Evidence map›Paper›PMID 37197477›Full record

ArticleACS medicinal chemistry letters2023

Rational Design of Highly Potent and Selective Covalent MAP2K7 Inhibitors.

Dalton R Kim, Meghan J Orr, Ada J Kwong, Kristine K Deibler, Hasan H Munshi, Cory Seth Bridges, Taylor Jie Chen, Xiaoyu Zhang, H Daniel Lacorazza, Karl A Scheidt

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.2field-weighted citation impact, top 20% 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

3 citing papers in PubMed, 4 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
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

10 authors at 2 institutions in 1 country.

Dalton R KimDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.
Meghan J OrrDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.
Ada J KwongDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.ORCID https://orcid.org/0000-0003-2608-7442
Kristine K DeiblerDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.
Hasan H MunshiDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.
Cory Seth BridgesDepartment of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.ORCID https://orcid.org/0000-0002-5200-2513
Taylor Jie ChenDepartment of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Xiaoyu ZhangDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.ORCID https://orcid.org/0000-0002-0951-9664
H Daniel LacorazzaDepartment of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, United States.
Karl A ScheidtDepartment of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.ORCID https://orcid.org/0000-0003-4856-3569
Northwestern University · USBaylor College of Medicine · US

Funding

MEDICAL SCIENTIST TRAINING PROGRAMT32GM008152 · NIGMS · NORTHWESTERN UNIVERSITY AT CHICAGO · PI ARDEHALI, HOSSEIN · 1987 to 2021
$24.0M
TRAINING PROGRAM IN CELL AND MOLECULAR BIOLOGYT32GM008231 · NIGMS · BAYLOR COLLEGE OF MEDICINE · PI NELSON, DAVID LOREN · 1990 to 2019
$7.2M
Chemistry of Life Processes Predoctoral Training ProgramT32GM105538 · NIGMS · NORTHWESTERN UNIVERSITY · PI KELLEHER, NEIL L · 2013 to 2022
$2.7M
Mechanisms of KLF4 suppression in pediatric leukemiaR01CA207086 · NCI · BAYLOR COLLEGE OF MEDICINE · PI LACORAZZA, DANIEL · 2017 to 2021
$1.8M
Discovery of Selective MAP2K4 Inhibitors to Target MetastasisR01CA188015 · NCI · NORTHWESTERN UNIVERSITY · PI SCHEIDT, KARL A · 2015 to 2017
$1.0M
The design, synthesis, and characterization of potent and selective MEK7 inhibitors as targeted therapies for T-cell acute lymphoblastic leukemiaF31CA228431 · NCI · NORTHWESTERN UNIVERSITY · PI KIM, DALTON ROBERT · 2018 to 2022
$196k
The design, synthesis, and evaluation of natural product-inspired small molecules targeting the 5-HT2C receptor as novel therapeutics for opioid use disorderF30DA050445 · NIDA · NORTHWESTERN UNIVERSITY · PI ORR, MEGHAN JO · 2020 to 2022
$134k
Synthesis, and Evaluation of Potent and Selective MEK4 Inhibitors as a Targeted Therapeutic for Metastatic Pancreatic Ductal AdenocarcinomaF31CA250353 · NCI · NORTHWESTERN UNIVERSITY · PI KWONG, ADA JADE · 2020 to 2021
$75k
NCI NIH HHS F31 CA228431NCI NIH HHS F31 CA250353NCI NIH HHS R01 CA188015NCI NIH HHS R01 CA207086NIDA NIH HHS F30 DA050445NIGMS NIH HHS T32 GM008152NIGMS NIH HHS T32 GM008231NIGMS NIH HHS T32 GM105538
6 · The paper itself

Abstract

The mitogen-activated protein kinase signaling cascade is conserved across eukaryotes, where it plays a critical role in the regulation of activities including proliferation, differentiation, and stress responses. This pathway propagates external stimuli through a series of phosphorylation events, which allows external signals to influence metabolic and transcriptional activities. Within the cascade, MEK, or MAP2K, enzymes occupy a molecular crossroads immediately upstream to significant signal divergence and cross-talk. One such kinase, MAP2K7, also known as MEK7 and MKK7, is a protein of great interest in the molecular pathophysiology underlying pediatric T cell acute lymphoblastic leukemia (T-ALL). Herein, we describe the rational design, synthesis, evaluation, and optimization of a novel class of irreversible MAP2K7 inhibitors. With a streamlined one-pot synthesis, favorable

Identifiers

PMID37197477
PMCPMC10184151
OpenAlexW4366158572

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.