Evidence map›Paper›PMID 33209191›Full record

ArticleACS medicinal chemistry letters2020

Targeted Covalent Inhibition of

Thomas C Atack, Donald D Raymond, Christa A Blomquist, Charisse Flerida Pasaje, Patrick R McCarren, Jamie Moroco, Henock B Befekadu, Foxy P Robinson, Debjani Pal, Lisl Y Esherick and 3 more

Open access · hybridAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.2field-weighted citation impact, top 22% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

9 citing papers in PubMed, 18 citations in OpenAlex.

  1. Review
  2. Barbituric Acid Derivatives as Covalent Inhibitors ofJournal of medicinal chemistry · 2025
    Article
  3. Article
  4. Article
  5. Review
  6. Article
  7. Article
  8. Structural insights intoFrontiers in cellular and infection microbiology · 2022
    Review
  9. Development of NanoBRET-Binding Assays for FKBP-Ligand Profiling in Living Cells.Chembiochem : a European journal of chemical biology · 2021
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors at 2 institutions in 1 country.

Thomas C AtackBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Donald D RaymondBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Christa A BlomquistBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Charisse Flerida PasajeDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
Patrick R McCarrenBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Jamie MorocoBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Henock B BefekaduBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Foxy P RobinsonBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Debjani PalBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Lisl Y EsherickDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
Alessandra IanariBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Jacquin C NilesDepartment of Biological Engineering, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, United States.
William R SellersBroad Institute of MIT and Harvard, 415 Main Street, Cambridge, Massachusetts 02142, United States.
Broad Institute · USMassachusetts Institute of Technology · US

Funding

TRAINING GRANTS IN ENVIROMENTAL TOXICOLOGYT32ES007020 · NIEHS · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI ESSIGMANN, JOHN M · 1985 to 2024
$13.1M
NIEHS NIH HHS T32 ES007020
6 · The paper itself

Abstract

FK506-binding protein 35, FKBP35, has been implicated as an essential malarial enzyme. Rapamycin and FK506 exhibit antiplasmodium activity in cultured parasites. However, due to the highly conserved nature of the binding pockets of FKBPs and the immunosuppressive properties of these drugs, there is a need for compounds that selectively inhibit FKBP35 and lack the undesired side effects. In contrast to human FKBPs, FKBP35 contains a cysteine, C106, adjacent to the rapamycin binding pocket, providing an opportunity to develop targeted covalent inhibitors of

Identifiers

PMID33209191
PMCPMC7667655
OpenAlexW3081835244

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.