Evidence map›Paper›PMID 34788896›Full record

ArticleChemistry (Weinheim an der Bergstrasse, Germany)2022

Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders.

Paola Marzullo, Zlata Boiarska, Helena Pérez-Peña, Anne-Catherine Abel, Beatriz Álvarez-Bernad, Daniel Lucena-Agell, Francesca Vasile, Maurizio Sironi, Karl-Heinz Altmann, Andrea E Prota and 3 more

Abstract read
In one paragraph

Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
  4. Antibody-drug conjugates: Recent advances in payloads.Acta pharmaceutica Sinica. B · 2023
    Review
  5. Synthesis and Biological Evaluation of C(13)/C(13')-Bis(desmethyl)disorazole Z.Angewandte Chemie (International ed. in English) · 2023
    Article
  6. Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022
    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.

Paola MarzulloDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Zlata BoiarskaDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Helena Pérez-PeñaDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Anne-Catherine AbelLaboratory of Biomolecular Research, Paul Scherrer Institute, Forschungsstrasse 111, 5232, Villigen PSI, Switzerland.
Beatriz Álvarez-BernadCentro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas, Ramiro de Maeztu 9, 28040, Madrid, Spain.
Daniel Lucena-AgellCentro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas, Ramiro de Maeztu 9, 28040, Madrid, Spain.
Francesca VasileDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Maurizio SironiDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Karl-Heinz AltmannDepartment of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH, Zürich, Vladimir-Prelog Weg 4, HCI H405, 8093, Zürich, Switzerland.
Andrea E ProtaLaboratory of Biomolecular Research, Paul Scherrer Institute, Forschungsstrasse 111, 5232, Villigen PSI, Switzerland.
J Fernando DíazCentro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas, Ramiro de Maeztu 9, 28040, Madrid, Spain.
Stefano PieracciniDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.
Daniele PassarellaDepartment of Chemistry, Università degli Studi di Milano, Via Golgi 19, 20133, Milan, Italy.ORCID http://orcid.org/0000-0001-6180-9581

Funding

Horizon 2020 Framework Programme 860070 TUBINTRAINMinisterio de Ciencia e Innovación PID2019-104545RB-I00
6 · The paper itself

Abstract

Maytansinol is a valuable precursor for the preparation of maytansine derivatives (known as maytansinoids). Inspired by the intriguing structure of the macrocycle and the success in targeted cancer therapy of the derivatives, we explored the maytansinol acylation reaction. As a result, we were able to obtain a series of derivatives with novel modifications of the maytansine scaffold. We characterized these molecules by docking studies, by a comprehensive biochemical evaluation, and by determination of their crystal structures in complex with tubulin. The results shed further light on the intriguing chemical behavior of maytansinoids and confirm the relevance of this peculiar scaffold in the scenario of tubulin binders.

Indexed as

MaytansineNeoplasmsHumansMicrotubulesTubulinTubulin ModulatorsMaytansinemaytansinolTubulinTubulin Modulatorsmaytansine binding sitemaytansinolmicrotubulestubulintubulin binders

Identifiers

PMID34788896
PMCPMC9299702

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.