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Teratogenicity01:07

Teratogenicity

The ability of a drug to produce structural deformations and functional abnormalities in the developing embryo or the fetus is called teratogenicity, and the drug producing this effect is known as a teratogen. Teratogenic effects include stillbirth, miscarriage, intrauterine growth restriction, and neurocognitive delay. A teratogen may affect the embryo at different stages of development, which is important in determining the type and extent of the damage. During blastocyst formation, the early...
Chirality in Nature02:30

Chirality in Nature

Chirality is the most intriguing yet essential facet of nature, governing life’s biochemical processes and precision. It can be observed from a snail shell pattern in a macroscopic world to an amino acid, the minutest building block of life. Most of the snails around the world have right-coiled shells because of the intrinsic chirality in their genes. All the amino acids present in the human body exist in an enantiomerically pure state, except for glycine - the sole achiral amino acid. The...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
Drug Biotransformation: Overview01:28

Drug Biotransformation: Overview

Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...

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Related Experiment Video

Updated: Jul 6, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

Thalidomide as a multi-template for development of biologically active compounds.

Yuichi Hashimoto1

  • 1Institute of Molecular & Cellular Biosciences, The University of Tokyo, Bunkyo-ku, Tokyo, Japan. hashimot@iam.u-tokyo.ac.jp

Archiv Der Pharmazie
|April 5, 2008
PubMed
Summary

Thalidomide

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Pharmacology

Background:

  • Thalidomide exhibits diverse biological activities, suggesting its potential as a scaffold for novel drug development.
  • Structural modifications of thalidomide can yield compounds with varied pharmacological effects.

Purpose of the Study:

  • To review structural development strategies for thalidomide-based compounds.
  • To highlight recent advancements in thalidomide derivatives, focusing on specific therapeutic targets.

Main Methods:

  • Two distinct strategies for structural development were employed: target-based and hypothetical target-based approaches.
  • Compounds were designed based on known thalidomide targets and potential pharmacological responses.

Main Results:

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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

Related Experiment Videos

Last Updated: Jul 6, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

  • Target-based development yielded agents regulating tumor necrosis factor-alpha, inhibiting cyclooxygenase, nitric oxide synthase, histone deacetylase, angiogenesis, and tubulin polymerization.
  • Hypothetical target-based development produced androgen/progesterone antagonists, inducers of cell differentiation, and inhibitors of aminopeptidase, thymidine phosphorylase, mu-calpain, and alpha-glucosidase, alongside nuclear liver X receptor antagonists.

Conclusions:

  • Structural diversification of thalidomide is a viable strategy for creating novel therapeutic agents.
  • Recent developments focus on thalidomide derivatives as tubulin polymerization inhibitors, alpha-glucosidase inhibitors, and nuclear liver X receptor antagonists.