Type: research

Recent Advances in the Studies of Metabolic Syndromes and Applications to the Development of New Drugs
Yakugaku Zasshi. 2022;142(5):447-448. doi: 10.1248/yakushi.21-00176-F.NO ABSTRACTPMID:35491147 | DOI:10.1248/yakushi.21-00176-F (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Akifumi Kushiyama Yusuke Nakatsu Source Type: research

Prolyl Isomerase Pin1 Impacts on Metabolism in Muscle and Adipocytes
Yakugaku Zasshi. 2022;142(5):449-456. doi: 10.1248/yakushi.21-00176-1.ABSTRACTProlyl isomerase Pin1 is associated with various substrates and controls their functions through the isomerization of proline. Interestingly, a high fat diet increases Pin1 levels in adipose tissues. Accordingly, we investigated how Pin1 regulates energy metabolism in adipose tissues. Currently, adipocytes are divided into three types with distinct features. White adipocytes (WATs) store energy as triglycerides under fed conditions and release non-esterified fatty acids and glycerol through lipolysis while fasting. Brown and beige adipocytes, whi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Yusuke Nakatsu Tomoichiro Asano Source Type: research

Involvement of Diacylglycerol Kinase on the Regulation of Insulin Secretion in Pancreatic β-Cells during Type 2 Diabetes
Yakugaku Zasshi. 2022;142(5):457-463. doi: 10.1248/yakushi.21-00176-2.ABSTRACTDepression of lipid metabolism in β-cells has been indicated to be one of the causes of impaired insulin secretion in type 2 diabetes. Diacylglycerol (DAG) is an important lipid mediator and is known to regulate insulin secretion in pancreatic β-cells. Intracellular DAG accumulation is involved in β-cell dysfunction in the pathogenesis of type 2 diabetes; thus, the regulation of intracellular DAG levels is likely important for maintaining the β-cell function. We focused on diacylglycerol kinases (DGKs), which strictly regulate intracellular D...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Yukiko K Kaneko Toshiaki Sawatani Tomohisa Ishikawa Source Type: research

Metabolism-dependent Vascular Pathophysiology in Adult Diseases
In conclusion, it was strongly suggested that macrophages regulate inflammation and intracellular lipids depending on metabolism and that they may be involved in angiopathy in adult diseases.PMID:35491150 | DOI:10.1248/yakushi.21-00176-3 (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Akifumi Kushiyama Masahiro Takahashi Sakura Kushiyama Takako Kikuchi Tomoichiro Asano Source Type: research

Role of Fatty Acid Elongase Elovl6 in the Regulation of Fatty Acid Quality and Lifestyle-related Diseases
Yakugaku Zasshi. 2022;142(5):473-476. doi: 10.1248/yakushi.21-00176-4.ABSTRACTThe increasing prevalence of obesity worldwide has become an alarming public health concern because of dramatic increases in the incidence of obesity-associated diseases, including type 2 diabetes mellitus (T2DM). Peripheral insulin resistance and impaired insulin secretion remain the core defects in T2DM. Despite significant advances in unraveling the mechanisms underlying these defects, many of the metabolic pathways and regulators involved in insulin resistance and β-cell dysfunction are not completely understood. This review proposes that ma...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Takashi Matsuzaka Hitoshi Shimano Source Type: research

Frontier of Photopharmacology for High-speed Molecular Movies of Proteins
Yakugaku Zasshi. 2022;142(5):477-478. doi: 10.1248/yakushi.21-00203-F.NO ABSTRACTPMID:35491152 | DOI:10.1248/yakushi.21-00203-F (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Hideko Nagasawa Shigeki Kiyonaka Source Type: research

What Kind of Measurements Can Be Made with an X-ray Free Electron Laser at SACLA?
Yakugaku Zasshi. 2022;142(5):479-485. doi: 10.1248/yakushi.21-00203-1.ABSTRACTThree-dimensional structural information is indispensable to understand the function of proteins in living organisms and X-ray crystallography plays a major role in determining the three-dimensional structure. X-ray free-electron laser (XFEL), which is intense and femtosecond X-ray pulses, enables us to obtain X-ray diffraction intensity data before the destruction of protein molecules, and is expected to be a technology to obtain dynamic structural information. This year marks the 10th anniversary of SPring-8 Angstrom Compact Free Electron Laser...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Toru Nakatsu Source Type: research

Visualization of Enzymatic Reaction by Time-resolved Structural Analysis with Photosensitive Caged Substrate
Yakugaku Zasshi. 2022;142(5):487-494. doi: 10.1248/yakushi.21-00203-2.ABSTRACTElucidation of molecular mechanism for metalloeznyme-catalyzed reactions is longstanding topics in the bio-inorganic chemistry field, since metalloeznymes play pivotal roles in various biological processes and catalyze reactions with high efficiency under mild conditions. Structural determination of reaction intermediates is key to visualizing the reactions catalyzed by metalloenzymes. Although it is not easy to determine the structure of the transient species by conventional crystallography, newly developed time-resolved X-ray crystallography us...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Takehiko Tosha Source Type: research

