Non-Fiction Books:

RNA as a Drug Target

The Next Frontier for Medicinal Chemistry
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Description

Addressing a long-standing challenge for medicinal chemists, this practical reference provides the concepts and tools for developing drug-like small molecules that selectively modulate non-coding RNAs. The introductory parts describes the wide range of druggable RNAs, available techniques for their characterization, binding assay development as well privileged structures in small molecule RNA binders. The main part systematically covers different RNA targets and how to approach them from a drug discovery angle, from splice modulation to riboswitches to targeted degradation, translation blockers and RNA modification. Throughout, the first successful examples of RNA-targeting drug candidates from the development pipeline of small and large pharmaceutical companies are discussed. This seminal reference on a new paradigm in drug discovery is required reading for every medicinal chemists who needs to stay abreast of current developments.

Author Biography:

John Schneekloth received his undergraduate degree from Dartmouth College in 2001 where he worked with Prof. Gordon Gribble. He then moved to Yale University and obtained a Ph.D. from the chemistry department with Prof. Craig Crews in 2006. As a graduate student he studied natural product total synthesis and developed the first cell-permeable PROTAC molecules. He then pursued an NIH postdoctoral fellowship with Prof. Erik Sorensen at Princeton University where he worked on the development of a new multicomponent reaction and the application of this reaction to the synthesis of analgesic natural products. He returned to Yale in 2009 where he worked as a medicinal chemist at the Yale Small Molecule Discovery Center. In 2011, Dr. Schneekloth joined NCI where his research involves using synthetic chemistry and high throughput chemical biology approaches to develop chemical probes of RNA, with a particular emphasis on targeting RNA with druglike small molecules. Martin Pettersson is a medicinal chemistry / drug discovery leader with 18+ years of industrial experience. He received his undergraduate degree from Indiana University in 1998, working with David R. Williams. After four years working for Pfizer, he then joined the University of Texas at Austin for a Ph.D. in Organic Chemistry with Stephen F. Martin. He continued to work for Pfizer, where he delivered multiple compounds into clinical development. He co-led Pfizer's COVID-19 oral protease inhibitor program from project inception until August 2020, during which time the clinical candidate PF-07321332 (Paxlovid) was designed and synthesized. In 2020, he became senior director Neuroscience/Pain at Grünenthal Group, where he is also a member of the Research Board. His publication record includes more than 70 publications, patents/patent applications, and presentations.
Release date NZ
September 11th, 2024
Audience
  • Professional & Vocational
Contributors
  • Edited by John Schneekloth
  • Edited by Martin Pettersson
  • Series edited by Helmut Buschmann
  • Series edited by Jorg Holenz
  • Series edited by Raimund Mannhold
Pages
392
ISBN-13
9783527351008
Product ID
35636667

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