Electronic Resource

FRONTIERS RESEARCH TOPICS : Phenotypic Screening in the 21st Century

---

Since the advent of molecular cloning, target based screening has become the norm in pharmaceutical drug discovery. A large number of potential drug targets have been cloned and functionally expressed, and enormous progress has been made in the development, miniaturization and automation of cell based assays on target molecules recombinantly expressed in mammalian cell lines. This approach has delivered many clinical candidates but relatively few new drugs. Target based screening is likely to provide very good drug candidates for monogenic diseases, and the following collection of manuscripts is not meant to discourage the use of target based approaches. However, most of the more prevalent human diseases are most likely multifactorial and require interaction with multiple targets to produce clinically meaningful efficacy. In addition, high potency, selective interaction with a single target may increases the risk of adverse events or be limited by redundancies and adaptive resistance. Here, target agnostic approaches using phenotypic assays may offer significant benefit. Making such approaches viable requires addressing a number of challenges. This e-book attempts to discuss some of these challenges and illustrate recent advances. Prior to the 1980s, most drugs were discovered using phenotypic assays in live animals or isolated tissues (Swinney, 2013). Most of these drugs interact relatively weakly with a number of targets, and the complete profile of their molecular interactions is not well-known. Examples include most anti-convulsants, diuretics, and vasodilators. Screening in vivo typically returns compounds with acceptable ADME properties and access to the target in vivo; issues that often frustrate the present target based drug discovery programs.

---

Ketersediaan

EBK-00217

615/Bir-f

Perpus Pusat

Tersedia

Informasi Detail

Judul Seri

-

No. Panggil

615/Bir-f

Penerbit

United States of America : Frontiers in Pharmacology., 2007

Deskripsi Fisik

68 hlm

Bahasa

Indonesia

ISBN/ISSN

978-2-88919-469-8

Klasifikasi

615

Tipe Isi

text

Tipe Media

e-book

Tipe Pembawa

-

Edisi

-

Subjek

PHENOTYPIC SCREENING
FRONTIERS RESEARCH

Info Detail Spesifik

Electronic Version

Pernyataan Tanggungjawab

-

Versi lain/terkait

Lampiran Berkas

Komentar

---

Anda harus masuk sebelum memberikan komentar