Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
ATAD2 in cancer: a pharmacologically challenging but tractable target
KTH, School of Biotechnology (BIO), Theoretical Chemistry and Biology. Albanova University Center.
Show others and affiliations
2018 (English)In: Expert opinion on therapeutic targets, ISSN 1472-8222, E-ISSN 1744-7631, Vol. 22, no 1, p. 85-96Article in journal (Refereed) Published
Abstract [en]

Introduction: ATAD2 protein is an emerging oncogene that has strongly been linked to the etiology of multiple advanced human cancers. Therapeutically, despite the fact that genetic suppression/knockdown studies have validated it as a compelling drug target for future therapeutic development, recent druggability assessment data suggest that direct targeting of ATAD2’s bromodomain (BRD) may be a very challenging task. ATAD2’s BRD has been predicted as a ‘difficult to drug’ or ‘least druggable’ target due to the concern that its binding pocket, and the areas around it, seem to be unfeasible for ligand binding. Areas covered: In this review, after shedding light on the multifaceted roles of ATAD2 in normal physiology as well as in cancer-etiology, we discuss technical challenges rendered by ATAD2’s BRD active site and the recent drug discovery efforts to find small molecule inhibitors against it. Expert opinion: The identification of a novel low-nanomolar semi-permeable chemical probe against ATAD2’s BRD by recent drug discovery campaign has demonstrated it to be a pharmacologically tractable target. Nevertheless, the development of high quality bioavailable inhibitors against ATAD2 is still a pending task. Moreover, ATAD2 may also potentially be utilized as a promising target for future development of RNAi-based therapy to treat cancers. 

Place, publisher, year, edition, pages
Taylor and Francis Ltd , 2018. Vol. 22, no 1, p. 85-96
Keywords [en]
AAA ATPase, ATAD2, BRD, cancer, druggable, ligandability, metastasis, siRNA, adenosine triphosphatase, antineoplastic agent, gsk 8814, molecular marker, protein ATAD2, small interfering RNA, unclassified drug, AAA protein, ATAD2 protein, human, DNA binding protein, apoptosis, breast cancer, cancer growth, carcinogenesis, cell cycle arrest, cell proliferation, cell survival, colorectal cancer, drug protein binding, drug structure, drug targeting, endometrium cancer, endometrium tumor, gene overexpression, human, ligand binding, liver cell carcinoma, lung cancer, malignant neoplasm, molecular dynamics, nonhuman, ovary cancer, physiological process, protein domain, protein expression, protein function, proto oncogene, Review, RNA interference, stomach cancer, transcription regulation, tumor cell, uterine cervix cancer, animal, antagonists and inhibitors, drug design, drug development, genetics, metabolism, molecularly targeted therapy, neoplasm, pathology, procedures, Animals, Antineoplastic Agents, ATPases Associated with Diverse Cellular Activities, DNA-Binding Proteins, Drug Discovery, Humans, Molecular Targeted Therapy, Neoplasms, RNA, Small Interfering
National Category
Clinical Medicine
Identifiers
URN: urn:nbn:se:kth:diva-223183DOI: 10.1080/14728222.2018.1406921ISI: 000428296500009Scopus ID: 2-s2.0-85038221486OAI: oai:DiVA.org:kth-223183DiVA, id: diva2:1186377
Note

Export Date: 13 February 2018; Review; CODEN: EOTTA; Correspondence Address: Zhang, J.; Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Science Park, China; email: zhang_jiancun@gibh.ac.cn. QC 20180228

Available from: 2018-02-28 Created: 2018-02-28 Last updated: 2018-04-11Bibliographically approved

Open Access in DiVA

No full text in DiVA

Other links

Publisher's full textScopus

Search in DiVA

By author/editor
Zhou, YangTu, Yaoquan
By organisation
Theoretical Chemistry and Biology
In the same journal
Expert opinion on therapeutic targets
Clinical Medicine

Search outside of DiVA

GoogleGoogle Scholar

doi
urn-nbn

Altmetric score

doi
urn-nbn
Total: 18 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf