Mid-size Drugs Based on Peptides and Peptidomimetics: A New Drug Category

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This brief describes studies conducted by the authors on mid-size drugs utilizing peptides and peptidomimetics, and on the development of anti-HIV agents. Peptides are important biological molecules and have various physiological actions. Peptide-based drug discovery may help bring about the development of useful medicines that are highly safe and show potent pharmacological effects in small doses. Recently, it has been shown that there is an important drug-like space in the mid-sized region between low- and high-molecular-weight compounds. Thus, mid-size drugs such as peptide compounds are being focused on. To date, several peptidomimetics that mimic primary, secondary, and tertiary structures of peptides have been developed to maintain and improve biological activities and actions of peptides. In this book, the features and advantages of mid-size drugs are described in detail. In addition, the merits of utilizing peptidomimetics in the development of mid-size drugs are referred to. Understanding such peptide-derived mid-size drugs will lead to a comprehensive expansion of medicinal chemistry.
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About the author

Hirokazu Tamamura received his Ph.D. in Pharmacy from Kyoto University in 1995. His research interests include chemical biology, medicinal chemistry, peptide–protein chemistry, and organic chemistry. Currently, he is a professor at Tokyo Medical and Dental University, with a total of 27 years of teaching experience at Kyoto University and Tokyo Medical and Dental University.Dr. Tamamura won the Award for Distinguished Young Scientists from the Japanese Peptide Society in 1998 and the Award for Young Scientists from the Pharmaceutical Society of Japan in 2001.He has published 230 articles and contributed to 107 books, with his work appearing in internationally renowned journals including Angew. Chem., Int. Ed., J. Am. Chem. Soc., ACS Chem. Biol., Org. Lett., J. Med. Chem., Bioconjugate Chem., ChemBioChem, ChemMedChem, Bioorg. Med. Chem., Bioorg. Med. Chem. Lett., and Biopolymers: Peptide Science.

Takuya Kobayakawa received his Ph.D. from Tokyo Medical and Dental University in 2017. From 2016 to 2017, he worked as a Research Fellow of the Japan Society for the Promotion of Science under Prof. Hirokazu Tamamura. He is currently (since October 2017) an assistant professor in Prof. Tamamura’s research group at Tokyo Medical and Dental University.His research interests include synthetic organic chemistry, chemical biology, medicinal chemistry, and peptide and peptidomimetic chemistry.
He has published more than 10 articles in internationally renowned journals such as Org. Lett., Bioconjugate Chem., ChemMedChem, and Tetrahedron.He has won a number of awards, including the best presentation award at the 136th Annual Meeting of the Pharmaceutical Society of Japan, the best poster award at the 52nd Japanese Peptide Symposium, etc.

Nami Ohashi received her Ph.D. in Medicine from Tokyo Medical and Dental University in 2011.Her research interests include chemical biology, medicinal chemistry, and peptide–protein chemistry. Dr. Ohashi is currently an assistant professor at Tokyo Medical and Dental University, where she has 4 years of teaching experience. She won the Travel Award for Students and Young Scientists from the Japanese Peptide Society in 2007 and the Presidential Grant-in-Aid for Young Scientists from Tokyo Medical and Dental University in 2014.
She has published 29 articles and contributed to 22 books. Her published articles have appeared in internationally recognized journals including Nat. Commun., Angew. Chem., Int. Ed., ACS Chem. Biol., Org. Lett., Bioconjugate Chem., ChemBioChem, ChemMedChem, Bioorg. Med. Chem., Bioorg. Med. Chem. Lett., and Biopolymers: Peptide Science.
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Additional Information

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Published on
Jan 16, 2018
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Medical / General
Medical / Pharmacy
Science / Chemistry / Clinical
Science / Chemistry / Organic
Science / Life Sciences / Biochemistry
Technology & Engineering / Chemical & Biochemical
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This thesis mainly describes the development of a screening process for a mirror-image library of chiral natural products. It demonstrates how, by using mirror-image proteins for the screening of available natural products, unavailable mirror-image isomers of natural products can be screened in a mirror process. Moreover, as mirror-image isomers including target proteins and natural products are mainly prepared by means of chemical synthesis, the screening strategy presented here suggests the importance of organic chemistry.

Natural products are commonly used as valuable resources for drug discovery. However, as they are mostly produced as single enantiomeric forms, researchers have tested o

nly natural products bearing one stereochemistry available in nature. As natural products and their enantiomers have identical physicochemical properties and different biological activities, mirror-image isomers of natural products are promising candidates for novel medicinal resources.

