Evidence map›Paper›PMID 36557929›Full record

ArticleMolecules (Basel, Switzerland)2022

Synthesis and Preclinical Evaluation of Small-Molecule Prostate-Specific Membrane Antigen-Targeted Abiraterone Conjugate.

Aleksei E Machulkin, Ekaterina A Nimenko, Nikolay U Zyk, Anastasiia A Uspenskaia, Galina B Smirnova, Irina I Khan, Vadim S Pokrovsky, Alexander N Vaneev, Roman V Timoshenko, Vugara V Mamed-Nabizade and 7 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.5field-weighted citation impact, top 16% 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

4 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. 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

17 authors at 4 institutions in 1 country.

Aleksei E MachulkinChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.ORCID 0000-0001-7975-0346
Ekaterina A NimenkoChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Nikolay U ZykChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Anastasiia A UspenskaiaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Galina B SmirnovaN.N. Blokhin Russian Cancer Research Center, 24 Kashirskoye sh., 115478 Moscow, Russia.
Irina I KhanN.N. Blokhin Russian Cancer Research Center, 24 Kashirskoye sh., 115478 Moscow, Russia.
Vadim S PokrovskyN.N. Blokhin Russian Cancer Research Center, 24 Kashirskoye sh., 115478 Moscow, Russia.
Alexander N VaneevChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.ORCID 0000-0001-8201-8498
Roman V TimoshenkoLaboratory of Biophysics, National University of Science and Technology MISiS, 4 Leninskiy pr, 119049 Moscow, Russia.
Vugara V Mamed-NabizadeLaboratory of Biophysics, National University of Science and Technology MISiS, 4 Leninskiy pr, 119049 Moscow, Russia.
Maria V ZavertkinaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.ORCID 0000-0002-8421-7180
Alexander ErofeevChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Petr GorelkinLaboratory of Biophysics, National University of Science and Technology MISiS, 4 Leninskiy pr, 119049 Moscow, Russia.ORCID 0000-0002-4860-9013
Alexander G MajougaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Nikolay V ZykChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.
Elena S KhazanovaLLC Izvarino-Pharma, v. Vnukovskoe, Vnukovskoe sh., 5th km., Building 1, 108817 Moscow, Russia.
Elena K BeloglazkinaChemistry Department, Lomonosov Moscow State University, Leninskie Gory, Building 1/3, GSP-1, 119991 Moscow, Russia.ORCID 0000-0001-6796-8241
Lomonosov Moscow State University · RUNational University of Science and Technology · RUPeoples' Friendship University of Russia · RURussian Cancer Research Center NN Blokhin · RU

Funding

Ministry of Education and Science of the Russian Federation 03.G25.31.0219Russian Science Foundation 22-15-00098Russian Science Foundation 22-19-00824
6 · The paper itself

Abstract

Prostate cancer is the second most common type of cancer among men. The main method of its treatment is androgen deprivation therapy, which has a wide range of side effects. One of the solutions to this challenge is the targeted delivery of drugs to prostate cancer cells. In this study, we performed the synthesis of a novel small-molecule PSMA-targeted conjugate based on abiraterone. Cytotoxicity, the induction of intracellular reactive oxygen species, and P450-cytochrome species inhibition were investigated for this conjugate PSMA-abiraterone. The conjugate demonstrated a preferential effect on prostate tumor cells, remaining inactive at up to 100 µM in human fibroblast cells. In addition, it revealed preferential efficacy, specifically on PSMA-expressing lines with a 65% tumor growth inhibition level on 22Rv1 (PSMA+) xenografts after 14-fold oral administration of

Indexed as

Prostatic NeoplasmsAndrogen AntagonistsAndrostenesAntigens, SurfaceHumansMaleProstateabirateroneAndrogen AntagonistsAndrostenesAntigens, Surfaceabirateronedrug deliveryprostate cancerprostate-specific membrane antigen

Identifiers

PMID36557929
PMCPMC9783881
OpenAlexW4311154290

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.