Abstract
The completion of the human genome has resulted in the identification of large numbers of novel targets for drug development. Many of these targets belong to protein families with homologous structures and similar active sites. Against these targets, successful drugs must display high affinity and high selectivity, goals that have been difficult to accomplish and that emphasize the need for better optimization strategies. Those strategies require control over the forces that maximize affinity towards the intended target and minimize affinity towards other proteins. Because isothermal titration calorimetry (ITC) is the only experimental technique that provides a partition of the binding energy into its enthalpic and entropic components, it is rapidly becoming a key technology in lead optimization.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 295-299 |
| Number of pages | 5 |
| Journal | Drug Discovery Today: Technologies |
| Volume | 1 |
| Issue number | 3 |
| DOIs | |
| State | Published - Dec 2004 |
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ASJC Scopus subject areas
- Drug Discovery
- Molecular Medicine
Cite this
Isothermal titration calorimetry : Controlling binding forces in lead optimization. / Freire, Ernesto I.
In: Drug Discovery Today: Technologies, Vol. 1, No. 3, 12.2004, p. 295-299.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Isothermal titration calorimetry
T2 - Controlling binding forces in lead optimization
AU - Freire, Ernesto I
PY - 2004/12
Y1 - 2004/12
N2 - The completion of the human genome has resulted in the identification of large numbers of novel targets for drug development. Many of these targets belong to protein families with homologous structures and similar active sites. Against these targets, successful drugs must display high affinity and high selectivity, goals that have been difficult to accomplish and that emphasize the need for better optimization strategies. Those strategies require control over the forces that maximize affinity towards the intended target and minimize affinity towards other proteins. Because isothermal titration calorimetry (ITC) is the only experimental technique that provides a partition of the binding energy into its enthalpic and entropic components, it is rapidly becoming a key technology in lead optimization.
AB - The completion of the human genome has resulted in the identification of large numbers of novel targets for drug development. Many of these targets belong to protein families with homologous structures and similar active sites. Against these targets, successful drugs must display high affinity and high selectivity, goals that have been difficult to accomplish and that emphasize the need for better optimization strategies. Those strategies require control over the forces that maximize affinity towards the intended target and minimize affinity towards other proteins. Because isothermal titration calorimetry (ITC) is the only experimental technique that provides a partition of the binding energy into its enthalpic and entropic components, it is rapidly becoming a key technology in lead optimization.
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UR - http://www.scopus.com/inward/citedby.url?scp=13344284025&partnerID=8YFLogxK
U2 - 10.1016/j.ddtec.2004.11.016
DO - 10.1016/j.ddtec.2004.11.016
M3 - Article
C2 - 24981498
AN - SCOPUS:13344284025
VL - 1
SP - 295
EP - 299
JO - Drug Discovery Today: Technologies
JF - Drug Discovery Today: Technologies
SN - 1740-6749
IS - 3
ER -