Literature DB >> 11012021

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.

L D Arnold1, D J Calderwood, R W Dixon, D N Johnston, J S Kamens, R Munschauer, P Rafferty, S E Ratnofsky.   

Abstract

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of Ick in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells.

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Year:  2000        PMID: 11012021     DOI: 10.1016/s0960-894x(00)00441-8

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


  16 in total

1.  In vivo modulation of avidity in highly sensitive CD8(+) effector T cells following viral infection.

Authors:  Beth C Holbrook; Rama D Yammani; Lance K Blevins; Martha A Alexander-Miller
Journal:  Viral Immunol       Date:  2013-08-24       Impact factor: 2.257

2.  In Vitro Evolution Reveals a Single Mutation as Sole Source of Src-Family Kinase C-Helix-out Inhibitor Resistance.

Authors:  Ravi K Patel; Yash K Patel; Thomas E Smithgall
Journal:  ACS Chem Biol       Date:  2020-07-15       Impact factor: 5.100

3.  High-throughput identification of small molecules that affect human embryonic vascular development.

Authors:  Helena Vazão; Susana Rosa; Tânia Barata; Ricardo Costa; Patrícia R Pitrez; Inês Honório; Margreet R de Vries; Dimitri Papatsenko; Rui Benedito; Daniel Saris; Ali Khademhosseini; Paul H A Quax; Carlos F Pereira; Nadia Mercader; Hugo Fernandes; Lino Ferreira
Journal:  Proc Natl Acad Sci U S A       Date:  2017-03-27       Impact factor: 11.205

4.  Development of small molecules targeting the pseudokinase Her3.

Authors:  Sang Min Lim; Ting Xie; Kenneth D Westover; Scott B Ficarro; Hyun Seop Tae; Deepak Gurbani; Taebo Sim; Jarrod A Marto; Pasi A Jänne; Craig M Crews; Nathanael S Gray
Journal:  Bioorg Med Chem Lett       Date:  2015-05-11       Impact factor: 2.823

5.  The associated pyrazolopyrimidines PP1 and PP2 inhibit protein tyrosine kinase 6 activity and suppress breast cancer cell proliferation.

Authors:  Hyun Jae Shim; Han Ie Kim; Seung-Taek Lee
Journal:  Oncol Lett       Date:  2017-01-02       Impact factor: 2.967

6.  Structures of human Bruton's tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases.

Authors:  Douglas J Marcotte; Yu-Ting Liu; Robert M Arduini; Catherine A Hession; Konrad Miatkowski; Craig P Wildes; Patrick F Cullen; Victor Hong; Brian T Hopkins; Elisabeth Mertsching; Tracy J Jenkins; Michael J Romanowski; Darren P Baker; Laura F Silvian
Journal:  Protein Sci       Date:  2010-03       Impact factor: 6.725

7.  CD8+ T cell immunodominance shifts during the early stages of acute LCMV infection independently from functional avidity maturation.

Authors:  Hans-Peter Raué; Mark K Slifka
Journal:  Virology       Date:  2009-06-18       Impact factor: 3.616

8.  Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.

Authors:  Akira Kawamura; Sagit Hindi; Doina M Mihai; Laurence James; Olga Aminova
Journal:  Bioorg Med Chem       Date:  2008-09-03       Impact factor: 3.641

9.  Discovery of consensus gene signature and intermodular connectivity defining self-renewal of human embryonic stem cells.

Authors:  Jeffrey J Kim; Omar Khalid; AmirHosien Namazi; Thanh G Tu; Omid Elie; Connie Lee; Yong Kim
Journal:  Stem Cells       Date:  2014-06       Impact factor: 6.277

10.  New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights.

Authors:  Ahmed Elkamhawy; Eslam M H Ali; Kyeong Lee
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

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