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The following term was not found in PubMed: Renggono
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Druggable Transient Pockets in Protein Kinases.
Umezawa K, Kii I. Umezawa K, et al. Molecules. 2021 Jan 27;26(3):651. doi: 10.3390/molecules26030651. Molecules. 2021. PMID: 33513739 Free PMC article. Review.
Kii and colleagues identified an inhibitor targeting a transient pocket in the kinase DYRK1A during its folding process and termed it FINDY. FINDY exhibits a unique inhibitory profile; that is, FINDY does not inhibit the fully folded form of DYRK1A, indicatin …
Kii and colleagues identified an inhibitor targeting a transient pocket in the kinase DYRK1A during its folding process and termed it FIN …
Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A.
Miyazaki Y, Kikuchi M, Umezawa K, Descamps A, Nakamura D, Furuie G, Sumida T, Saito K, Kimura N, Niwa T, Sumida Y, Umehara T, Hosoya T, Kii I. Miyazaki Y, et al. Eur J Med Chem. 2022 Jan 5;227:113948. doi: 10.1016/j.ejmech.2021.113948. Epub 2021 Oct 28. Eur J Med Chem. 2022. PMID: 34742017
However, the structural features of FINDY (1) responsible for this intermediate-selective inhibition remain elusive. ...In addition, a potent derivative 3 was identified, which inhibited the folding intermediate more strongly than FINDY (1); it was designated as dp- …
However, the structural features of FINDY (1) responsible for this intermediate-selective inhibition remain elusive. ...In addition, …
Expression and purification of DYRK1A kinase domain in complex with its folding intermediate-selective inhibitor FINDY.
Kimura N, Saito K, Niwa T, Yamakawa M, Igaue S, Ohkanda J, Hosoya T, Kii I. Kimura N, et al. Protein Expr Purif. 2022 Aug;195-196:106089. doi: 10.1016/j.pep.2022.106089. Epub 2022 Mar 18. Protein Expr Purif. 2022. PMID: 35307559
The amount of FINDY in the elution fraction was measured by UV absorbance specific for FINDY. The eluate contained FINDY with the ratio of FINDY to DYRK1A protein being 0.15 in quadruplicate experiments. ...
The amount of FINDY in the elution fraction was measured by UV absorbance specific for FINDY. The eluate contained FINDY …
Selective inhibition of the kinase DYRK1A by targeting its folding process.
Kii I, Sumida Y, Goto T, Sonamoto R, Okuno Y, Yoshida S, Kato-Sumida T, Koike Y, Abe M, Nonaka Y, Ikura T, Ito N, Shibuya H, Hosoya T, Hagiwara M. Kii I, et al. Nat Commun. 2016 Apr 22;7:11391. doi: 10.1038/ncomms11391. Nat Commun. 2016. PMID: 27102360 Free PMC article.
FINDY also suppresses Ser97 autophosphorylation of recombinant DYRK1A, suggesting direct inhibition, and shows high selectivity for DYRK1A over other DYRK family members. In addition, FINDY rescues DYRK1A-induced developmental malformations in Xenopus laevis embryos …
FINDY also suppresses Ser97 autophosphorylation of recombinant DYRK1A, suggesting direct inhibition, and shows high selectivity for D …