Evidence map›Paper›PMID 31226791›Full record

ArticleMolecules (Basel, Switzerland)2019

Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties.

Anthony W Partridge, Hung Yi Kristal Kaan, Yu-Chi Juang, Ahmad Sadruddin, Shuhui Lim, Christopher J Brown, Simon Ng, Dawn Thean, Fernando Ferrer, Charles Johannes and 13 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed, 1 pooled it
3.5field-weighted citation impact, top 7% 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

22 citing papers in PubMed, 1 synthesis or guideline pooled it, 54 citations in OpenAlex.

  1. Passion fruit (Frontiers in nutrition · 2024
    Pooled it
  2. Review
  3. Review
  4. Article
  5. Article
  6. Article
  7. Review
  8. Article
  9. Article
  10. Review
  11. Review
  12. Review
  13. Article
  14. Stapled β-Hairpins Featuring 4-Mercaptoproline.Journal of the American Chemical Society · 2021
    Article
  15. Article
  16. Review
  17. Article
  18. Stapled Peptide Inhibitors of Autophagy Adapter LC3B.Chembiochem : a European journal of chemical biology · 2020
    Article
  19. Review
  20. Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors.Bioorganic & medicinal chemistry · 2020
    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

23 authors at 3 institutions in 2 countries.

Anthony W PartridgeMSD International, 8 Biomedical Grove, #04-01/05 Neuros Building, Singapore 138665, Singapore. anthony_partridge@merck.com.ORCID 0000-0001-8568-2079
Hung Yi Kristal KaanMSD International, 8 Biomedical Grove, #04-01/05 Neuros Building, Singapore 138665, Singapore. kristal.kaan@merck.com.
Yu-Chi JuangMSD International, 8 Biomedical Grove, #04-01/05 Neuros Building, Singapore 138665, Singapore. angela.juang@merck.com.
Ahmad SadruddinMSD International, 8 Biomedical Grove, #04-01/05 Neuros Building, Singapore 138665, Singapore. ahmad.sadruddin@merck.com.
Shuhui LimMSD International, 8 Biomedical Grove, #04-01/05 Neuros Building, Singapore 138665, Singapore. shuhui.lim@merck.com.
Christopher J Brownp53Lab, Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove, #06-04/05 Neuros/Immunos, Singapore 138648, Singapore. CJBrown@p53lab.a-star.edu.sg.
Simon Ngp53Lab, Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove, #06-04/05 Neuros/Immunos, Singapore 138648, Singapore. simon.ng@merck.com.ORCID 0000-0001-6778-0820
Dawn Theanp53Lab, Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove, #06-04/05 Neuros/Immunos, Singapore 138648, Singapore. dthean@p53Lab.a-star.edu.sg.
Fernando Ferrerp53Lab, Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove, #06-04/05 Neuros/Immunos, Singapore 138648, Singapore. fjferrer@p53Lab.a-star.edu.sg.
Charles JohannesInstitute of Chemical and Engineering Sciences (ICES), Agency for Science, Technology and Research (A*STAR), 8 Biomedical Grove, #07, Neuros Building, Singapore 138665, Singapore. charles_johannes@p53lab.a-star.edu.sg.ORCID 0000-0002-5170-058X
Tsz Ying YuenInstitute of Chemical and Engineering Sciences (ICES), Agency for Science, Technology and Research (A*STAR), 8 Biomedical Grove, #07, Neuros Building, Singapore 138665, Singapore. yuenty@ices.a-star.edu.sg.
Srinivasaraghavan KannanBioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, #07-01 Matrix, Singapore 138671, Singapore. raghavk@bii.a-star.edu.sg.
Pietro AronicaBioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, #07-01 Matrix, Singapore 138671, Singapore. pietroa@bii.a-star.edu.sg.ORCID 0000-0002-2927-8378
Yaw Sing TanBioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, #07-01 Matrix, Singapore 138671, Singapore. tanys@bii.a-star.edu.sg.
Mohan R PradhanBioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, #07-01 Matrix, Singapore 138671, Singapore. mohanrp@bii.a-star.edu.sg.
Chandra S VermaBioinformatics Institute (BII), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, #07-01 Matrix, Singapore 138671, Singapore. chandra@bii.a-star.edu.sg.
Jerome HochmanMerck & Co., Inc., West Point, PA 19486, USA. jerome_hochman@merck.com.
Shiying ChenMerck & Co., Inc., Kenilworth, NJ 07033, USA. shiying.chen@merck.com.
Hui WanMerck & Co., Inc., Kenilworth, NJ 07033, USA. hui.wan@merck.com.
Sookhee HaMerck & Co., Inc., Kenilworth, NJ 07033, USA. sookhee_ha@merck.com.
Brad SherborneMerck & Co., Inc., Kenilworth, NJ 07033, USA. tomi.sawyer@merck.com.
David P Lanep53Lab, Agency for Science, Technology and Research (A*STAR), 8A Biomedical Grove, #06-04/05 Neuros/Immunos, Singapore 138648, Singapore. dplane@p53Lab.a-star.edu.sg.
Tomi K SawyerMerck & Co., Inc., Boston, MA 02115, USA. sawyerkrt@aol.com.
Agency for Science, Technology and Research · SGMerck & Co., Inc., Rahway, NJ, USA (United States) · USUnited States Military Academy · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Stapled α-helical peptides represent an emerging superclass of macrocyclic molecules with drug-like properties, including high-affinity target binding, protease resistance, and membrane permeability. As a model system for probing the chemical space available for optimizing these properties, we focused on dual Mdm2/MdmX antagonist stapled peptides related to the p53 N-terminus. Specifically, we first generated a library of ATSP-7041 (Chang et al., 2013) analogs iteratively modified by L-Ala and D-amino acids. Single L-Ala substitutions beyond the Mdm2/(X) binding interfacial residues (i.e., Phe

Indexed as

Protein ConformationAmino AcidsAmino Acid SequenceAmino Acid SubstitutionCell-Penetrating PeptidesCircular DichroismDipeptidesHumansOligopeptidesPeptide FragmentsPeptides, CyclicPermeabilityProtein Structure, SecondaryProto-Oncogene Proteins c-mdm2alanylalanineAmino AcidsATSP-7041Cell-Penetrating PeptidesDipeptidesleucyl-seryl-glutamyl-leucineOligopeptidesPeptide FragmentsPeptides, CyclicProto-Oncogene Proteins c-mdm2D-amino acidhelix-breakermacrocyclic peptidepeptide permeabilitystapled peptide

Identifiers

PMID31226791
PMCPMC6632053
OpenAlexW2951116619

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.