Evidence map›Paper›PMID 22218294›Full record

ReviewNature structural & molecular biology2012

New approaches for dissecting protease functions to improve probe development and drug discovery.

Edgar Deu, Martijn Verdoes, Matthew Bogyo

Abstract readReview
In one paragraph

Review in Nature structural & molecular biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 62 papers.

0numbers the graph read from it
0cells of the map it votes in
62citing 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

62 citing papers in PubMed.

  1. Praluzatamab Ravtansine, a CD166-Targeting Antibody-Drug Conjugate, in Patients with Advanced Solid Tumors: An Open-Label Phase I/II Trial.Clinical cancer research : an official journal of the American Association for Cancer Research · 2022
    Trial
  2. Article
  3. Review
  4. Achieving protease substrate-specific inhibition by mAb dual functional selections.Protein science : a publication of the Protein Society · 2026
    Article
  5. Article
  6. Review
  7. Article
  8. Article
  9. Generation of Protease Inhibitory Antibodies by Functional In Vivo Selection.Methods in molecular biology (Clifton, N.J.) · 2024
    Article
  10. Article
  11. Substrate derived sequences act as subsite-blocking motifs in protease inhibitory antibodies.Protein science : a publication of the Protein Society · 2023
    Article
  12. Molecular Engineering of Self-Immolative Bioresponsive MR Probes.Journal of the American Chemical Society · 2023
    Article
  13. Review
  14. Approaches to Avoid Proteolysis During Protein Expression and Purification.Methods in molecular biology (Clifton, N.J.) · 2023
    Article
  15. Article
  16. Article
  17. Review
  18. Review
  19. Article
  20. Review

2 more citing papers are in PubMed but not listed here.

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.

Edgar DeuDepartment of Pathology, Stanford University School of Medicine, Stanford, California, USA.
Martijn Verdoes
Matthew Bogyo

Funding

Small Molecule Imaging of Protease ActivityR01EB005011 · NIBIB · STANFORD UNIVERSITY · PI BOGYO, MATTHEW · 2005 to 2013
$3.0M
Chemically Mapping Malarial Rupture ProteasesR01AI078947 · NIAID · STANFORD UNIVERSITY · PI BOGYO, MATTHEW · 2009 to 2013
$2.0M
Development of small molecule probes of matrix metallo protease functionR21EB012311 · NIBIB · STANFORD UNIVERSITY · PI BOGYO, MATTHEW · 2010 to 2010
$240k
NIAID NIH HHS R01 AI078947NIBIB NIH HHS R01 EB005011NIBIB NIH HHS R21 EB012311
6 · The paper itself

Abstract

Proteases are well-established targets for pharmaceutical development because of their known enzymatic mechanism and their regulatory roles in many pathologies. However, many potent clinical lead compounds have been unsuccessful either because of a lack of specificity or because of our limited understanding of the biological roles of the targeted protease. In order to successfully develop protease inhibitors as drugs, it is necessary to understand protease functions and to expand the platform of inhibitor development beyond active site-directed design and in vitro optimization. Several newly developed technologies will enhance assessment of drug selectivity in living cells and animal models, allowing researchers to focus on compounds with high specificity and minimal side effects in vivo. In this review, we highlight advances in the development of chemical probes, proteomic methods and screening tools that we feel will help facilitate this paradigm shift in drug discovery.

Indexed as

AnimalsBiocatalysisDrug DiscoveryHumansModels, ChemicalMolecular StructurePeptide HydrolasesProtease InhibitorsProteolysisProteomicsPeptide HydrolasesProtease Inhibitors

Identifiers

PMID22218294
PMCPMC3513415

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.