Evidence map›Paper›PMID 34795874›Full record

ArticleACS medicinal chemistry letters2021

Discovery and Development of Cyclic Peptide Inhibitors of CIB1.

Victoria A Haberman, Steven R Fleming, Tina M Leisner, Ana C Puhl, Emerald Feng, Ling Xie, Xian Chen, Yuki Goto, Hiroaki Suga, Leslie V Parise and 3 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
2.8field-weighted citation impact, top 9% 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

15 citing papers in PubMed, 29 citations in OpenAlex.

  1. HFGuidedDesign:Chemical science · 2026
    Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Identification of Covalent Cyclic Peptide Inhibitors in mRNA Display.Journal of the American Chemical Society · 2023
    Article
  10. Tyrosinase-Catalyzed Peptide Macrocyclization for mRNA Display.Journal of the American Chemical Society · 2023
    Article
  11. Cell-free Biosynthesis of Peptidomimetics.Biotechnology and bioprocess engineering : BBE · 2023
    Review
  12. Article
  13. Article
  14. Review
  15. 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

13 authors at 3 institutions in 2 countries.

Victoria A HabermanDivision of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Steven R FlemingDivision of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Tina M LeisnerCenter for Integrative Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Ana C PuhlCenter for Integrative Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID https://orcid.org/0000-0002-1456-8882
Emerald FengDepartment of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Ling XieDepartment of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Xian ChenDepartment of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Yuki GotoDepartment of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.ORCID https://orcid.org/0000-0003-4317-0790
Hiroaki SugaDepartment of Chemistry, Graduate School of Science, The University of Tokyo, Tokyo 113-0033, Japan.ORCID https://orcid.org/0000-0002-5298-9186
Leslie V PariseDepartment of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Dmitri KireevCenter for Integrative Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID https://orcid.org/0000-0001-8479-8555
Kenneth H PearceCenter for Integrative Chemical Biology and Drug Discovery, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
Albert A BowersDivision of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, United States.ORCID https://orcid.org/0000-0001-8214-7484
University of North Carolina at Chapel Hill · USJapan Science and Technology Agency · JPThe University of Tokyo · JP

Funding

MIRA Equipment SupplementR35GM125005 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Albert A Bowers · 2017 to 2026
$3.9M
Molecular mechanisms of CIB1 signalingR01GM133107 · NIGMS · UNIV OF NORTH CAROLINA CHAPEL HILL · PI CHEN, XIAN · 2019 to 2020
$617k
NIGMS NIH HHS R01 GM133107NIGMS NIH HHS R35 GM125005
6 · The paper itself

Abstract

Calcium and integrin binding protein 1 (CIB1) is a small, intracellular protein recently implicated in survival and proliferation of triple-negative breast cancer (TNBC). Considering its interactions with PAK1 and downstream signaling, CIB1 has been suggested as a potential therapeutic target in TNBC. As such, CIB1 has been the focus of inhibitor discovery efforts. To overcome issues of potency and stability in previously reported CIB1 inhibitors, we deploy mRNA display to discover new cyclic peptide inhibitors with improved biophysical properties and cellular activity. We advance UNC10245131, a cyclic peptide with low nanomolar affinity and good selectivity for CIB1 over other EF-hand domain proteins and improved permeability and stability over previously identified linear peptide inhibitor UNC10245092. Unlike UNC10245092, UNC10245131 lacks cytotoxicity and does not affect downstream signaling. Despite this, UNC10245131 is a potent ligand that could aid in clarifying roles of CIB1 in TNBC survival and proliferation and other CIB1-associated biological phenotypes.

Identifiers

PMID34795874
PMCPMC8591747
OpenAlexW3208692306

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.