Evidence map›Paper›PMID 17993409›Full record

ReviewDrug discovery today2007

Kinase packing defects as drug targets.

Alejandro Crespo, Ariel Fernández

Erratum issuedOpen access · greenAbstract readReview
In one paragraph

Review in Drug discovery today, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
1.6field-weighted citation impact, top 17% 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

0 citing papers in PubMed, 23 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

  • Erratum issued
5 · Who and what money

Authors and funding

2 authors at 1 institution in 1 country.

Alejandro CrespoDepartment of Bioengineering, Rice University, Houston, TX 77005, United States. alecrespo@rice.edu
Ariel Fernández
Rice University · US

Funding

Protein Packing Defects as Functional Markers and Drug TargetsR01GM072614 · NIGMS · RICE UNIVERSITY · PI FERNANDEZ, ARIEL · 2005 to 2008
$1.2M
NIGMS NIH HHS R01 GM072614NIGMS NIH HHS R01-GM072614
6 · The paper itself

Abstract

Protein kinases constitute major targets in molecular cancer therapy. The structural conservation of kinases causes specificity problems in most drug inhibitors, often resulting in dangerous side effects. Here we survey recent approaches in drug design that exploit a molecular marker for specificity: the pattern of packing defects. These packing defects are solvent-exposed intramolecular hydrogen bonds that may be protected by drugs upon association. In this light, we review design strategies to achieve paralogue discrimination, to control cross reactivity and to overcome drug resistance induced by target mutations.

Indexed as

Drug DesignAnimalsAntineoplastic AgentsBenzamidesCross ReactionsDrug Resistance, NeoplasmHumansHydrogen BondingImatinib MesylatePiperazinesProtein Kinase InhibitorsProtein KinasesPyrimidinesAntineoplastic AgentsBenzamidesImatinib MesylatePiperazinesProtein Kinase InhibitorsProtein KinasesPyrimidines

Identifiers

PMID17993409
PMCPMC2136416
OpenAlexW2011368575

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.