α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer

scientific article published on 17 February 2016

α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1002/CMDC.201500600
P698PubMed publication ID26889658
P5875ResearchGate publication ID295077311

P50authorScott A. WildmanQ38802377
James W. JanetkaQ38802400
P2093author name stringZhenfu Han
Lidija Klampfer
Tommy Kim
Partha Karmakar
Peter K W Harris
Ben Y Owusu
P2860cites workCross-talk between the proto-oncogenes Met and RonQ22254408
Structural insight into distinct mechanisms of protease inhibition by antibodiesQ27649305
Unraveling the allosteric mechanism of serine protease inhibition by an antibodyQ27658583
A Reverse Binding Motif That Contributes to Specific Protease Inhibition by AntibodiesQ27676066
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase InhibitorsQ27684175
Discovery of O-(3-carbamimidoylphenyl)-l-serine amides as matriptase inhibitors using a fragment-linking approachQ27697286
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionQ27860958
Proteolytic activation of pro-macrophage-stimulating protein by hepsin.Q27865259
Roles of c-Met and RON kinases in tumor progression and their potential as therapeutic targetsQ28081193
Activation of hepatocyte growth factor and urokinase/plasminogen activator by matriptase, an epithelial membrane serine proteaseQ28144714
Hepatocyte growth factor is a preferred in vitro substrate for human hepsin, a membrane-anchored serine protease implicated in prostate and ovarian cancersQ31161402
Pericellular activation of hepatocyte growth factor by the transmembrane serine proteases matriptase and hepsin, but not by the membrane-associated protease uPA.Q33518855
Potential therapeutics specific to c-MET/RON receptor tyrosine kinases for molecular targeting in cancer therapyQ33652455
Emerging molecular targets in oncology: clinical potential of MET/hepatocyte growth-factor inhibitorsQ33769437
An allosteric anti-hepsin antibody derived from a constrained phage display libraryQ34132742
Activation of hepatocyte growth factor in the injured tissues is mediated by hepatocyte growth factor activator.Q34379859
A history of cancer chemotherapyQ34869530
Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.Q35604797
Coordinate expression and functional profiling identify an extracellular proteolytic signaling pathwayQ35719884
Oncogene addiction as a foundational rationale for targeted anti-cancer therapy: promises and perilsQ36038823
Scatter factor: molecular characteristics and effect on the invasiveness of epithelial cellsQ36223889
Mechanisms of resistance to EGFR tyrosine kinase inhibitorsQ36238664
Co-expression of RON and MET is a prognostic indicator for patients with transitional-cell carcinoma of the bladderQ36615866
SPINT2 Deregulation in Prostate CarcinomaQ36737100
Knockdown of RON receptor kinase delays but does not prevent tumor progression while enhancing HGF/MET signaling in pancreatic cancer cell linesQ37275734
Targeting MET in cancer: rationale and progressQ37978193
MSP-RON signalling in cancer: pathogenesis and therapeutic potentialQ38116308
Targeting receptor tyrosine kinase MET in cancer: small molecule inhibitors and clinical progressQ38169807
Targeting the oncogenic Met receptor by antibodies and gene therapyQ38216590
Mechanisms of hepatocyte growth factor activation in cancer tissuesQ38255480
Hepatocyte growth factor activator inhibitor type‑1 in cancer: advances and perspectives (Review).Q38259598
Clinical and biological significance of hepsin overexpression in breast cancer.Q38411489
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor ActivationQ38433828
Mechanisms of Resistance to EGFR Tyrosine Kinase Inhibitors and Therapeutic Approaches: An UpdateQ38669280
c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers.Q38826543
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitorsQ38831317
Erk2 but not Erk1 regulates crosstalk between Met and EGFR in squamous cell carcinoma cell linesQ38885876
Conversion from the "oncogene addiction" to "drug addiction" by intensive inhibition of the EGFR and MET in lung cancer with activating EGFR mutationQ39434507
HGF-induced DU145 cell scatter assayQ39508346
Strong expression association between matriptase and its substrate prostasin in breast cancerQ39523621
Ron kinase transphosphorylation sustains MET oncogene addictionQ39611289
Design and synthesis of potent, selective inhibitors of matriptase.Q39734758
Therapeutic potential of hepatocyte growth factor/scatter factor neutralizing antibodies: inhibition of tumor growth in both autocrine and paracrine hepatocyte growth factor/scatter factor:c-Met-driven models of leiomyosarcomaQ39787985
Collaboration of RON and epidermal growth factor receptor in human bladder carcinogenesis.Q40214759
Prognostic significance of co-expression of RON and MET receptors in node-negative breast cancer patients.Q40443024
Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in CancerQ42837140
The hepatocyte growth factor regulatory factors in human breast cancerQ44735694
Hepatocyte growth factor activator is a serum activator of single-chain precursor macrophage-stimulating protein.Q46003940
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug designQ46383079
The prognostic significance of RON and MET receptor coexpression in patients with colorectal cancerQ46553705
Cancer chemotherapy: a critical analysis of its 60 years of historyQ48449340
Plasma macrophage-stimulating protein and hepatocyte growth factor levels are associated with prostate cancer progression.Q54254288
Processing of hepatocyte growth factor to the heterodimeric form is required for biological activityQ67543328
Proteolytic cleavage and activation of pro-macrophage-stimulating protein and upregulation of its receptor in tissue injuryQ77386429
Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptaseQ79842080
Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptase and matriptase-2Q85942507
New 3-amidinophenylalanine-derived inhibitors of matriptaseQ104520902
P433issue6
P304page(s)585-599
P577publication date2016-02-17
P1433published inChemMedChemQ2962252
P1476titleα-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer
P478volume11

Reverse relations

cites work (P2860)
Q90141187Cell surface-anchored serine proteases in cancer progression and metastasis
Q38831784Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment
Q60920626Hepatocyte growth factor activator inhibitor-2 stabilizes Epcam and maintains epithelial organization in the mouse intestine
Q39816968Inhibition of pro-HGF activation by SRI31215, a novel approach to block oncogenic HGF/MET signaling
Q98164379Targeted therapies in gynecological cancers: a comprehensive review of clinical evidence
Q41825773Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation.
Q39274990The c-Met receptor: Implication for targeted therapies in colorectal cancer
Q39015415The role of type II transmembrane serine protease-mediated signaling in cancer

Search more.