Literature DB >> 16216497

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Andrew Burchat1, David W Borhani, David J Calderwood, Gavin C Hirst, Biqin Li, Robert F Stachlewitz.   

Abstract

We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.

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Year:  2005        PMID: 16216497     DOI: 10.1016/j.bmcl.2005.09.039

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


  19 in total

Review 1.  Targeting non-malignant disorders with tyrosine kinase inhibitors.

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Review 2.  Selected signalling proteins recruited to the T-cell receptor-CD3 complex.

Authors:  Jatuporn Ngoenkam; Wolfgang W Schamel; Sutatip Pongcharoen
Journal:  Immunology       Date:  2017-09-05       Impact factor: 7.397

3.  Ectopic Lck expression in CLL demarcates intratumoral subpopulations with aberrant B-cell receptor signaling.

Authors:  Efthymia Theofani; Spyridon Alexis; Paul Costeas; Christos Andriopoulos; Georgia Feleskoura; Panagiotis Zikos; Anthi Aktypi; Alexandros Spyridonidis; Konstantina Nika
Journal:  Blood Adv       Date:  2018-04-24

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.  Flexibility and charge asymmetry in the activation loop of Src tyrosine kinases.

Authors:  Nilesh K Banavali; Benoît Roux
Journal:  Proteins       Date:  2009-02-01

6.  Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation.

Authors:  Andrew E Schade; Gary L Schieven; Robert Townsend; Anna M Jankowska; Vojkan Susulic; Rosemary Zhang; Hadrian Szpurka; Jaroslaw P Maciejewski
Journal:  Blood       Date:  2007-10-25       Impact factor: 22.113

7.  Identification of lymphocyte cell-specific protein-tyrosine kinase (LCK) as a driver for invasion and migration of oral cancer by tumor heterogeneity exploitation.

Authors:  Julia Rosemann; Lisa Müller; Jonas Weiße; Matthias Kappler; Alexander W Eckert; Markus Glaß; Danny Misiak; Stefan Hüttelmaier; Wolfgang G Ballhausen; Mechthild Hatzfeld; Monika Haemmerle; Tony Gutschner
Journal:  Mol Cancer       Date:  2021-06-11       Impact factor: 27.401

8.  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

9.  Lck tyrosine kinase mediates β1-integrin signalling to regulate Schwann cell migration and myelination.

Authors:  Jennifer K Ness; Kristin M Snyder; Nikos Tapinos
Journal:  Nat Commun       Date:  2013       Impact factor: 14.919

10.  Dopamine signaling regulates hematopoietic stem and progenitor cell function.

Authors:  Yang Liu; Qi Chen; Hyun-Woo Jeong; Dong Han; Jörg Fabian; Hannes C A Drexler; Martin Stehling; Hans R Schöler; Ralf H Adams
Journal:  Blood       Date:  2021-11-25       Impact factor: 25.476

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