Evidence map›Paper›PMID 33666424›Full record

ArticleJournal of medicinal chemistry2021

Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.

Jean-Olivier Zirimwabagabo, Ameera B A Jailani, Paris Avgoustou, Matthew J Tozer, Karl R Gibson, Paul A Glossop, James E J Mills, Roderick A Porter, Paul Blaney, Ning Wang and 3 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.7field-weighted citation impact, top 37% 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

3 citing papers in PubMed, 7 citations in OpenAlex.

  1. Review
  2. Review
  3. 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

13 authors at 5 institutions in 1 country.

Jean-Olivier ZirimwabagaboDepartment of Chemistry, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0002-4303-2139
Ameera B A JailaniDepartment of Oncology and Metabolism, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0001-9837-6062
Paris AvgoustouDepartment of Oncology and Metabolism, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0002-1642-1083
Matthew J TozerMatt Tozer Consultancy, Bognor Regis PO21 1DY, U.K.ORCID 0000-0002-9046-4065
Karl R GibsonSandexis Medicinal Chemistry Ltd., Sandwich, Kent CT13 9ND, U.K.ORCID 0000-0002-7967-8476
Paul A GlossopSandexis Medicinal Chemistry Ltd., Sandwich, Kent CT13 9ND, U.K.ORCID 0000-0001-6567-5648
James E J MillsSandexis Medicinal Chemistry Ltd., Sandwich, Kent CT13 9ND, U.K.ORCID 0000-0002-2567-3872
Roderick A PorterRod Porter Consultancy, Ashwell, Hertfordshire SG7 5PG, U.K.ORCID 0000-0001-8252-0429
Paul BlaneyConcept Life Sciences, High Peak SK23 0PG, U.K.ORCID 0000-0001-8121-8594
Ning WangDepartment of Oncology and Metabolism, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0002-2663-7515
Timothy M SkerryDepartment of Oncology and Metabolism, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0003-1319-5575
Gareth O RichardsDepartment of Oncology and Metabolism, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0001-7984-6882
Joseph P A HarrityDepartment of Chemistry, University of Sheffield, Sheffield S10 2TN, U.K.ORCID 0000-0001-5038-5699
University of Sheffield · GBPfizer (United Kingdom) · GBAshwell Museum · GBBognor Regis War Memorial Hospital · GBConcept Life Sciences (United Kingdom) · GB

Funding

Prostate Cancer UK PA12-12Wellcome TrustWellcome Trust 104046/Z/14/1Wellcome Trust 205291/Z/16/Z
6 · The paper itself

Abstract

Class B G-protein-coupled receptors (GPCRs) remain an underexploited target for drug development. The calcitonin receptor (CTR) family is particularly challenging, as its receptors are heteromers comprising two distinct components: the calcitonin receptor-like receptor (CLR) or calcitonin receptor (CTR) together with one of three accessory proteins known as receptor activity-modifying proteins (RAMPs). CLR/RAMP1 forms a CGRP receptor, CLR/RAMP2 forms an adrenomedullin-1 (AM

Indexed as

AnimalsAntineoplastic AgentsCell Line, TumorDrug DiscoveryFemaleHumansMiceMice, Inbred BALB CMolecular Docking SimulationReceptors, AdrenomedullinSmall Molecule LibrariesStructure-Activity RelationshipTriple Negative Breast NeoplasmsAntineoplastic AgentsReceptors, AdrenomedullinSmall Molecule Libraries

Identifiers

PMID33666424
PMCPMC8006142
OpenAlexW3133647296

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.