Tyrosine Kinase Inhibitors Targeted to the Epidermal Growth Factor Receptor Subfamily

Human Breast Cancer: Correlation of Relapse and Survival with Amplification of the HER-2/ neu Oncogene

1987 • 11,429 citations

Studies of the HER-2/ neu Proto-Oncogene in Human Breast and Ovarian Cancer

1989 • 6,734 citations

The Protein Kinase Family: Conserved Features and Deduced Phylogeny of the Catalytic Domains

1988 • 5,115 citations

Genistein, a specific inhibitor of tyrosine-specific protein kinases.

1987 • 3,773 citations

Protein kinases 6. The eukaryotic protein kinase superfamily: kinase (catalytic) domain structure and classification.

1995 • 2,534 citations

The eukaryotic protein kinase superfamily: kinase (catalytic) domain structure and classification ¹

1995 • 2,199 citations

Tyrosine Kinase Inhibition: An Approach to Drug Development

1995 • 1,655 citations

[2] Protein kinase catalytic domain sequence database: Identification of conserved features of primary structure and classification of family members

1991 • 1,225 citations

Structures of the Tyrosine Kinase Domain of Fibroblast Growth Factor Receptor in Complex with Inhibitors

1997 • 1,098 citations

Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment.

1998 • 1,086 citations

Crystal structure of the tyrosine kinase domain of the human insulin receptor

1994 • 1,071 citations

SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumor vascularization, and growth of multiple tumor types.

1999 • 1,044 citations

Recombinant humanized anti-HER2 antibody (Herceptin) enhances the antitumor activity of paclitaxel and doxorubicin against HER2/neu overexpressing human breast cancer xenografts.

1998 • 1,013 citations

Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog

1997 • 929 citations

A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase

1994 • 800 citations

Cooperation between oncogenes

1991 • 792 citations

Biological efficacy of a chimeric antibody to the epidermal growth factor receptor in a human tumor xenograft model.

1995 • 791 citations

p185^HER2 Monoclonal Antibody Has Antiproliferative Effects In Vitro and Sensitizes Human Breast Tumor Cells to Tumor Necrosis Factor

1989 • 672 citations

Anti-epidermal growth factor receptor antibody C225 inhibits angiogenesis in human transitional cell carcinoma growing orthotopically in nude mice.

1999 • 599 citations

CONVERSION OF PHOSPHORYLASE b TO PHOSPHORYLASE a IN MUSCLE EXTRACTS

1955 • 496 citations

p185HER2 monoclonal antibody has antiproliferative effects in vitro and sensitizes human breast tumor cells to tumor necrosis factor.

1989 • 479 citations

Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain

1998 • 477 citations

Activating SRC mutation in a subset of advanced human colon cancers

1999 • 473 citations

Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor

1998 • 414 citations

Down-modulation of an oncogene protein product and reversion of the transformed phenotype by monoclonal antibodies

1985 • 408 citations

In Vivo Eradication of Human BCR/ABL-Positive Leukemia Cells With an ABL Kinase Inhibitor

1999 • 388 citations

The addition of Herceptin (humanized anti-HER2 antibody) to first-line chemotherapy for HER2-overexpressing metastatic breast cancer (HER2+ MBC) markedly increases anti-cancer activity: A randomized, multinational controlled phase II trial.

1998 • 366 citations

Antitumor activity of sequential treatment with topotecan and anti-epidermal growth factor receptor monoclonal antibody C225.

1999 • 335 citations

Eradication of established tumors by a fully human monoclonal antibody to the epidermal growth factor receptor without concomitant chemotherapy.

1999 • 329 citations

Transformation by Rous sarcoma virus: A cellular substrate for transformation-specific protein phosphorylation contains phosphotyrosine

1980 • 328 citations

Epidermal growth factor receptor inhibition by a monoclonal antibody as anticancer therapy.

