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Related Concept Videos

Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Complexometric Titration: Ligands00:43

Complexometric Titration: Ligands

Different monodentate and polydentate ligands are used as complexing agents in complexometric titration reactions. The formation of complexes by mono- and bidentate ligands involves two or more intermediate steps, limiting their use as complexing agents. In comparison, polydentate ligands can form complexes with metal ions in a single-step process, facilitating sharper end points. This means polydentate ligands, such as amino carboxylic acid derivatives, are most commonly employed in...
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...
EDTA: Chemistry and Properties01:22

EDTA: Chemistry and Properties

Polydentate ligands are most widely used in complexometric titrations because they form more stable complexes with the metal ions than mono- or bidentate ligands due to the chelate effect. Examples of polydentate ligands are ethylenediaminetetraacetic acid (EDTA), crown ethers, and cryptands. The most important feature of optimal polydentate ligands is the ability to form 1:1 complexes in a single-step process. Amino carboxylic acid derivatives are frequently used as complexing agents. EDTA is...

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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Designed multiple ligands: basic research vs clinical outcomes.

L Costantino1, D Barlocco

  • 1University of Modena e Reggio Emilia, Dipartimento di Scienze Farmaceutiche, Via Campi 183, 41100 Modena, Italy. luca.costantino@unimore.it

Current Medicinal Chemistry
|June 12, 2012
PubMed
Summary
This summary is machine-generated.

Designing multitarget drugs for complex diseases like cancer remains challenging. While various strategies exist, current clinical options often favor drug combinations over designed multiple ligands, awaiting systems biology advancements.

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Systems Biology

Background:

  • Multifactorial pathologies (e.g., cancer, Alzheimer's disease) present significant clinical treatment challenges.
  • Developing single compounds that target multiple disease-relevant molecules is an active research area.

Purpose of the Study:

  • To review clinical outcomes of multitarget compounds.
  • To critically evaluate design strategies and their effectiveness.
  • To assess the current therapeutic utility of designed multitarget ligands versus alternatives.

Main Methods:

  • Literature review of published research on multitarget compound design and clinical results.
  • Analysis of various design strategies employed for multitarget ligands.
  • Comparison of designed multitarget ligands with drug co-administration and fixed-dose formulations.

Main Results:

  • Several effective design strategies for multitarget compounds are available.
  • The optimal strategy often depends on the specific therapeutic area.
  • Currently, drug co-administration or fixed-dose formulations are often more clinically useful than designed multitarget ligands.

Conclusions:

  • The design of multitarget ligands faces challenges, with current clinical practice favoring simpler approaches.
  • Advancements in systems biology, enabling identification of critical nodal targets, are expected to drive future success in multitarget drug design.
  • A systems biology-driven approach promises a renaissance in medicinal chemistry for complex diseases.