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Grant support

A Maiques-Diaz and T Somervaille are supported by Cancer Research UK Grant Number C5759/A12328. T Somervaille has ongoing research collaborations with Oryzon Genomics and consults for Imago Biosciences. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Analysis of institutional authors

Maiques-Diaz, AAuthor

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Review

LSD1: biologic roles and therapeutic targeting

Publicated to:Epigenomics. 8 (8): 1103-1116 - 2016-08-01 8(8), DOI: 10.2217/epi-2016-0009

Authors: Maiques-Diaz, A; Somervaille, TCP

Affiliations

Abstract

LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase activity and has since been shown to have multiple essential roles in mammalian biology. Given its enzymatic activity and its high-level expression in many human malignancies, a significant recent focus has been the development of pharmacologic inhibitors. Here we summarize structural and biochemical knowledge of this important epigenetic regulator, with a particular emphasis on the functional and preclinical studies in oncology that have provided justification for the evaluation of tranylcypromine derivative LSD1 inhibitors in early phase clinical trials.

Keywords

acute myeloid leukemiagsk2879552histone demethylaselsd1ory1001Acute myeloid leukemiaAnimalAnimalsAntagonists and inhibitorsAntineoplastic agentAntineoplastic agentsChemistryCorestDrug effectsDrug potencyEnhancer regionEnzyme activityEnzyme inhibitionEnzyme inhibitorEnzyme inhibitorsEnzyme structureEpigenesis, geneticEpigeneticsGene activationGene expressionGene expression regulationGene expression regulation, neoplasticGenetic epigenesisGeneticsGsk2879552Histone acetylationHistone demethylaseHistone demethylase lsd1Histone demethylasesHistone demethylationHumanHumansInhibitionKdm1a protein, humanLeukemia, myeloid, acuteLsd1Lsd1/kdm1a promotesLysine demethylase 1Lysine demethylase 1 inhibitorLysine demethylasesMechanism-based inactivatorMetabolismMolecular targeted therapyMolecularly targeted therapyNerve cell differentiationNeural stem cellNucleosomeOry1001Priority journalProceduresPromoter regionProtein protein interactionReviewSmall-cell lung cancerSnag domainStructural basisTranscription initiationTranscriptional repressionTranylcypromine derivativeUnclassified drug

Quality index

Bibliometric impact. Analysis of the contribution and dissemination channel

The work has been published in the journal Epigenomics due to its progression and the good impact it has achieved in recent years, according to the agency WoS (JCR), it has become a reference in its field. In the year of publication of the work, 2016, it was in position 31/167, thus managing to position itself as a Q1 (Primer Cuartil), in the category Genetics & Heredity.

From a relative perspective, and based on the normalized impact indicator calculated from World Citations provided by WoS (ESI, Clarivate), it yields a value for the citation normalization relative to the expected citation rate of: 3.73. This indicates that, compared to works in the same discipline and in the same year of publication, it ranks as a work cited above average. (source consulted: ESI Nov 14, 2024)

This information is reinforced by other indicators of the same type, which, although dynamic over time and dependent on the set of average global citations at the time of their calculation, consistently position the work at some point among the top 50% most cited in its field:

  • Weighted Average of Normalized Impact by the Scopus agency: 5.03 (source consulted: FECYT Feb 2024)
  • Field Citation Ratio (FCR) from Dimensions: 17.16 (source consulted: Dimensions Jun 2025)

Specifically, and according to different indexing agencies, this work has accumulated citations as of 2025-06-05, the following number of citations:

  • WoS: 124
  • Scopus: 175
  • Google Scholar: 194
  • OpenCitations: 173

Impact and social visibility

From the perspective of influence or social adoption, and based on metrics associated with mentions and interactions provided by agencies specializing in calculating the so-called "Alternative or Social Metrics," we can highlight as of 2025-06-05:

  • The use, from an academic perspective evidenced by the Altmetric agency indicator referring to aggregations made by the personal bibliographic manager Mendeley, gives us a total of: 193.
  • The use of this contribution in bookmarks, code forks, additions to favorite lists for recurrent reading, as well as general views, indicates that someone is using the publication as a basis for their current work. This may be a notable indicator of future more formal and academic citations. This claim is supported by the result of the "Capture" indicator, which yields a total of: 193 (PlumX).

With a more dissemination-oriented intent and targeting more general audiences, we can observe other more global scores such as:

  • The Total Score from Altmetric: 27.

It is essential to present evidence supporting full alignment with institutional principles and guidelines on Open Science and the Conservation and Dissemination of Intellectual Heritage. A clear example of this is:

  • The work has been submitted to a journal whose editorial policy allows open Open Access publication.

Leadership analysis of institutional authors

This work has been carried out with international collaboration, specifically with researchers from: United Kingdom.

There is a significant leadership presence as some of the institution’s authors appear as the first or last signer, detailed as follows: First Author (Maiques Diaz, Alba) .