1997 • 314 citations

Single-Chain Antibody-Mediated Intracellular Retention of ErbB-2 Impairs Neu Differentiation Factor and Epidermal Growth Factor Signaling

1995 • 300 citations

Structure of the amino-terminal domain of Cbl complexed to its binding site on ZAP-70 kinase

1999 • 299 citations

Biotherapy of B-cell precursor leukemia by targeting genistein to CD19-associated tyrosine kinases

1995 • 279 citations

Efficient reversion of simian sarcoma virus-transformation and inhibition of growth factor-induced mitogenesis by suramin.

1986 • 270 citations

Crystal structure of the first three domains of the type-1 insulin-like growth factor receptor

1998 • 253 citations

A monoclonal antibody against the c-erbB-2 protein enhances the cytotoxicity of cis-diamminedichloroplatinum against human breast and ovarian tumor cell lines.

1991 • 229 citations

Suramin: a novel antineoplastic agent with multiple potential mechanisms of action.

1993 • 229 citations

Involvement of p27KIP1 in G1 arrest mediated by an anti-epidermal growth factor receptor monoclonal antibody.

1996 • 228 citations

Studies on a new epidermal growth factor-receptor kinase inhibitor, erbstatin, produced by MH435-hF3.

1986 • 214 citations

The structural basis for substrate recognition and control by protein kinases¹

1998 • 204 citations

Use of a Pharmacophore Model for the Design of EGF-R Tyrosine Kinase Inhibitors: 4-(Phenylamino)pyrazolo[3,4-d]pyrimidines

1997 • 201 citations

Protein Kinase InhibitorsThe Tyrosine-Specific Protein Kinases

1998 • 197 citations

Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: a key enzyme in angiogenesis

1999 • 196 citations

Rational Design and Synthesis of a Novel Anti-leukemic Agent Targeting Bruton′s Tyrosine Kinase (BTK), LFM-A13 [α-Cyano-β-Hydroxy-β-Methyl-N-(2,5-Dibromophenyl)Propenamide]

1999 • 187 citations

Selective inhibition of cell proliferation and BCR-ABL phosphorylation in acute lymphoblastic leukemia cells expressing Mr 190,000 BCR-ABL protein by a tyrosine kinase inhibitor (CGP-57148).

1998 • 185 citations

Phase Ia/Ib trial of bispecific antibody MDX-210 in patients with advanced breast or ovarian cancer that overexpresses the proto-oncogene HER-2/neu.

1995 • 184 citations

Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.

1999 • 169 citations

A truncated intracellular HER2/neu receptor produced by alternative RNA processing affects growth of human carcinoma cells.

1993 • 161 citations

Inactivation and Activation of Liver Phosphorylase

1955 • 158 citations

4-(Phenylamino)pyrrolopyrimidines: Potent and Selective, ATP Site Directed Inhibitors of the EGF-Receptor Protein Tyrosine Kinase

1996 • 148 citations

Clinical experience with CD64-directed immunotherapy. An overview

1997 • 146 citations

Single‐chain Fvs

1995 • 143 citations

Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine 1 1Edited by I. A. Wilson

1999 • 138 citations

Tyrosine kinase inhibitors, emodin and its derivative repress HER-2/neu-induced cellular transformation and metastasis-associated properties

1998 • 118 citations

Tyrosine Kinase Inhibitors. 10. Isomeric 4-[(3-Bromophenyl)amino]pyrido[d]- pyrimidines Are Potent ATP Binding Site Inhibitors of the Tyrosine Kinase Function of the Epidermal Growth Factor Receptor

1996 • 116 citations

Crystal structure of the ligand-binding domain of the receptor tyrosine kinase EphB2

1998 • 114 citations

Tyrosine Kinase Inhibitors. 14. Structure−Activity Relationships for Methyl- amino-Substituted Derivatives of 4-[(3-Bromophenyl)amino]-6-(methylamino)- pyrido[3,4-d]pyrimidine (PD 158780), a Potent and Specific Inhibitor of the Tyrosine Kinase Activity of Receptors for the EGF Family of Growth Factors

1998 • 112 citations

Inhibitors of tyrosine kinase

1997 • 107 citations

4,5-Dianilinophthalimide: a protein-tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity.

