Evidence map›Paper›PMID 28605671›Full record

ReviewCurrent opinion in chemical biology2017

Targeted protein knockdown using small molecule degraders.

Kanak Raina, Craig M Crews

Open access · greenAbstract readReview
In one paragraph

Review in Current opinion in chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 56 papers.

0numbers the graph read from it
0cells of the map it votes in
56citing papers in PubMed
5.7field-weighted citation impact, top 3% 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

56 citing papers in PubMed, 111 citations in OpenAlex.

  1. Review
  2. Article
  3. Discovery of SKP2-Recruiting PROTACs for Target Protein Degradation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026
    Article
  4. Review
  5. Article
  6. Article
  7. Review
  8. EGFR: New Insights on Its Activation and Mutation in Tumor and Tumor Immunotherapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025
    Review
  9. Review
  10. The Role of CELMoD Agents in Multiple Myeloma.OncoTargets and therapy · 2025
    Review
  11. The tumor-intrinsic role of the mScience immunology · 2024
    Article
  12. Review
  13. Article
  14. Review
  15. Ubiquitination of Immune System and Cancer Therapy.Advances in experimental medicine and biology · 2024
    Review
  16. Review
  17. Article
  18. Review
  19. Review
  20. A comprehensive review of SHP2 and its role in cancer.Cellular oncology (Dordrecht, Netherlands) · 2022
    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

2 authors at 2 institutions in 1 country.

Kanak RainaArvinas LLC, New Haven, CT 06511, United States.
Craig M CrewsDepartment of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT 06520, United States; Department of Chemistry, Yale University, New Haven, CT 06520, United States; Department of Pharmacology, Yale University, New Haven, CT 06520, United States. Electronic address: craig.crews@yale.edu.
Arvinas (United States) · USYale University · US

Funding

Inducing Proximity: An Emerging Paradigm for New Therapeutic ModalitiesR35CA197589 · NCI · YALE UNIVERSITY · PI CRAIG M CREWS · 2015 to 2026
$10.7M
NCI NIH HHS R35 CA197589
6 · The paper itself

Abstract

Small molecule probes of biological systems have traditionally been designed to bind to and inhibit the active sites of their protein targets. While this class of pharmacological agents has been broadened by the development of a small number of allosteric and protein-protein interaction (PPI) inhibitors, conventional drug design still excludes 'undruggable' proteins that are neither enzymes nor receptors. Recent years have seen the emergence of new classes of small molecules that can target hitherto undruggable proteins by recruiting the cellular proteostasis machinery to selectively tag them for degradation. These molecules, especially the class known as Proteolysis Targeting Chimera (PROTACs), represent a paradigm shift in chemical genetics, but their most tantalizing potential is as novel therapeutic agents. This review briefly summarizes the preclinical development of small molecule-based protein degraders, and describes the recent improvements in the technology that have positioned PROTACs on the cusp of entering the clinic.

Indexed as

Amino Acid SequenceAnimalsHumansProteinsProteolysisSmall Molecule LibrariesProteinsSmall Molecule Libraries

Identifiers

PMID28605671
PMCPMC5584562
OpenAlexW2621934513

What OpenQuestion holds

Textmetadata
LicenceTDM
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.