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Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein

Overview of attention for article published in Bioorganic & Medicinal Chemistry Letters, February 2014
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About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (90th percentile)
  • High Attention Score compared to outputs of the same age and source (96th percentile)

Mentioned by

blogs
1 blog
patent
14 patents

Citations

dimensions_citation
69 Dimensions

Readers on

mendeley
72 Mendeley
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Title
Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein
Published in
Bioorganic & Medicinal Chemistry Letters, February 2014
DOI 10.1016/j.bmcl.2014.02.010
Pubmed ID
Authors

Andrew M. Petros, Steven L. Swann, Danying Song, Kerren Swinger, Chang Park, Haichao Zhang, Michael D. Wendt, Aaron R. Kunzer, Andrew J. Souers, Chaohong Sun

Abstract

Apoptosis is regulated by the BCL-2 family of proteins, which is comprised of both pro-death and pro-survival members. Evasion of apoptosis is a hallmark of malignant cells. One way in which cancer cells achieve this evasion is thru overexpression of the pro-survival members of the BCL-2 family. Overexpression of MCL-1, a pro-survival protein, has been shown to be a resistance factor for Navitoclax, a potent inhibitor of BCL-2 and BCL-XL. Here we describe the use of fragment screening methods and structural biology to drive the discovery of novel MCL-1 inhibitors from two distinct structural classes. Specifically, cores derived from a biphenyl sulfonamide and salicylic acid were uncovered in an NMR-based fragment screen and elaborated using high throughput analog synthesis. This culminated in the discovery of selective and potent inhibitors of MCL-1 that may serve as promising leads for medicinal chemistry optimization efforts.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 72 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Denmark 2 3%
United Kingdom 1 1%
Japan 1 1%
Germany 1 1%
Unknown 67 93%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 19 26%
Researcher 17 24%
Student > Doctoral Student 5 7%
Other 5 7%
Student > Bachelor 4 6%
Other 9 13%
Unknown 13 18%
Readers by discipline Count As %
Chemistry 23 32%
Agricultural and Biological Sciences 14 19%
Pharmacology, Toxicology and Pharmaceutical Science 9 13%
Biochemistry, Genetics and Molecular Biology 9 13%
Engineering 2 3%
Other 3 4%
Unknown 12 17%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 14. 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 08 December 2022.
All research outputs
#2,638,586
of 25,373,627 outputs
Outputs from Bioorganic & Medicinal Chemistry Letters
#321
of 13,779 outputs
Outputs of similar age
#31,036
of 330,518 outputs
Outputs of similar age from Bioorganic & Medicinal Chemistry Letters
#4
of 110 outputs
Altmetric has tracked 25,373,627 research outputs across all sources so far. Compared to these this one has done well and is in the 89th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 13,779 research outputs from this source. They receive a mean Attention Score of 4.9. This one has done particularly well, scoring higher than 97% 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 330,518 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 90% of its contemporaries.
We're also able to compare this research output to 110 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 96% of its contemporaries.