Evidence map›Paper›PMID 27798265›Full record

ArticleScience translational medicine2016

Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer.

Lu Zhang, Panayotis C Theodoropoulos, Ugur Eskiocak, Wentian Wang, Young-Ah Moon, Bruce Posner, Noelle S Williams, Woodring E Wright, Sang Bum Kim, Deepak Nijhawan and 2 more

Open access · greenAbstract read
In one paragraph

Article in Science translational medicine, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
48citing papers in PubMed, 1 pooled it
5.2field-weighted citation impact, top 4% 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

48 citing papers in PubMed, 1 synthesis or guideline pooled it, 85 citations in OpenAlex.

  1. Pooled it
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  7. Review
  8. Trimming the fat from Dishevelled.Nature chemical biology · 2025
    Article
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  20. Identification of a novel CNV at theFrontiers in molecular biosciences · 2023
    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

12 authors at 2 institutions in 1 country.

Lu ZhangDepartment of Cell Biology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Panayotis C TheodoropoulosDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Ugur EskiocakChildren's Medical Center Research Institute, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Wentian WangDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Young-Ah MoonDepartment of Molecular Medicine, Inha University College of Medicine, 100 Inha-ro, Nam-gu, Incheon 22212, Korea.
Bruce PosnerDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Noelle S WilliamsDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Woodring E WrightDepartment of Cell Biology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Sang Bum KimDepartment of Cell Biology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Deepak NijhawanDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Jef K De BrabanderDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Jerry W ShayDepartment of Cell Biology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. jerry.shay@utsouthwestern.edu.
The University of Texas Southwestern Medical Center · USChildren's Medical Center · US

Funding

UT Southwestern Medical Center Simmons Comprehensive Cancer CenterP30CA142543 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI Sandi Leigh Pruitt · 2010 to 2026
$53.7M
Structure guided discovery of small molecule antagonists of Smac (DIABLO)/XIPAP01CA095471 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI FRANTZ, DOUGLAS E · 2002 to 2011
$34.1M
Cell Biology Research Improvements and RenovationsC06RR030414 · NCRR · UT SOUTHWESTERN MEDICAL CENTER · PI FITZ, JOHN GREGORY · 2010 to 2010
$15.0M
In Cell Analyzer 6000 for UTSW HTS CoreS10OD018005 · OD · UT SOUTHWESTERN MEDICAL CENTER · PI POSNER, BRUCE ARTHUR · 2014 to 2014
$598k
NCI NIH HHS P01 CA095471NCI NIH HHS P30 CA142543NCRR NIH HHS C06 RR030414NIH HHS S10 OD018005
6 · The paper itself

Abstract

Mutations in the adenomatous polyposis coli (APC) gene are common in colorectal cancer (CRC), and more than 90% of those mutations generate stable truncated gene products. We describe a chemical screen using normal human colonic epithelial cells (HCECs) and a series of oncogenically progressed HCECs containing a truncated APC protein. With this screen, we identified a small molecule, TASIN-1 (truncated APC selective inhibitor-1), that specifically kills cells with APC truncations but spares normal and cancer cells with wild-type APC. TASIN-1 exerts its cytotoxic effects through inhibition of cholesterol biosynthesis. In vivo administration of TASIN-1 inhibits tumor growth of CRC cells with truncated APC but not APC wild-type CRC cells in xenograft models and in a genetically engineered CRC mouse model with minimal toxicity. TASIN-1 represents a potential therapeutic strategy for prevention and intervention in CRC with mutant APC.

Indexed as

Molecular Targeted TherapyAdenomatous Polyposis Coli ProteinAnimalsCell ProliferationCholesterolColonic NeoplasmsColorectal NeoplasmsFemaleGenes, Tumor SuppressorHCT116 CellsHumansMaleMiceMice, NudeMutationPiperidinesAdenomatous Polyposis Coli ProteinCholesterolPiperidinesSREBF2 protein, humanSterol Regulatory Element Binding Protein 2SulfonamidesTASIN-1 compound

Identifiers

PMID27798265
PMCPMC7262871
OpenAlexW2532861674

What OpenQuestion holds

Textmetadata
LicenceTDM
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.