Artikel ; Online: Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway.
International journal of molecular sciences
2021 Band 22, Heft 21
Abstract: Proteins targeted to the secretory pathway start their intracellular journey by being transported across biological membranes such as the endoplasmic reticulum (ER). A central component in this protein translocation process across the ER is the Sec61 ... ...
Abstract | Proteins targeted to the secretory pathway start their intracellular journey by being transported across biological membranes such as the endoplasmic reticulum (ER). A central component in this protein translocation process across the ER is the Sec61 translocon complex, which is only intracellularly expressed and does not have any enzymatic activity. In addition, Sec61 translocon complexes are difficult to purify and to reconstitute. Screening for small molecule inhibitors impairing its function has thus been notoriously difficult. However, such translocation inhibitors may not only be valuable tools for cell biology, but may also represent novel anticancer drugs, given that cancer cells heavily depend on efficient protein translocation into the ER to support their fast growth. In this review, different inhibitors of protein translocation will be discussed, and their specific mode of action will be compared. In addition, recently published screening strategies for small molecule inhibitors targeting the whole SRP-Sec61 targeting/translocation pathway will be summarized. Of note, slightly modified assays may be used in the future to screen for substances affecting SecYEG, the bacterial ortholog of the Sec61 complex, in order to identify novel antibiotic drugs. |
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Mesh-Begriff(e) | Animals ; Anti-Bacterial Agents/pharmacology ; Antineoplastic Agents/pharmacology ; Antiviral Agents/pharmacology ; Endoplasmic Reticulum/drug effects ; Endoplasmic Reticulum/metabolism ; High-Throughput Screening Assays ; Humans ; Protein Transport ; SEC Translocation Channels/antagonists & inhibitors ; SEC Translocation Channels/metabolism |
Chemische Substanzen | Anti-Bacterial Agents ; Antineoplastic Agents ; Antiviral Agents ; SEC Translocation Channels |
Sprache | Englisch |
Erscheinungsdatum | 2021-11-05 |
Erscheinungsland | Switzerland |
Dokumenttyp | Journal Article ; Review |
ZDB-ID | 2019364-6 |
ISSN | 1422-0067 ; 1422-0067 ; 1661-6596 |
ISSN (online) | 1422-0067 |
ISSN | 1422-0067 ; 1661-6596 |
DOI | 10.3390/ijms222112007 |
Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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