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Characterizing Drug-Target Interactions: Shifting towards the Clinic
1Novartis Institutes for BioMedical Research, Inc., 181 Massachusetts Avenue, Cambridge, MA 02139, USA.
Trends in Pharmacological Sciences
|March 21, 2020
Summary
Thermal proteome profiling (TPP) now analyzes complex tissues and blood for drug discovery. This unbiased proteomics method identifies organ-specific drug targets in late-stage research and clinical settings.
Area of Science:
- Biochemistry
- Proteomics
- Pharmacology
Background:
- Thermal proteome profiling (TPP) is a cellular thermal shift assay.
- TPP offers an unbiased proteomics readout.
- Previous applications were limited, not extending to complex tissues.
Purpose of the Study:
- To demonstrate the application of TPP in complex tissue samples.
- To showcase TPP's utility in organ-specific drug target engagement studies.
- To validate TPP for late-stage drug discovery and clinical settings.
Main Methods:
- Application of TPP to complex tissue samples from model organisms.
- Utilizing TPP with patient-derived whole blood.
- Employing unbiased proteomics for readout.
Main Results:
- Successful application of TPP to complex tissues and whole blood.
- Demonstration of organ-specific drug target engagement studies.
- Identification of drug targets in late-stage drug discovery.
Conclusions:
- TPP is effective for analyzing complex biological samples.
- TPP facilitates organ-specific drug target identification and engagement.
- TPP is a valuable tool for late-stage drug discovery and clinical research.
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