Evidence map›Paper›PMID 34114360›Full record

ReviewChemMedChem2021

Chemical and Structural Strategies to Selectively Target mTOR Kinase.

Chiara Borsari, Martina De Pascale, Matthias P Wymann

Open access · hybridAbstract readReview
In one paragraph

Review in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.1field-weighted citation impact, top 24% 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

12 citing papers in PubMed, 23 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Synthesis andACS omega · 2026
    Article
  5. Article
  6. Review
  7. Review
  8. Review
  9. Article
  10. Article
  11. Article
  12. 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

3 authors at 1 institution in 1 country.

Chiara BorsariDepartment of Biomedicine, University of Basel, Mattenstrasse 28, 4058, Basel, Switzerland.ORCID 0000-0002-4688-8362
Martina De PascaleDepartment of Biomedicine, University of Basel, Mattenstrasse 28, 4058, Basel, Switzerland.
Matthias P WymannDepartment of Biomedicine, University of Basel, Mattenstrasse 28, 4058, Basel, Switzerland.
University of Basel · CH

Funding

Innosuisse 37213.1Novartis Foundation 14B095Stiftung für Krebsbekämpfung 341Swiss Commission for Technology and Innovation 17241.1Swiss National Science Foundation 310030_189065
6 · The paper itself

Abstract

Dysregulation of the mechanistic target of rapamycin (mTOR) pathway is implicated in cancer and neurological disorder, which identifies mTOR inhibition as promising strategy for the treatment of a variety of human disorders. First-generation mTOR inhibitors include rapamycin and its analogues (rapalogs) which act as allosteric inhibitors of TORC1. Structurally unrelated, ATP-competitive inhibitors that directly target the mTOR catalytic site inhibit both TORC1 and TORC2. Here, we review investigations of chemical scaffolds explored for the development of highly selective ATP-competitive mTOR kinase inhibitors (TORKi). Extensive medicinal chemistry campaigns allowed to overcome challenges related to structural similarity between mTOR and the phosphoinositide 3-kinase (PI3K) family. A broad region of chemical space is covered by TORKi. Here, the investigation of chemical substitutions and physicochemical properties has shed light on the compounds' ability to cross the blood brain barrier (BBB). This work provides insights supporting the optimization of TORKi for the treatment of cancer and central nervous system disorders.

Indexed as

Dose-Response Relationship, DrugHumansMolecular StructureProtein Kinase InhibitorsStructure-Activity RelationshipTOR Serine-Threonine KinasesMTOR protein, humanProtein Kinase InhibitorsTOR Serine-Threonine KinasesBBB permeabilitybinding modeschemical scaffoldsmTOR inhibitorsphysicochemical properties

Identifiers

PMID34114360
PMCPMC8518124
OpenAlexW3169938155

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.