In an effort to identify anticancer agents from the mirror-image library, chemical protein syntheses of some target oncoproteins, MDM2, MDMX and Grb2, and their applications to the chemical array screening process were achieved. In the course of this process the NP843 enantiomer, which is the enantiomer of an α-tocopherol derivative, was successfully identified as a novel MDM2-p53 interaction inhibitor. These results clearly show that a mirror-image library of chiral natural products represents an invaluable medicinal resource. Accordingly, the chemistry-based screening strategy described in this thesis will be of great interest to a broad range of chemists involved in natural product, medicinal, and synthetic chemistry.

Covering everything you need to study for and pass the Pharmacy Technician Certification Board (PTCB) and ExCPT exams, Mosby's Review for the Pharmacy Technician Certification Examination, 3rd Edition makes exam preparation easy. Review the content you'll see on the exam with handy outlines, test-taking tips and strategies, and electronic flash cards. Written by noted pharmacy technician educator James J. Mizner, this complete review tests your knowledge and simulates the actual PTCB exam with 17 different, 100-question practice exams in the book and online. This edition is modeled after the updated Pharmacy Technician Certification Exam Blueprint.A total of 1,700 review questions are included in 17 practice exams in the book and online.100-question format of each practice exam simulates the PTCB and ExCPT exams, with multiple-choice questions and the same balance of content, for a realistic test taking experience.700 electronic flash cards help you learn and remember facts by covering the top 200 most prescribed pharmaceuticals, top 50 herbals, abbreviations, and sound-alike drugs.Review content reflects the new percentages covered on the PTCB exam.A convenient outline format helps you to quickly review important information you'll see on the exam.Tips and suggestions prepare you for test-taking success by providing an insider’s perspective on what to expect and how to prepare for your exam when you have limited time. Seven practice exams in the book feature the same format and content emphasis as the national exam. Ten practice exams on the Evolve companion website in both timed and untimed modes help you identify any areas of weakness, and include instant feedback and remediation. UPDATED content includes current drug information and pharmacy practice procedures based on the new Pharmacy Technician Certification Exam Blueprint.NEW! Chapter objectives provide a clear breakdown of content and goals for review.
Medicinal chemistry is a complex topic. Written in an easy to follow and conversational style, Basic Concepts in Medicinal Chemistry focuses on the fundamental concepts that govern the discipline of medicinal chemistry as well as how and why these concepts are essential to therapeutic decisions. The book emphasizes functional group analysis and the basics of drug structure evaluation.

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About the Authors

Marc W. Harrold, BS, Pharm, PhD, is Professor of Medicinal Chemistry at the Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA. Professor Harrold is the 2011 winner of the Omicron Delta Kappa "Teacher of the Year" award at Duquesne University. He is also the two-time winner of the "TOPS"  (Teacher of the Pharmacy School) award at the Mylan School of Pharmacy.

Robin M. Zavod, PhD, is Associate Professor for Pharmaceutical Sciences at the Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, where she was awarded the 2012 Outstanding Faculty of the Year award. Professor Zavod also serves on the adjunct faculty for Elmhurst College and the Illinois Institute of Technology. She currently serves as Editor-in-Chief of the journal Currents in Pharmacy Teaching and Learning.

Concise Review for the PTCB Exam is a comprehensive approach to preparing for the pharmacy technician certification exam. It does not try to cover every aspect about the field of pharmacy. Rather, it targets the information that is relevant to the certification exam. The text includes drug information, test-taking strategies, examples and practice questions that will prepare a student to pass the test the first time. . Instruction in all test areas: math, law, hospital, drug information. . Contains strategies you MUST know to ace the exam. . Over 750 practice questions that will familiarize you with the PTCB format and help you master the techniques taught. . Detailed answer explanations that will help you avoid making the same mistake twice. . Pharmacy calculations are completely worked out so that all math problems on the exam can be easily understood and solved. . Gives unique ways to learn many of the drugs that will be on the exam. . Includes three practice PTCB tests. All of these questions are similar to those that you will see on the actual PTCB exam. . Covers pharmacy law and hospital information in a way that will make it easy to recall the information. .Contains a list of the top 200 drugs with brand, generic, indication and class. About the Authors Brian Tuschl, Pharm. D., is the president of Tech Prep Solutions. He is an Adjunct Clinical Assistant Professor in the Department of Clinical Sciences and Administration in the College of Pharmacy at the University of Houston and was presented with the Roche Preceptor of the Year Award in 2006. Dr. Tuschl currently serves as a member of the advisory boards of two local technical schools with pharmacy technician programs and also practices retail pharmacy in Houston, Texas. Christopher Ardoin, BSPharm, is the co-founder of Tech Prep Solutions. He is a preceptor with the University of Houston College of Pharmacy. He is a licensed pharmacist in both Texas and Louisiana. Mr. Ardoin has over ten years of pharmacy experience in areas including hospital, compounding, and retail pharmacy.
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