1994 • 101 citations

1001 Protein Kinases Redux—Towards 2000

1994 • 91 citations

Intracellular expression of a single-chain antibody directed to the EGFR leads to growth inhibition of tumor cells.

1996 • 85 citations

EGFR blockade by tyrosine kinase inhibitor or monoclonal antibody inhibits growth, directs terminal differentiation and induces apoptosis in the human squamous cell carcinoma HN5.

1998 • 82 citations

Genes and cancer

1999 • 79 citations

Naamidine A Is an Antagonist of the Epidermal Growth Factor Receptor and an in Vivo Active Antitumor Agent

1998 • 79 citations

In vivo toxicity, pharmacokinetics, and anticancer activity of Genistein linked to recombinant human epidermal growth factor.

1998 • 78 citations

ZD1839, AN EPIDERMAL GROWTH FACTOR TYROSINE KINASE INHIBITOR SELECTED FOR CLINICAL DEVELOPMENT

1997 • 70 citations

Cytotoxic activity of epidermal growth factor-genistein against breast cancer cells.

1998 • 69 citations

Antitumor activity of anti-epidermal growth factor receptor monoclonal antibodies and cisplatin in ten human head and neck squamous cell carcinoma lines.

1998 • 68 citations

Single-step purification of bispecific monoclonal antibodies for immunotherapeutic use by hydrophobic interaction chromatography

1997 • 64 citations

Prognostic significance of the receptor for epidermal growth factor in human mammary carcinomas.

1987 • 63 citations

Bispecific antibody-dependent cellular cytotoxicity of HER2/neu-overexpressing tumor cells by Fc gamma receptor type I-expressing effector cells.

1997 • 60 citations

Suppression of metastasis formation by a recombinant single chain antibody-toxin targeted to full-length and oncogenic variant EGF receptors

1999 • 59 citations

Differential pp60c-src activity in well and poorly differentiated human colon carcinomas and cell lines.

1992 • 55 citations

Systemic treatment with a recombinant erbB-2 receptor-specific tumor toxin efficiently reduces pulmonary metastases in mice injected with genetically modified carcinoma cells.

1998 • 53 citations

A bivalent single-chain antibody-toxin specific for ErbB-2 and the EGF receptor

1996 • 52 citations

Solution structure of acidic fibroblast growth factor bound to 1,3,6-naphthalenetrisulfonate: A minimal model for the anti-tumoral action of suramins and suradistas 1 1Edited by P. E. Wright

1998 • 50 citations

Synthesis and biological evaluation of aeroplysinin analogues: a new class of receptor tyrosine kinase inhibitors

1998 • 49 citations

Human pancreatic RNase1-human epidermal growth factor fusion: an entirely human 'immunotoxin analog' with cytotoxic properties against squamous cell carcinomas

1998 • 45 citations

Recombinant immunotoxins directed against the c-erb-2/HER2/neu oncogene product: in vitro cytotoxicity, pharmacokinetics, and in vivo efficacy studies in xenograft models.

1999 • 44 citations

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity restores β1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors

1998 • 44 citations

Targeted inhibition of tumour cell growth by a bispecific single-chain toxin containing an antibody domain and TGF α

1996 • 42 citations

Therapy of human transitional cell carcinoma of the bladder by oral administration of the epidermal growth factor receptor protein tyrosine kinase inhibitor 4,5-dianilinophthalimide.

1997 • 36 citations

SRC as a target for anti-cancer drugs.

1996 • 34 citations

Targeting tumor cellsvia EGF receptors: Selective toxicity of an HBEGF-toxin fusion protein

1998 • 34 citations

Cytolytic and cytostatic properties of an anti-human Fc gammaRI (CD64) x epidermal growth factor bispecific fusion protein.

