Targeting the Grb2 cSH3 domain: Design, synthesis and biological evaluation of the first series of modulators.

[1]  M. Zhang,et al.  Synthesis and Structural Characterization of a Monocarboxylic Inhibitor for GRB2 SH2 Domain. , 2021, Bioorganic & medicinal chemistry letters.

[2]  A. Coluccia,et al.  Targeting the Interaction between the SH3 Domain of Grb2 and Gab2 , 2020, Cells.

[3]  B. Perillo,et al.  ROS in cancer therapy: the bright side of the moon , 2020, Experimental & Molecular Medicine.

[4]  R. Nussinov,et al.  High-affinity Interactions of the nSH3/cSH3 Domains of Grb2 with the C-terminal Proline-rich Domain of SOS1. , 2020, Journal of the American Chemical Society.

[5]  Fengshan Wang,et al.  The Role of Grb2 in Cancer and Peptides as Grb2 Antagonists. , 2017, Protein and peptide letters.

[6]  B. Neel,et al.  Distinct GAB2 signaling pathways are essential for myeloid and lymphoid transformation and leukemogenesis by BCR-ABL1. , 2016, Blood.

[7]  Junmin Luo,et al.  Gab2 facilitates epithelial-to-mesenchymal transition via the MEK/ERK/MMP signaling in colorectal cancer , 2016, Journal of experimental & clinical cancer research : CR.

[8]  H. Cheung,et al.  Overexpression of GAB2 in ovarian cancer cells promotes tumor growth and angiogenesis by upregulating chemokine expression , 2015, Oncogene.

[9]  Weina Yu,et al.  Structure and function of Gab2 and its role in cancer (Review) , 2015, Molecular medicine reports.

[10]  John S McMurray,et al.  Targeting SH2 domains in breast cancer. , 2014, Future medicinal chemistry.

[11]  Yanqiong Zhang,et al.  Identification of GRB2 and GAB1 Coexpression as an Unfavorable Prognostic Factor for Hepatocellular Carcinoma by a Combination of Expression Profile and Network Analysis , 2013, PloS one.

[12]  Tony Pawson,et al.  Molecular mechanisms of SH2- and PTB-domain-containing proteins in receptor tyrosine kinase signaling. , 2013, Cold Spring Harbor perspectives in biology.

[13]  P. Simister,et al.  Novel inhibitors of a Grb2 SH3C domain interaction identified by a virtual screen. , 2013, Bioorganic & medicinal chemistry.

[14]  Woody Sherman,et al.  Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments , 2013, Journal of Computer-Aided Molecular Design.

[15]  P. Gunning,et al.  Progress towards the development of SH2 domain inhibitors. , 2013, Chemical Society reviews.

[16]  M. Jin,et al.  Overexpression of Grb2-associated Binder 2 in Human Lung Cancer , 2011, International journal of biological sciences.

[17]  David E. Gloriam,et al.  SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism. , 2010, ACS medicinal chemistry letters.

[18]  Roger J Daly,et al.  Function, regulation and pathological roles of the Gab/DOS docking proteins , 2009, Cell Communication and Signaling.

[19]  M. Lewitzky,et al.  Distinct binding modes of two epitopes in Gab2 that interact with the SH3C domain of Grb2. , 2009, Structure.

[20]  Ying Chen,et al.  Overexpression of Grb2/HER2 signaling in Chinese gastric cancer: their relationship with clinicopathological parameters and prognostic significance , 2009, Journal of Cancer Research and Clinical Oncology.

[21]  T. Burke,et al.  Grb2 signaling in cell motility and cancer , 2008, Expert opinion on therapeutic targets.

[22]  G. Feng,et al.  Role of Gab2 in mammary tumorigenesis and metastasis , 2007, Oncogene.

[23]  Jung Young Lee,et al.  Increased expression of Gab2, a scaffolding adaptor of the tyrosine kinase signalling, in gastric carcinomas , 2007, Pathology.

[24]  Tony Pawson,et al.  Dynamic control of signaling by modular adaptor proteins. , 2007, Current opinion in cell biology.

[25]  Matthew P. Repasky,et al.  Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes. , 2006, Journal of medicinal chemistry.

[26]  F. Speleman,et al.  GAB2 is a novel target of 11q amplification in AML/MDS , 2006, Genes, chromosomes & cancer.

[27]  T. Burke Development of Grb2 SH2 Domain Signaling Antagonists: A Potential New Class of Antiproliferative Agents , 2006, International Journal of Peptide Research and Therapeutics.

[28]  R. Austin,et al.  A UNIFIED MODEL FOR PREDICTING HUMAN HEPATIC, METABOLIC CLEARANCE FROM IN VITRO INTRINSIC CLEARANCE DATA IN HEPATOCYTES AND MICROSOMES , 2005, Drug Metabolism and Disposition.

[29]  F. Malatesta The study of bimolecular reactions under non-pseudo-first order conditions. , 2005, Biophysical chemistry.

[30]  C. Eyermann,et al.  SRC homology-2 inhibitors: peptidomimetic and nonpeptide. , 2002, Mini reviews in medicinal chemistry.

[31]  H. Iwasaki,et al.  Critical role for Gab2 in transformation by BCR/ABL. , 2002, Cancer cell.

[32]  P. Jeffrey,et al.  Utility of metabolic stability screening: comparison of in vitro and in vivo clearance , 2001, Xenobiotica; the fate of foreign compounds in biological systems.

[33]  P. Furet,et al.  Structure-based design of compounds inhibiting Grb2-SH2 mediated protein-protein interactions in signal transduction pathways. , 2000, Current pharmaceutical design.

[34]  N. Shinohara,et al.  Significance of the Grb2 and Son of Sevenless (Sos) Proteins in Human Bladder Cancer Cell Lines , 2000, IUBMB life.

[35]  F. Lombardo,et al.  Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings , 1997 .

[36]  D. Cussac,et al.  The Grb2 adaptor , 1995, FEBS letters.

[37]  J B Houston,et al.  Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. , 1994, Biochemical pharmacology.

[38]  Nanxin Li,et al.  BCR-ABL-induced oncogenesis is mediated by direct interaction with the SH2 domain of the GRB-2 adaptor protein , 1993, Cell.

[39]  Tim Morris,et al.  Physiological Parameters in Laboratory Animals and Humans , 1993, Pharmaceutical Research.

[40]  Andrea Richardson,et al.  A role for the scaffolding adapter GAB2 in breast cancer , 2006, Nature Medicine.