Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands

NMR utilization in fragment-based drug discovery requires techniques to detect weakly binding fragments and to subsequently identify cooperatively binding fragments. Such cooperatively binding fragments can then be optimized or linked in order to develop viable drug candidates. Similarly, ligands or...

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Main Authors: Shiva V. Patnala, Roberto Robles, David A. Snyder
Format: Article
Language:English
Published: MDPI AG 2024-09-01
Series:Biomolecules
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Online Access:https://www.mdpi.com/2218-273X/14/9/1136
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author Shiva V. Patnala
Roberto Robles
David A. Snyder
author_facet Shiva V. Patnala
Roberto Robles
David A. Snyder
author_sort Shiva V. Patnala
collection DOAJ
description NMR utilization in fragment-based drug discovery requires techniques to detect weakly binding fragments and to subsequently identify cooperatively binding fragments. Such cooperatively binding fragments can then be optimized or linked in order to develop viable drug candidates. Similarly, ligands or substrates that bind macromolecules (including enzymes) in competition with the endogenous ligand or substrate are valuable probes of macromolecular chemistry and function. The lengthy and costly process of identifying competitive or cooperative binding can be streamlined by coupling computational biochemistry and spectroscopy tools. The Clustering of Ligand Diffusion Coefficient Pairs (CoLD-CoP) method, previously developed by Snyder and co-workers, detects weakly binding ligands by analyzing pairs of diffusion spectra, obtained in the absence and the presence of a protein. We extended the CoLD-CoP method to analyze spectra pairs (each in the presence of a protein) with or without a critical ligand, to detect both competitive and cooperative binding.
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spelling doaj-art-11f4683ad8694eeeb47c020b4aea6f3f2025-08-20T01:56:10ZengMDPI AGBiomolecules2218-273X2024-09-01149113610.3390/biom14091136Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding LigandsShiva V. Patnala0Roberto Robles1David A. Snyder2Department of Chemistry, College of Science and Health, William Paterson University, 300 Pompton Road, Wayne, NJ 07470, USADepartment of Chemistry, College of Science and Health, William Paterson University, 300 Pompton Road, Wayne, NJ 07470, USADepartment of Chemistry, College of Science and Health, William Paterson University, 300 Pompton Road, Wayne, NJ 07470, USANMR utilization in fragment-based drug discovery requires techniques to detect weakly binding fragments and to subsequently identify cooperatively binding fragments. Such cooperatively binding fragments can then be optimized or linked in order to develop viable drug candidates. Similarly, ligands or substrates that bind macromolecules (including enzymes) in competition with the endogenous ligand or substrate are valuable probes of macromolecular chemistry and function. The lengthy and costly process of identifying competitive or cooperative binding can be streamlined by coupling computational biochemistry and spectroscopy tools. The Clustering of Ligand Diffusion Coefficient Pairs (CoLD-CoP) method, previously developed by Snyder and co-workers, detects weakly binding ligands by analyzing pairs of diffusion spectra, obtained in the absence and the presence of a protein. We extended the CoLD-CoP method to analyze spectra pairs (each in the presence of a protein) with or without a critical ligand, to detect both competitive and cooperative binding.https://www.mdpi.com/2218-273X/14/9/1136nuclear magnetic resonance (NMR)cooperative/competitive ligand bindingdiffusion spectroscopy (DOSY)fragment-based drug discovery (FBDD)
spellingShingle Shiva V. Patnala
Roberto Robles
David A. Snyder
Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
Biomolecules
nuclear magnetic resonance (NMR)
cooperative/competitive ligand binding
diffusion spectroscopy (DOSY)
fragment-based drug discovery (FBDD)
title Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
title_full Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
title_fullStr Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
title_full_unstemmed Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
title_short Application of CoLD-CoP to Detecting Competitively and Cooperatively Binding Ligands
title_sort application of cold cop to detecting competitively and cooperatively binding ligands
topic nuclear magnetic resonance (NMR)
cooperative/competitive ligand binding
diffusion spectroscopy (DOSY)
fragment-based drug discovery (FBDD)
url https://www.mdpi.com/2218-273X/14/9/1136
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