7z4v: Difference between revisions

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== Function ==

[[https://www.uniprot.org/uniprot/STK25_HUMAN STK25_HUMAN]] Oxidant stress-activated serine/threonine kinase that may play a role in the response to environmental stress. Targets to the Golgi apparatus where it appears to regulate protein transport events, cell adhesion, and polarity complexes important for cell migration.<ref>PMID:15037601</ref>

== Publication Abstract from PubMed ==

We describe the synthesis of a series of 3-t-butyl 5-aminopyrazole p-substituted arylamides as inhibitors of serine-threonine25 (STK25), an enzyme implicated in the progression of non-alcoholic fatty liver disease (NAFLD). Appending a p-N-pyrrolidinosulphonamide group to the arylamide group led to a 'first-in kind' inhibitor with IC50 = 228 nM. A co-crystal structure with STK 25 revealed productive interactions which were also reproduced using molecular docking. A new series of triazolo dihydro oxazine carboxamides of 3-t-butyl 5-aminopyrazole was not active against STK25.

Targeting non-alcoholic fatty liver disease: Design, X-ray co-crystal structure and synthesis of 'first-in-kind' inhibitors of serine/threonine kinase25.,Kiyeleko S, Hocine S, Mautino G, Kuenemann M, Nawrotek A, Miallau L, Vuillard LM, Mirguet O, Kotschy A, Hanessian S Bioorg Med Chem Lett. 2022 Aug 24;75:128950. doi: 10.1016/j.bmcl.2022.128950. PMID:36030002<ref>PMID:36030002</ref>

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>

</div>

== References ==

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 == Function ==
 [[https://www.uniprot.org/uniprot/STK25_HUMAN STK25_HUMAN]] Oxidant stress-activated serine/threonine kinase that may play a role in the response to environmental stress. Targets to the Golgi apparatus where it appears to regulate protein transport events, cell adhesion, and polarity complexes important for cell migration.<ref>PMID:15037601</ref>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+We describe the synthesis of a series of 3-t-butyl 5-aminopyrazole p-substituted arylamides as inhibitors of serine-threonine25 (STK25), an enzyme implicated in the progression of non-alcoholic fatty liver disease (NAFLD). Appending a p-N-pyrrolidinosulphonamide group to the arylamide group led to a 'first-in kind' inhibitor with IC50 = 228 nM. A co-crystal structure with STK 25 revealed productive interactions which were also reproduced using molecular docking. A new series of triazolo dihydro oxazine carboxamides of 3-t-butyl 5-aminopyrazole was not active against STK25.
+Targeting non-alcoholic fatty liver disease: Design, X-ray co-crystal structure and synthesis of 'first-in-kind' inhibitors of serine/threonine kinase25.,Kiyeleko S, Hocine S, Mautino G, Kuenemann M, Nawrotek A, Miallau L, Vuillard LM, Mirguet O, Kotschy A, Hanessian S Bioorg Med Chem Lett. 2022 Aug 24;75:128950. doi: 10.1016/j.bmcl.2022.128950. PMID:36030002<ref>PMID:36030002</ref>
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
+<div class="pdbe-citations 7z4v" style="background-color:#fffaf0;"></div>
 == References ==
 <references/>