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Review
, 56 (18), 7161-76

Contributions of Academic Laboratories to the Discovery and Development of Chemical Biology Tools

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Review

Contributions of Academic Laboratories to the Discovery and Development of Chemical Biology Tools

Donna M Huryn et al. J Med Chem.

Abstract

The academic setting provides an environment that may foster success in the discovery of certain types of small molecule tools while proving less suitable in others. For example, small molecule probes for poorly understood systems, those that exploit a specific resident expertise, and those whose commercial return is not apparent are ideally suited to be pursued in a university setting. In this review, we highlight five projects that emanated from academic research groups and generated valuable tool compounds that have been used to interrogate biological phenomena: reactive oxygen species (ROS) sensors, GPR30 agonists and antagonists, selective CB2 agonists, Hsp70 modulators, and β-amyloid PET imaging agents. By taking advantage of the unique expertise resident in university settings and the ability to pursue novel projects that may have great scientific value but with limited or no immediate commercial value, probes from academic research groups continue to provide useful tools and generate a long-term resource for biomedical researchers.

Figures

Figure 1
Figure 1
The mitochondrially-targeted fluorescent dyes 1, MitoTracker Red CXMRos, and the ROS detecting MitoSOX and 2.
Figure 2
Figure 2
Structure of 17-β-estradiol and 7.
Figure 3
Figure 3
GPR30 imaging agents.
Figure 4
Figure 4
Structure of GPR30 antagonists 11 and 12.
Figure 5
Figure 5
Structures of inhibitors of Hsp70 and related heat shock pathway modulators.
Figure 6
Figure 6
Structures of CB2 Agonists.
Figure 7
Figure 7
Recent examples of selective CB2 agonists
Figure 8
Figure 8
Non-indole CB2 agonists.
Figure 9
Figure 9
Structure of Pittsburgh Compound B (PiB).
Figure 10
Figure 10
Structures of compound 26, [F-18]Floretapir and [F-18]Florbetaben
Scheme 1
Scheme 1
Categories of reactive species.
Scheme 2
Scheme 2
ROS trigger apoptosis through the release of cytochrome c from mitochondria.
Scheme 3
Scheme 3
Triple sensing fluorescent probe design.
Scheme 4
Scheme 4
Preparation of Hsp70 modulators by consecutive multicomponent reactions: Tandem Biginelli-Ugi process and structure of lead compound 18.
Scheme 5
Scheme 5
Dihydropyrimidinone library synthesis.
Scheme 6
Scheme 6
Structural modifications of the Hsp70 probe molecule 18 lead to changes in the biological profile.
Scheme 7
Scheme 7
Evolution of PiB from Thioflavin T.

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