Evidence map›Paper›PMID 36544740›Full record

ArticleChemical science2022

Structure-guided design and characterization of a clickable, covalent PARP16 inhibitor.

Daniel S Bejan, Sunil Sundalam, Haihong Jin, Rory K Morgan, Ilsa T Kirby, Ivan R Siordia, Barr Tivon, Nir London, Michael S Cohen

Open access · diamondAbstract read
In one paragraph

Article in Chemical science, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed, 1 pooled it
1.5field-weighted citation impact, top 15% 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

11 citing papers in PubMed, 1 synthesis or guideline pooled it, 14 citations in OpenAlex.

  1. Pooled it
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  4. Review
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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

9 authors at 2 institutions in 2 countries.

Daniel S BejanDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.ORCID https://orcid.org/0000-0002-5090-0299
Sunil SundalamDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.
Haihong JinDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.
Rory K MorganDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.ORCID https://orcid.org/0000-0003-0194-0304
Ilsa T KirbyDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.
Ivan R SiordiaDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.
Barr TivonDepartment of Chemical and Structural Biology, The Weizmann Institute of Science Rehovot 7610001 Israel.
Nir LondonDepartment of Chemical and Structural Biology, The Weizmann Institute of Science Rehovot 7610001 Israel.ORCID https://orcid.org/0000-0003-2687-0699
Michael S CohenDepartment of Chemical Physiology and Biochemistry, Oregon Health & Science University Portland OR 97239 USA cohenmic@ohsu.edu.ORCID https://orcid.org/0000-0002-7636-4156
Oregon Health & Science University · USWeizmann Institute of Science · IL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

PARP16-the sole ER-resident PARP family member-is gaining attention as a potential therapeutic target for cancer treatment. Nevertheless, the precise function of the catalytic activity of PARP16 is poorly understood. This is primarily due to the lack of inhibitors that are selective for PARP16 over other PARP family members. Herein, we describe a structure-guided strategy for generating a selective PARP16 inhibitor by incorporating two selectivity determinants into a phthalazinone pan-PARP inhibitor scaffold: (i) an acrylamide-based inhibitor (DB008) designed to covalently react with a non-conserved cysteine (Cys169, human numbering) in the NAD

Identifiers

PMID36544740
PMCPMC9710212
OpenAlexW4312113337

What Socratic holds

Textmetadata
LicenceCC BY-NC
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 Socratic graph.