Evidence map›Paper›PMID 33997272›Full record

ArticleAdvanced therapeutics2021

SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C.

Peter D Koch, Jeremy Quintana, Maaz Ahmed, Rainer H Kohler, Ralph Weissleder

Abstract read
In one paragraph

Article in Advanced therapeutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
–field-weighted citation impact
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

5 citing papers in PubMed.

  1. Chemical Genetic Targeting of the LRRK2 GTPase Domain.bioRxiv : the preprint server for biology · 2026
    Article
  2. Article
  3. Molecular Imaging: Unveiling Metabolic Abnormalities in Pancreatic Cancer.International journal of molecular sciences · 2025
    Review
  4. Preclinical Evaluation of [ACS pharmacology & translational science · 2024
    Article
  5. In Vivo Click Chemistry Enables Multiplexed Intravital Microscopy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022
    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

5 authors.

Peter D KochCenter for Systems Biology, Massachusetts General Hospital, 185 Cambridge St, CPZN 5206, Boston, MA 02114.
Jeremy QuintanaCenter for Systems Biology, Massachusetts General Hospital, 185 Cambridge St, CPZN 5206, Boston, MA 02114.
Maaz AhmedCenter for Systems Biology, Massachusetts General Hospital, 185 Cambridge St, CPZN 5206, Boston, MA 02114.
Rainer H KohlerCenter for Systems Biology, Massachusetts General Hospital, 185 Cambridge St, CPZN 5206, Boston, MA 02114.
Ralph WeisslederCenter for Systems Biology, Massachusetts General Hospital, 185 Cambridge St, CPZN 5206, Boston, MA 02114.

Funding

Training Grant in Molecular Imaging Research (MGH/HMS)T32CA079443 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI WEISSLEDER, MD, PHD, RALPH · 2000 to 2025
$10.1M
Cellular mechanisms by which exhausted T cell responses are restoredR01AI123349 · NIAID · MASSACHUSETTS GENERAL HOSPITAL · PI Thorsten Roman Mempel · 2017 to 2026
$4.5M
Imaging of nanotherapeutic drug actionU01CA206997 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI WEISSLEDER, MD, PHD, RALPH · 2017 to 2021
$2.9M
Imaging tumor associated macrophage (TAM) functionR01CA206890 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI PITTET, MIKAEL, WEISSLEDER, MD, PHD, RALPH · 2017 to 2021
$1.9M
Analysis of scant cancer cells in fine needle aspiratesR33CA202064 · NCI · MASSACHUSETTS GENERAL HOSPITAL · PI WEISSLEDER, MD, PHD, RALPH · 2016 to 2018
$1.3M
NCI NIH HHS R01 CA206890NCI NIH HHS R33 CA202064NCI NIH HHS T32 CA079443NCI NIH HHS U01 CA206997NIAID NIH HHS R01 AI123349
6 · The paper itself

Abstract

Multiple potent covalent inhibitors for mutant KRAS G12C have been described and some are in clinical trials. These small molecule inhibitors potentially allow for companion imaging probe development, thereby expanding the chemical biology toolkit to investigate mutant KRAS biology. Herein, we synthesized and tested a series of fluorescent companion imaging drugs (CID) for KRAS G12C, using two scaffolds, ARS-1323 and AMG-510. We created four fluorescent derivatives of each by attaching BODIPY dyes. We found that two fluorescent derivatives (BODIPY FL and BODIPY TMR) of ARS-1323 bind mutant KRAS and can be used for biochemical binding screens. Unfortunately, these drugs could not be used as direct imaging agents in cells, likely because of non-specific membrane labeling. To circumvent this challenge, we then used a two step procedure in cancer cells where an ARS-1323 alkyne is used for target binding followed by fluorescence imaging after

Indexed as

Companion imaging drugin situ click chemistryKRAS G12C inhibitors

Identifiers

PMID33997272
PMCPMC8115719

What OpenQuestion holds

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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.