Purinergic Receptors and Their Modulators

Colotta, Vittoria, Supuran, Claudiu T.

Purinergic Receptors and Their Modulators
  • 出版商: Springer
  • 出版日期: 2024-09-30
  • 售價: $10,380
  • 貴賓價: 9.5 折 $9,861
  • 語言: 英文
  • 頁數: 354
  • 裝訂: Quality Paper - also called trade paper
  • ISBN: 3031397274
  • ISBN-13: 9783031397271

    • 海外代購書籍(需單獨結帳)

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商品描述

This book overviews purinergic receptors that are playing key roles in human and pathophysiological processes. The book elaborates on how selective P1 and P2 modulators have been developed as therapeutics for a variety of diseases. It also provides an overview of current perspectives in the design of purinergic receptor modulators and future challenges such as the availability of selective ligands for all receptor subtypes.

Divided into 12 chapters, this comprehensive volume also offers a multidisciplinary perspective on the historical evolution, starting with a chapter devoted to the roots and early discoveries of adenosine and its receptors, followed by a twenty-year retrospective on the synthesis, properties, and functional potential of adenosine receptor ligands, probes, and functional conjugates. In the next chapters, experts in the field delve into topics such as the therapeutic potential of adenosine receptor ligands in wound healing and fibrosis, the therapeutic benefits of A2A receptor antagonists, the A2B adenosine receptor as a target for brain ischemia or demyelination, the development and latest advancements in clinical trials of A3 adenosine receptor ligands. Other chapters describe bifunctional tools to study adenosine receptors, allosteric modulators of adenosine receptors, and new computational approaches to inspect adenosine receptor-ligand recognition processes. Furthermore, the book discusses the role of P2X4 receptors in immunity and inflammation. The final chapters illustrate CD73 inhibitors as antitumor agents, and bacterial ectonucleotidases as underexplored antibacterial drug targets.

This book is a valuable resource for scholars working in the field of medicinal chemistry, as well as researchers in the industry, providing readers with a comprehensive understanding of adenosine receptor biology and its therapeutic potential.

商品描述(中文翻譯)

本書概述了在人體及病理生理過程中扮演關鍵角色的嘌呤能受體。書中詳細說明了如何開發選擇性 P1 和 P2 調節劑作為各種疾病的治療藥物。它還提供了目前在嘌呤能受體調節劑設計方面的觀點，以及未來挑戰，例如所有受體亞型的選擇性配體的可用性。

本書分為12章，這本綜合性著作還提供了多學科的視角，從一章專門介紹腺苷及其受體的根源和早期發現開始，接著是對腺苷受體配體、探針和功能性共軛物的合成、特性和功能潛力的二十年回顧。在接下來的章節中，該領域的專家深入探討了腺苷受體配體在傷口癒合和纖維化中的治療潛力、A2A 受體拮抗劑的治療益處、A2B 腺苷受體作為腦缺血或脫髓鞘的靶點、以及 A3 腺苷受體配體的臨床試驗的發展和最新進展。其他章節描述了研究腺苷受體的雙功能工具、腺苷受體的變構調節劑，以及檢查腺苷受體-配體識別過程的新計算方法。此外，本書還討論了 P2X4 受體在免疫和炎症中的作用。最後幾章介紹了 CD73 抑制劑作為抗腫瘤劑，以及細菌外核苷酸酶作為尚未充分探索的抗菌藥物靶點。

本書是從事藥物化學領域的學者以及業界研究人員的重要資源，為讀者提供了對腺苷受體生物學及其治療潛力的全面理解。

作者簡介

Vittoria Colotta is an Associate Professor of Medicinal Chemistry at Dipartimento Neurofarba, Universita` degli Studi di Firenze, Sezione di Scienze Farmaceutiche e Nutraceutiche, Italy. She completed her degree in Pharmaceutical Chemistry and Technology in 1985 and her PhD in Medicinal Chemistry in 1988, both at University of Florence. Her past research interest was the synthesis of new biologically active compounds designed as ligands of benzodiazepine and glutamate receptors. Current research is mainly focused on the development of adenosine receptors' ligands and inhibitors of the enzymes 5'-ectonucleotidase (CD73), carbonic anhydrases and casein kinases 1 and 2. The aim of the work is the identification of selective or multitarget-directed ligands as potential therapeutic agents for cancer and neurodegenerative diseases. She is co-author of more than 110 peer-reviewed articles and co-inventor of 2 Patents. She is an Editor of the journal Pharmaceuticals and a Review Editorof Frontiers in Pharmacology (Experimental Pharmacology and Drug Discovery section). She is an active reviewer for high-impact medicinal chemistry journals.

