Literature DB >> 19299564

Targeting protein serine/threonine phosphatases for drug development.

Jamie L McConnell1, Brian E Wadzinski.   

Abstract

With the recent clinical success of drugs targeting protein kinase activity, drug discovery efforts are focusing on the role of reversible protein phosphorylation in disease states. The activity of protein phosphatases, enzymes that oppose protein kinases, can also be manipulated to alter cellular signaling for therapeutic benefits. In this review, we present protein serine/threonine phosphatases as viable therapeutic targets, discussing past successes, current challenges, and future strategies for modulating phosphatase activity.

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Year:  2009        PMID： 19299564      PMCID： PMC2684880          DOI： 10.1124/mol.108.053140

Source DB:  PubMed          Journal:  Mol Pharmacol        ISSN： 0026-895X            Impact factor:   4.436


  154 in total

1.  The design, synthesis, and biological evaluation of analogues of the serine-threonine protein phosphatase 1 and 2A selective inhibitor microcystin LA: rational modifications imparting PP1 selectivity.

Authors:  J B Aggen; J M Humphrey; C M Gauss; H B Huang; A C Nairn; A R Chamberlin
Journal:  Bioorg Med Chem       Date:  1999-03       Impact factor: 3.641

2.  Importance of the beta12-beta13 loop in protein phosphatase-1 catalytic subunit for inhibition by toxins and mammalian protein inhibitors.

Authors:  J H Connor; T Kleeman; S Barik; R E Honkanen; S Shenolikar
Journal:  J Biol Chem       Date:  1999-08-06       Impact factor: 5.157

3.  Methylated C-terminal leucine residue of PP2A catalytic subunit is important for binding of regulatory Balpha subunit.

Authors:  J C Bryant; R S Westphal; B E Wadzinski
Journal:  Biochem J       Date:  1999-04-15       Impact factor: 3.857

4.  Positive and negative regulation of IkappaB kinase activity through IKKbeta subunit phosphorylation.

Authors:  M Delhase; M Hayakawa; Y Chen; M Karin
Journal:  Science       Date:  1999-04-09       Impact factor: 47.728

5.  Protein phosphatase 1 modulation of neostriatal AMPA channels: regulation by DARPP-32 and spinophilin.

Authors:  Z Yan; L Hsieh-Wilson; J Feng; K Tomizawa; P B Allen; A A Fienberg; A C Nairn; P Greengard
Journal:  Nat Neurosci       Date:  1999-01       Impact factor: 24.884

6.  Doxorubicin-resistant LoVo adenocarcinoma cells display resistance to apoptosis induction by some but not all inhibitors of ser/thr phosphatases 1 and 2A.

Authors:  S Sieder; E Richter; K Becker; R Heins; H J Steinfelder
Journal:  Toxicology       Date:  1999-06-15       Impact factor: 4.221

7.  Long chain ceramides activate protein phosphatase-1 and protein phosphatase-2A. Activation is stereospecific and regulated by phosphatidic acid.

Authors:  C E Chalfant; K Kishikawa; M C Mumby; C Kamibayashi; A Bielawska; Y A Hannun
Journal:  J Biol Chem       Date:  1999-07-16       Impact factor: 5.157

8.  Molecular basis for TPR domain-mediated regulation of protein phosphatase 5.

Authors:  Jing Yang; S Mark Roe; Matthew J Cliff; Mark A Williams; John E Ladbury; Patricia T W Cohen; David Barford
Journal:  EMBO J       Date:  2004-12-02       Impact factor: 11.598

9.  Ser/Thr protein phosphatase 5 inactivates hypoxia-induced activation of an apoptosis signal-regulating kinase 1/MKK-4/JNK signaling cascade.