1997 • 32 citations

Small molecule inhibitors of the platelet-derived growth factor receptor, the fibroblast growth factor receptor, and Src family tyrosine kinases

1997 • 32 citations

Cloning and cytotoxicity of fusion proteins of EGF and angiogenin

1999 • 32 citations

A Truncated Intracellular HER2/neu Receptor Produced by Alternative RNA Processing Affects Growth of Human Carcinoma Cells

1993 • 32 citations

Redesigning small molecule—protein interfaces

1998 • 31 citations

In vitro and in vivo stability and anti-tumour efficacy of an anti-EGFR/anti-CD3 F(ab')2 bispecific monoclonal antibody

1995 • 30 citations

Expression of an oncogenic mutant EGF receptor markedly increases the sensitivity of cells to an EGF‐receptor‐specific antibody‐toxin

1998 • 30 citations

Role of target antigen in bispecific-antibody-mediated killing of human glioblastoma cells: A pre-clinical study

1999 • 28 citations

Recombinant heregulin-Pseudomonas exotoxin fusion proteins: interactions with the heregulin receptors and antitumor activity in vivo.

1998 • 27 citations

Peptide containing the BCR oligomerization domain (AA 1-160) reverses the transformed phenotype of p210bcr–abl positive 32D myeloid leukemia cells

1998 • 26 citations

Differential Expression of Alternatively Spliced c-erbB-2 mRNA in Primary Tumors, Lymph Node Metastases, and Bone Marrow Micrometastases from Breast Cancer Patients

1998 • 26 citations

Why toxins!

1996 • 25 citations

In vivo toxicity and pharmacokinetic features of B43 (anti-CD19)-genistein immunoconjugate in nonhuman primates.

1998 • 24 citations

Inhibition of signaling from Type 1 receptor tyrosine kinases via intracellular expression of single-chain antibodies

1996 • 24 citations

Tyrosine kinase inhibitors. 2. Synthesis of 2,2'-dithiobis(1H-indole-3-alkanamides) and investigation of their inhibitory activity against epidermal growth factor receptor and pp60v-src protein tyrosine kinases

1994 • 24 citations

Selective killing of tumor cells using EGF or TGF alpha-Pseudomonas exotoxin chimeric molecules.

1990 • 24 citations

Suramin Inhibits the Growth of Non-Small-Cell Lung Cancer Cells That Express the Epidermal Growth Factor Receptor

1997 • 22 citations

Expression of an oncogenic mutant EGF receptor markedly increases the sensitivity of cells to an EGF-receptor-specific antibody-toxin

1998 • 21 citations

The current state of oncogenes and cancer: Experimental approaches for analyzing oncogenetic events in human cancer

1990 • 21 citations

EGF Family Receptors and Their Ligands in Human Cancer

1998 • 19 citations

In Vivo., Toxicity and Pharmacokinetic Features of B43(Anti-CD19)-Genistein Immunoconjugate

1998 • 16 citations

Activity of anti-erbB-2 recombinant toxin OLX-209 on lung cancer cell lines in the absence of erbB-2 gene amplification

1996 • 16 citations

Design of a potent peptide inhibitor of the epidermal growth factor receptor tyrosine kinase utilizing sequences based on the natural phosphorylation sites of phospholipase C-γ1

1994 • 16 citations

Preclinical testing of an anti-erbB-2 recombinant toxin

1996 • 15 citations

Alpha-cyano-beta-hydroxy-beta-methyl-N-[4-(trifluoromethoxy)phenyl] propenamide: an inhibitor of the epidermal growth factor receptor tyrosine kinase with potent cytotoxic activity against breast cancer cells.

1998 • 15 citations

Effect of Suramin on Human Esophageal Cancer Cells in Vitro and in Vivo

1997 • 10 citations

In vitro and in vivo activity of a recombinant toxin, OLX-209, which targets the erbB-2 oncoprotein

1994 • 4 citations

Bacterial Expression and Characterization of Recombinant Biologically Active Anti-Tyrosine Kinase Receptor Antibody Forms

1998 • 3 citations

ChemInform Abstract: Tyrosine Kinase Inhibitors. Part 2. Synthesis of 2,2′‐Dithiobis(1H‐ indole‐3‐alkanamides) and Investigation of Their Inhibitory Activity Against Epidermal Growth Factor (EGF) Receptor and pp60v‐src Protein Tyrosine Kinases.

1994 • 3 citations