Evidence map›Paper›PMID 25205195›Full record

ArticleBioorganic & medicinal chemistry letters2014

Imidazo[1,2-a]pyridine-based peptidomimetics as inhibitors of Akt.

Young B Kim, Chang Won Kang, Sujeewa Ranatunga, Hua Yang, Said M Sebti, Juan R Del Valle

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. 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. Imidazo[1,2‑ACS omega · 2026
    Review
  2. Article
  3. Article
  4. Article
  5. 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

6 authors.

Young B KimDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Chang Won KangDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Sujeewa RanatungaDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Hua YangDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Said M SebtiDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Juan R Del ValleDrug Discovery Department, H. Lee Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.

Funding

TRANSLATIONAL RESEARCHP30CA076292 · NCI · UNIVERSITY OF SOUTH FLORIDA · PI KENNETH Lynn WRIGHT · 1998 to 2026
$93.5M
Targeting Akt with substrate mimetic antagonistsR21CA167215 · NCI · H. LEE MOFFITT CANCER CTR & RES INST · PI DEL VALLE, JUAN R · 2012 to 2013
$392k
NCI NIH HHS P30 CA076292NCI NIH HHS P30CA76292NCI NIH HHS R21 CA167215NCI NIH HHS R21CA167215
6 · The paper itself

Abstract

We report the design, synthesis, and biological evaluation of imidazopyridine-based peptidomimetics based on the substrate consensus sequence of Akt, an AGC family serine/threonine kinase hyperactivated in over 50% of human tumors. Our ligand-based approach led to the identification of novel substrate mimetic inhibitors of Akt1 featuring an unnatural extended dipeptide surrogate. Compound 11 inhibits Akt isoforms in the sub-micromolar range and exhibits improved proteolytic stability relative to a parent pentapeptide.

Indexed as

Dose-Response Relationship, DrugHumansMolecular StructurePeptidomimeticsProtein Kinase InhibitorsProto-Oncogene Proteins c-aktPyridinesStructure-Activity Relationshipimidazo(1,2-a)pyridinePeptidomimeticsProtein Kinase InhibitorsProto-Oncogene Proteins c-aktPyridinesDipeptide surrogateKinase inhibitorPeptide mimicβ-Strand mimic

Identifiers

PMID25205195
PMCPMC4176526

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.