HOME

TheInfoList



OR:

Salubrinal is a drug which acts as a specific inhibitor of eIF2α
phosphatase In biochemistry, a phosphatase is an enzyme that uses water to cleave a phosphoric acid Ester, monoester into a phosphate ion and an Alcohol (chemistry), alcohol. Because a phosphatase enzyme catalysis, catalyzes the hydrolysis of its Substrate ...
enzymes and is primarily used experimentally, to study stress responses in
eukaryotic Eukaryotes () are organisms whose cells have a nucleus. All animals, plants, fungi, and many unicellular organisms, are Eukaryotes. They belong to the group of organisms Eukaryota or Eukarya, which is one of the three domains of life. Bacte ...
cell Cell most often refers to: * Cell (biology), the functional basic unit of life Cell may also refer to: Locations * Monastic cell, a small room, hut, or cave in which a religious recluse lives, alternatively the small precursor of a monastery ...
s associated with the action of eIF2. Salubrinal indirectly inhibits eIF2 as a result of reduced
dephosphorylation In biochemistry, dephosphorylation is the removal of a phosphate (PO43−) group from an organic compound by hydrolysis. It is a reversible post-translational modification. Dephosphorylation and its counterpart, phosphorylation, activate and deac ...
of its α- subunit, resulting in activation of stress response pathways usually triggered by events such as
oxidative stress Oxidative stress reflects an imbalance between the systemic manifestation of reactive oxygen species and a biological system's ability to readily Detoxification, detoxify the reactive intermediates or to repair the resulting damage. Disturbances ...
or buildup of unfolded
protein Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, respo ...
in the
endoplasmic reticulum The endoplasmic reticulum (ER) is, in essence, the transportation system of the eukaryotic cell, and has many other important functions such as protein folding. It is a type of organelle made up of two subunits – rough endoplasmic reticulum ( ...
. Salubrinal has putative
therapeutic A therapy or medical treatment (often abbreviated tx, Tx, or Tx) is the attempted remediation of a health problem, usually following a medical diagnosis. As a rule, each therapy has indications and contraindications. There are many different ...
value due to its function, but is as yet only used experimentally. Salubrinal is being studied at Indiana University for its potential to fight osteoporosis and accelerate bone healing.


References

{{Reflist, refs= {{cite journal , vauthors = Kessel D , title = Protection of Bcl-2 by salubrinal , journal = Biochemical and Biophysical Research Communications , volume = 346 , issue = 4 , pages = 1320–3 , date = August 2006 , pmid = 16806073 , pmc = 2978664 , doi = 10.1016/j.bbrc.2006.06.056 , publisher = Elsevier Inc {{dead link, date=March 2019, bot=medic{{cbignore, bot=medic {{cite journal , vauthors = Lewerenz J, Maher P , title = Basal levels of eIF2alpha phosphorylation determine cellular antioxidant status by regulating ATF4 and xCT expression , journal = The Journal of Biological Chemistry , volume = 284 , issue = 2 , pages = 1106–15 , date = January 2009 , pmid = 19017641 , pmc = 2613630 , doi = 10.1074/jbc.M807325200 , publisher = The American Society for Biochemistry and Molecular Biology, Inc , doi-access = free {{cite journal , vauthors = Boyce M, Bryant KF, Jousse C, Long K, Harding HP, Scheuner D, Kaufman RJ, Ma D, Coen DM, Ron D, Yuan J , display-authors = 6 , title = A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress , journal = Science , volume = 307 , issue = 5711 , pages = 935–9 , date = February 2005 , pmid = 15705855 , doi = 10.1126/science.1101902 , bibcode = 2005Sci...307..935B , s2cid = 86257684 , url = http://www.sciencemag.org/cgi/content/abstract/307/5711/935 {{cite web, title=Entrez Gene: EIF2S1 eukaryotic translation initiation factor 2, subunit 1 alpha, 35kDa, url=https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1965, access-date=2010-10-05, publisher=
National Center for Biotechnology Information The National Center for Biotechnology Information (NCBI) is part of the United States National Library of Medicine (NLM), a branch of the National Institutes of Health (NIH). It is approved and funded by the government of the United States. The ...
, U.S. National Library of Medicine
{{cite journal , vauthors = Wek RC, Jiang HY, Anthony TG , title = Coping with stress: eIF2 kinases and translational control , journal = Biochemical Society Transactions , volume = 34 , issue = Pt 1 , pages = 7–11 , date = February 2006 , pmid = 16246168 , doi = 10.1042/BST20060007 , publisher = Biochemical Society {{cite web , title=New compound may accelerate bone healing, prevent osteoporosis, url = http://www.cloningresources.com/research/New_compound_may_accelerate_bone_healing_prevent_osteoporosis.asp , archive-url = https://web.archive.org/web/20110929162126/http://www.cloningresources.com/research/New_compound_may_accelerate_bone_healing_prevent_osteoporosis.asp , archive-date = 29 September 2011 , access-date=2011-08-29 , date=August 2011 Drugs not assigned an ATC code Thioureas Quinolines Organochlorides