Literature DB >> 12699760

5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).

Jason Witherington1, Vincent Bordas, David Haigh, Deirdre M B Hickey, Robert J Ife, Anthony D Rawlings, Brian P Slingsby, David G Smith, Robert W Ward.   

Abstract

Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography.

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Year:  2003        PMID： 12699760     DOI： 10.1016/s0960-894x(03)00135-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  8 in total

1.  Comprehensive characterization of the Published Kinase Inhibitor Set.

Authors:  Jonathan M Elkins; Vita Fedele; Marta Szklarz; Kamal R Abdul Azeez; Eidarus Salah; Jowita Mikolajczyk; Sergei Romanov; Nikolai Sepetov; Xi-Ping Huang; Bryan L Roth; Ayman Al Haj Zen; Denis Fourches; Eugene Muratov; Alex Tropsha; Joel Morris; Beverly A Teicher; Mark Kunkel; Eric Polley; Karen E Lackey; Francis L Atkinson; John P Overington; Paul Bamborough; Susanne Müller; Daniel J Price; Timothy M Willson; David H Drewry; Stefan Knapp; William J Zuercher
Journal:  Nat Biotechnol       Date:  2015-10-26       Impact factor: 54.908

2.  Increased expression of the WNT antagonist sFRP-1 in glaucoma elevates intraocular pressure.

Authors:  Wan-Heng Wang; Loretta G McNatt; Iok-Hou Pang; J Cameron Millar; Peggy E Hellberg; Mark H Hellberg; H Thomas Steely; Jeffrey S Rubin; John H Fingert; Val C Sheffield; Edwin M Stone; Abbot F Clark
Journal:  J Clin Invest       Date:  2008-03       Impact factor: 14.808

3.  Glycogen synthase kinase-3 inhibition by 3-anilino-4-phenylmaleimides: insights from 3D-QSAR and docking.

Authors:  Sivaprakasam Prasanna; Pankaj R Daga; Aihua Xie; Robert J Doerksen
Journal:  J Comput Aided Mol Des       Date:  2008-10-07       Impact factor: 3.686

4.  DNA damage stress and inhibition of Jak2-V617F cause its degradation and synergistically induce apoptosis through activation of GSK3β.

Authors:  Toshikage Nagao; Gaku Oshikawa; Nan Wu; Tetsuya Kurosu; Osamu Miura
Journal:  PLoS One       Date:  2011-11-08       Impact factor: 3.240

5.  Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models.

Authors:  Thomas Kramer; Boris Schmidt; Fabio Lo Monte
Journal:  Int J Alzheimers Dis       Date:  2012-07-22

6.  Inhibition of the PI3K/Akt/GSK3 pathway downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD downregulates DNA damage-induced Chk1 activation as well as G2/M arrest and prominently enhances induction of apoptosis.

Authors:  Tetsuya Kurosu; Toshikage Nagao; Nan Wu; Gaku Oshikawa; Osamu Miura
Journal:  PLoS One       Date:  2013-11-18       Impact factor: 3.240

7.  Down regulation of Chk1 by p53 plays a role in synergistic induction of apoptosis by chemotherapeutics and inhibitors for Jak2 or BCR/ABL in hematopoietic cells.

Authors:  Yoshihiro Umezawa; Tetsuya Kurosu; Hiroki Akiyama; Nang Wu; Ayako Nogami; Toshikage Nagao; Osamu Miura
Journal:  Oncotarget       Date:  2016-07-12

8.  Computer-aided molecular design of pyrazolotriazines targeting glycogen synthase kinase 3.

Authors:  M Lourdes Sciú; Victor Sebastián-Pérez; Loreto Martinez-Gonzalez; Rocio Benitez; Daniel I Perez; Concepción Pérez; Nuria E Campillo; Ana Martinez; E Laura Moyano
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051
  8 in total

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