Claudiu T. Supuran is a Full Professor of Medicinal Chemistry at Dipartimento Neurofarba, Universita` degli Studi di Firenze, Sezione di Scienze Farmaceutiche e Nutraceutiche, Florence, Italy. He received his BSc in Chemistry from the Polytechnic University of Bucharest, Romania (1987), and Ph. D. in Chemistry at the same university in 1991. His research interests focus on drug development against Carbonic anhydrases and other enzymes. He has published 2000+ research articles on enzyme inhibitors/activators, being one of the most cited medicinal chemists worldwide. His research is also focused on metalloenzymes cloning, characterization and inhiibtion studies, carbonic anhydrases, proteases, heterocyclic chemistry, chemistry of sulfonamides, sulfamates and sulfamides, X-ray crystallography ofmetallo-enzymes, biologically active organo-element derivatives, quantitative structure-activity relationship (QSAR) studies, metal-based drugs, cyclooxygenases inhibitors, serine proteases, matrix metalloproteinases, bacterial proteases, antivirals, antitumor drugs, ophthalmologic drugs and amino acid derivatives. One sulfonamide carbonic anhydrase inhibitor discovered in his laboratory, SLC-0111, completed Phase I clinical trials as antitumor/antimetastatic agent in 2014 and is presently in Phase Ib/II clinical trials in North America, being developed for the treatment of advanced, metastatic solid tumors.


作者簡介(中文翻譯)

Vittoria Colotta 是義大利佛羅倫斯大學（Università degli Studi di Firenze）神經藥物部（Dipartimento Neurofarba）藥物化學的副教授。她於1985年完成藥物化學與技術學位，並於1988年在佛羅倫斯大學獲得藥物化學博士學位。她過去的研究興趣是合成新型生物活性化合物，這些化合物被設計為苯二氮平和谷氨酸受體的配體。目前的研究主要集中在腺苷受體的配體和5'-外核苷酸酶（CD73）、碳酸酐酶以及酪蛋白激酶1和2的抑制劑的開發。這項工作的目標是識別選擇性或多靶向的配體，作為癌症和神經退行性疾病的潛在治療劑。她是110多篇同行評審文章的共同作者，並擁有2項專利的共同發明人。她是期刊《Pharmaceuticals》的編輯，以及《Frontiers in Pharmacology》（實驗藥理學和藥物發現部分）的審稿編輯。她也是多本高影響力藥物化學期刊的活躍審稿人。

Claudiu T. Supuran 是義大利佛羅倫斯大學（Università degli Studi di Firenze）神經藥物部（Dipartimento Neurofarba）藥物化學的正教授。他於1987年在羅馬尼亞布加勒斯特理工大學獲得化學學士學位，並於1991年在同一所大學獲得化學博士學位。他的研究興趣集中在針對碳酸酐酶和其他酶的藥物開發上。他已發表超過2000篇有關酶抑制劑/激活劑的研究文章，是全球被引用最多的藥物化學家之一。他的研究還集中在金屬酶的克隆、特徵化和抑制研究、碳酸酐酶、蛋白酶、雜環化學、磺胺類化合物、硫酸酯和硫胺類化合物的化學、金屬酶的X射線晶體學、生物活性有機元素衍生物、定量結構-活性關係（QSAR）研究、金屬基藥物、環氧合酶抑制劑、絲氨酸蛋白酶、基質金屬蛋白酶、細菌蛋白酶、抗病毒藥物、抗腫瘤藥物、眼科藥物和氨基酸衍生物。他的實驗室發現的一種磺胺類碳酸酐酶抑制劑 SLC-0111，於2014年完成了作為抗腫瘤/抗轉移劑的第一期臨床試驗，目前在北美進行第一/第二期臨床試驗，正在開發用於治療晚期轉移性實體腫瘤。

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