Design and Synthesis of Gene-directed Caged Compounds toward Photopharmacology
Yakugaku Zasshi. 2022;142(5):495-502. doi: 10.1248/yakushi.21-00203-3.ABSTRACTPhotoresponsive molecules can be used to manipulate the physiological functions of cells with high spatiotemporal resolution. Caged compounds are photoresponsive molecules designed to temporarily mask their original biological activity through covalently bound photoremovable protecting groups. The introduction of additional properties into caged compounds without compromising photosensitivity would help expand the repertoire of caging groups. Therefore, we designed a modular caged compound consisting of three parts: a photoresponsive core, a chem...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Toshiaki Furuta Source Type: research

Development of Photoresponsive Probes to Investigate Cellular Functions
Yakugaku Zasshi. 2022;142(5):503-511. doi: 10.1248/yakushi.21-00203-4.ABSTRACTTechnologies for the optical control of biomolecular functions have recently attracted considerable attention because they can be combined with advanced laser and microscopic techniques for diverse applications at the cellular and intravital levels. In this account, I review the summary of optical control technologies for biomolecular functions based on organic chemistry or protein science, and then introduce our recent studies on the development of small molecule-based photoregulation techniques. The first is the development of a photoactivatabl...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Shin Mizukami Source Type: research

Photopharmacological Tools for Mitotic Cell Division
Yakugaku Zasshi. 2022;142(5):513-519. doi: 10.1248/yakushi.21-00203-5.ABSTRACTGenetic information is replicated and transmitted from a parent cell to two identical daughter cells through mitotic cell division. To accomplish this dynamic process with high accuracy and precision, various motor proteins work in a concerted manner. Especially in the metaphase, mitotic chromosomes are delivered by the motor protein of centromere-associated protein E (CENP-E) to the cell equatorial plane (metaphase plate) along mitotic spindles. However, the critical functional failure of CENP-E can activate the spindle assembly checkpoint throu...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Kazuya Matsuo Source Type: research

Pharmacological Cognitive Enhancement: Current Situation and Perspectives
Yakugaku Zasshi. 2022;142(5):521-526. doi: 10.1248/yakushi.21-00195.ABSTRACTPharmacological cognitive enhancement (PCE) refers to the use of biochemical enhancers for achieving improved mental performance in healthy individuals. One particular use of PCE prevalence is the misuse of these enhancers among university students for academic performance enhancement. The prevalence rates demonstrate the use of a broad spectrum of substances for PCE that can be classified as OTC, prescription, and illegal drugs. Given that certain substances have been widely used for years, their long-term effectiveness and side effects in the hea...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Midori Yamamoto Source Type: research

Impact of the Antimicrobial Stewardship Team Intervention Focusing on Changes in Prescribing Trends and the Rate of Carbapenem-resistant P. aeruginosa
Yakugaku Zasshi. 2022;142(5):527-534. doi: 10.1248/yakushi.21-00202.ABSTRACTAntimicrobial stewardship (AS) intervention strategy is a critical process in promoting appropriate antibiotic use, thus preventing unnecessarily prolonged therapy and reducing antimicrobial resistance (AMR). Although limiting unnecessary carbapenem use by AS intervention is speculated to reduce AMR, there is a lack of specific data on the efficacy of AS team (AST) intervention regarding carbapenem-resistant Pseudomonas aeruginosa (CRPA). Consequently, this study aimed to evaluate the impact of our AS strategy on carbapenem use and CRPA. The AS int...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Yuika Naito Masayuki Maeda Yasuhiro Nagatomo Kazuhisa Ugajin Etsuko Akima Michiko Tanaka Issei Tokimatsu Tadanori Sasaki Source Type: research

Discovery of Diverse Natural Products from Undeveloped Fungal Gene Resource by Using Epigenetic Regulation
Yakugaku Zasshi. 2022;142(5):439-446. doi: 10.1248/yakushi.21-00218.ABSTRACTDiscovery of natural products that possess novel chemical structures and pharmaceutical activities increases opportunities of drug development. Filamentous fungi have been recognized as an attractive source for pharmaceutically beneficial natural products. Genome sequencing innovation represented by Next-generation sequencer opened fungal genomes one after another, suggesting that one fungal strain has far more biosynthetic gene clusters than that are estimated from the number of previously isolated natural products. In addition, bioinformatics ana...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2022 Category: Drugs & Pharmacology Authors: Teigo Asai Source Type: research