Authors:  Guofei Zhou; Teresa Golden; Ileana V Aragon; Richard E Honkanen
Journal:  J Biol Chem       Date:  2004-08-24       Impact factor: 5.157

10.  Structural basis for the catalytic activity of human serine/threonine protein phosphatase-5.

Authors:  Mark R Swingle; Richard E Honkanen; Ewa M Ciszak
Journal:  J Biol Chem       Date:  2004-05-23       Impact factor: 5.157
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  61 in total

Review 1.  Novel Ser/Thr protein phosphatases in cell death regulation.

Authors:  Haipeng Sun; Yibin Wang
Journal:  Physiology (Bethesda)       Date:  2012-02

2.  Adaptation of HepG2 cells to a steady-state reduction in the content of protein phosphatase 6 (PP6) catalytic subunit.

Authors:  Joan M Boylan; Arthur R Salomon; Umadevi Tantravahi; Philip A Gruppuso
Journal:  Exp Cell Res       Date:  2015-05-18       Impact factor: 3.905

3.  Label-free electrochemical impedance detection of kinase and phosphatase activities using carbon nanofiber nanoelectrode arrays.

Authors:  Yifen Li; Lateef Syed; Jianwei Liu; Duy H Hua; Jun Li
Journal:  Anal Chim Acta       Date:  2012-07-24       Impact factor: 6.558

4.  Site-specific NMR mapping and time-resolved monitoring of serine and threonine phosphorylation in reconstituted kinase reactions and mammalian cell extracts.

Authors:  Francois-Xavier Theillet; Honor May Rose; Stamatios Liokatis; Andres Binolfi; Rossukon Thongwichian; Marchel Stuiver; Philipp Selenko
Journal:  Nat Protoc       Date:  2013-06-27       Impact factor: 13.491

Review 5.  Bacterial serine/threonine protein kinases in host-pathogen interactions.

Authors:  Marc J Canova; Virginie Molle
Journal:  J Biol Chem       Date:  2014-02-19       Impact factor: 5.157

6.  Platelets reduce anoikis and promote metastasis by activating YAP1 signaling.

Authors:  Monika Haemmerle; Morgan L Taylor; Tony Gutschner; Sunila Pradeep; Min Soon Cho; Jianting Sheng; Yasmin M Lyons; Archana S Nagaraja; Robert L Dood; Yunfei Wen; Lingegowda S Mangala; Jean M Hansen; Rajesha Rupaimoole; Kshipra M Gharpure; Cristian Rodriguez-Aguayo; Sun Young Yim; Ju-Seog Lee; Cristina Ivan; Wei Hu; Gabriel Lopez-Berestein; Stephen T Wong; Beth Y Karlan; Douglas A Levine; Jinsong Liu; Vahid Afshar-Kharghan; Anil K Sood
Journal:  Nat Commun       Date:  2017-08-21       Impact factor: 14.919

Review 7.  The Importance of Tyrosine Phosphorylation Control of Cellular Signaling Pathways in Respiratory Disease: pY and pY Not.

Authors:  Yael Aschner; Gregory P Downey
Journal:  Am J Respir Cell Mol Biol       Date:  2018-11       Impact factor: 6.914

Review 8.  The extended PP1 toolkit: designed to create specificity.

Authors:  Mathieu Bollen; Wolfgang Peti; Michael J Ragusa; Monique Beullens
Journal:  Trends Biochem Sci       Date:  2010-05-01       Impact factor: 13.807

9.  The molecular chaperone Hsp70 activates protein phosphatase 5 (PP5) by binding the tetratricopeptide repeat (TPR) domain.

Authors:  Jamie N Connarn; Victoria A Assimon; Rebecca A Reed; Eric Tse; Daniel R Southworth; Erik R P Zuiderweg; Jason E Gestwicki; Duxin Sun
Journal:  J Biol Chem       Date:  2013-12-10       Impact factor: 5.157

10.  InAKTivation of insulin/IGF-1 signaling by dephosphorylation.

Authors:  Sri Devi Narasimhan; Arnab Mukhopadhyay; Heidi A Tissenbaum
Journal:  Cell Cycle       Date:  2009-12       Impact factor: 4.534
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