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Covalent Chemical Cochaperones of the p300/CBP GACKIX Domain

Overview of attention for article published in ChemBioChem, September 2018
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  • Above-average Attention Score compared to outputs of the same age (52nd percentile)
  • Average Attention Score compared to outputs of the same age and source

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Title
Covalent Chemical Cochaperones of the p300/CBP GACKIX Domain
Published in
ChemBioChem, September 2018
DOI 10.1002/cbic.201800173
Pubmed ID
Authors

Jean M. Lodge, Chinmay Y. Majmudar, James Clayton, Anna K. Mapp

Abstract

The GACKIX activator-binding domain has been a compelling target for small molecule probe discovery because of the central role activator-GACKIX complexes play in diseases ranging from leukemia to memory disorders. Additionally, GACKIX is an ideal model to dissect the context-dependent function of activator-coactivator complexes. However, the dynamic and transient PPIs formed by GACKIX are difficult targets for small molecules. An additional complication is that activator-binding motifs such as GACKIX are found in multiple coactivators, making specificity difficult to attain. In this study, we demonstrate that the strategy of Tethering can be used to rapidly discover highly specific covalent modulators of the dynamic PPIs between activators and coactivators. These serve as both orthosteric and allosteric modulators, enabling the tunable assembly or disassembly of the activator-coactivator complexes formed between the KIX domain and its cognate activator binding partners MLL and CREB. The molecules maintain their function and selectivity even in human cell lysates and in bacterial cells and thus will ultimately be useful probes for cellular studies.

X Demographics

X Demographics

The data shown below were collected from the profiles of 7 X users who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 6 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 6 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 2 33%
Professor 1 17%
Researcher 1 17%
Student > Doctoral Student 1 17%
Unknown 1 17%
Readers by discipline Count As %
Chemistry 4 67%
Social Sciences 1 17%
Medicine and Dentistry 1 17%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 06 September 2018.
All research outputs
#8,407,234
of 25,116,143 outputs
Outputs from ChemBioChem
#2,157
of 6,030 outputs
Outputs of similar age
#135,849
of 341,471 outputs
Outputs of similar age from ChemBioChem
#56
of 98 outputs
Altmetric has tracked 25,116,143 research outputs across all sources so far. This one is in the 43rd percentile – i.e., 43% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,030 research outputs from this source. They receive a mean Attention Score of 4.5. This one has gotten more attention than average, scoring higher than 51% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 341,471 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 52% of its contemporaries.
We're also able to compare this research output to 98 others from the same source and published within six weeks on either side of this one. This one is in the 43rd percentile – i.e., 43% of its contemporaries scored the same or lower than it.