Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry

Cravatt, Benjamin F.; Wright, Aaron; Kozarich, John W.

doi:10.1146/annurev.biochem.75.101304.124125

Cited by 1,107 publications

(1,081 citation statements)

References 153 publications

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“…In this study, we revealed that vibsanin B preferentially targets HSP90b and has a very weak binding with HSP90a through activity-based protein profiling method (40), indicating that inhibition of HSP90b, but not HSP90a, would be mainly responsible for the inhibitory effect of vibsanin B on leukocyte migration. Because of high conservation in sequence, the function of HSP90a and HSP90b is very similar (41), although previous work reported that HSP90a, but not HSP90b, exerts an essential extracellular role in cancer cell invasiveness (42).…”

Section: Discussionmentioning

confidence: 84%

Vibsanin B Preferentially Targets HSP90β, Inhibits Interstitial Leukocyte Migration, and Ameliorates Experimental Autoimmune Encephalomyelitis

Deng

Shao

et al. 2015

The Journal of Immunology

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Interstitial leukocyte migration plays a critical role in inflammation and offers a therapeutic target for treating inflammation-associated diseases such as multiple sclerosis. Identifying small molecules to inhibit undesired leukocyte migration provides promise for the treatment of these disorders. In this study, we identified vibsanin B, a novel macrocyclic diterpenoid isolated from Viburnum odoratissimum Ker-Gawl, that inhibited zebrafish interstitial leukocyte migration using a transgenic zebrafish line (TG:zlyz–enhanced GFP). We found that vibsanin B preferentially binds to heat shock protein (HSP)90β. At the molecular level, inactivation of HSP90 can mimic vibsanin B’s effect of inhibiting interstitial leukocyte migration. Furthermore, we demonstrated that vibsanin B ameliorates experimental autoimmune encephalomyelitis in mice with pathological manifestation of decreased leukocyte infiltration into their CNS. In summary, vibsanin B is a novel lead compound that preferentially targets HSP90β and inhibits interstitial leukocyte migration, offering a promising drug lead for treating inflammation-associated diseases.

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Section: Discussionmentioning

confidence: 84%

Vibsanin B Preferentially Targets HSP90β, Inhibits Interstitial Leukocyte Migration, and Ameliorates Experimental Autoimmune Encephalomyelitis

Deng

Shao

et al. 2015

The Journal of Immunology

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“…Developing a gel-free sample processing workflow with on-bead enzymatic digestion of proteins would make identification of suicide inhibitor targets tractable (32,33) and would be more amenable to automation. Although analytical throughput was not the primary focus of our studies, our current implementation of SILAC-Target I.D.…”

Section: Discussionmentioning

confidence: 99%

Identifying the proteins to which small-molecule probes and drugs bind in cells

Ong

Schenone

Margolin³

et al. 2009

Proc. Natl. Acad. Sci. U.S.A.

279

265

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Most small-molecule probes and drugs alter cell circuitry by interacting with 1 or more proteins. A complete understanding of the interacting proteins and their associated protein complexes, whether the compounds are discovered by cell-based phenotypic or targetbased screens, is extremely rare. Such a capability is expected to be highly illuminating-providing strong clues to the mechanisms used by small-molecules to achieve their recognized actions and suggesting potential unrecognized actions. We describe a powerful method combining quantitative proteomics (SILAC) with affinity enrichment to provide unbiased, robust and comprehensive identification of the proteins that bind to small-molecule probes and drugs. The method is scalable and general, requiring little optimization across different compound classes, and has already had a transformative effect on our studies of small-molecule probes. Here, we describe in full detail the application of the method to identify targets of kinase inhibitors and immunophilin binders.SILAC ͉ small molecules ͉ target identification

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“…This latter knowledge can be obtained by using activity-based profiling of kinases 68 After labelling, affinity techniques were used to isolate 85 biotin-labelled proteins or peptides for identification and quantification through MS-based techniques. This approach was also used to determine the selectivity of protein kinase inhibitors towards a given protein kinase through competition studies 13 .…”

Section: E Activity-based Profiling Of Active Protein Kinasesmentioning

confidence: 99%

Chemical approaches towards unravelling kinase-mediated signalling pathways

Hodgson

Schröder

2011

Chem. Soc. Rev.

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Citation for published item:rodgsonD hF F F nd hr¤ oderD wF @PHIIA 9ghemi l ppro hes tow rds unr velling kin seEmedi ted sign lling p thw ysF9D ghemi l so iety reviewsFD RH @QAF ppF IPIIEIPPQF Further information on publisher's website:httpXGGdxFdoiForgGIHFIHQWGgHg HHHPHiPublisher's copyright statement:Additional information: Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-pro t purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details.

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Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry

Cited by 1,107 publications

References 153 publications

Vibsanin B Preferentially Targets HSP90β, Inhibits Interstitial Leukocyte Migration, and Ameliorates Experimental Autoimmune Encephalomyelitis

Vibsanin B Preferentially Targets HSP90β, Inhibits Interstitial Leukocyte Migration, and Ameliorates Experimental Autoimmune Encephalomyelitis

Identifying the proteins to which small-molecule probes and drugs bind in cells

Chemical approaches towards unravelling kinase-mediated signalling pathways

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