WO2012078982A3 - Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells - Google Patents

Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells Download PDF

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Publication number
WO2012078982A3
WO2012078982A3 PCT/US2011/064152 US2011064152W WO2012078982A3 WO 2012078982 A3 WO2012078982 A3 WO 2012078982A3 US 2011064152 W US2011064152 W US 2011064152W WO 2012078982 A3 WO2012078982 A3 WO 2012078982A3
Authority
WO
WIPO (PCT)
Prior art keywords
xzh
stat3 phosphorylation
interleukin
hepatocellular carcinoma
carcinoma cells
Prior art date
Application number
PCT/US2011/064152
Other languages
French (fr)
Other versions
WO2012078982A2 (en
Inventor
Chenglong Li
Jiayuh Lin
Hong Wang
Original Assignee
The Ohio State University
Nationwide Children's Hospital, Inc.
Miami University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Ohio State University, Nationwide Children's Hospital, Inc., Miami University filed Critical The Ohio State University
Publication of WO2012078982A2 publication Critical patent/WO2012078982A2/en
Publication of WO2012078982A3 publication Critical patent/WO2012078982A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6872—Intracellular protein regulatory factors and their receptors, e.g. including ion channels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701—Details
    • G01N2333/4703—Regulators; Modulating activity
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/70—Mechanisms involved in disease identification
    • G01N2800/7023—(Hyper)proliferation
    • G01N2800/7028—Cancer

Abstract

The present disclosure provides compounds, compositions of matter and methods related to XZH-5 and related chemical therapeutics. The inhibitory effects of a series of small molecules structurally related to XZH-5 on STAT3 phosphorylation is disclosed, as are the results of that inhibition, including induction of apoptosis, reduction of colony forming ability, inhibition of IL-6- induced STAT3 phosphorylation, and nuclear translocation and STAT3 DNA binding activity.
PCT/US2011/064152 2010-12-09 2011-12-09 Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells WO2012078982A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42134110P 2010-12-09 2010-12-09
US61/421,341 2010-12-09

Publications (2)

Publication Number Publication Date
WO2012078982A2 WO2012078982A2 (en) 2012-06-14
WO2012078982A3 true WO2012078982A3 (en) 2012-09-07

Family

ID=46207764

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/064152 WO2012078982A2 (en) 2010-12-09 2011-12-09 Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells

Country Status (1)

Country Link
WO (1) WO2012078982A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012078982A2 (en) * 2010-12-09 2012-06-14 The Ohio State University Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells
US11485750B1 (en) 2019-04-05 2022-11-01 Kymera Therapeutics, Inc. STAT degraders and uses thereof
KR102199141B1 (en) * 2019-05-03 2021-01-06 사회복지법인 삼성생명공익재단 Diagnostic biomarker of colorectal cancer using cytokine-induced STAT phosphorylation in peripheral blood immune cells by flow cytometry

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004073650A2 (en) * 2003-02-20 2004-09-02 University Of South Florida Peptidomimetic inhibitors of stat3 activity and their medical uses
US20090069420A1 (en) * 2006-05-19 2009-03-12 H. Lee Moffitt Cancer Center & Research Institute Small molecule inhibitors of STAT3 with anti-tumor activity
WO2009036099A1 (en) * 2007-09-10 2009-03-19 Boston Biomedical, Inc. A novel group of stat3 pathway inhibitors and cancer stem cell pathway inhibitors
WO2012078982A2 (en) * 2010-12-09 2012-06-14 The Ohio State University Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004073650A2 (en) * 2003-02-20 2004-09-02 University Of South Florida Peptidomimetic inhibitors of stat3 activity and their medical uses
US20090069420A1 (en) * 2006-05-19 2009-03-12 H. Lee Moffitt Cancer Center & Research Institute Small molecule inhibitors of STAT3 with anti-tumor activity
WO2009036099A1 (en) * 2007-09-10 2009-03-19 Boston Biomedical, Inc. A novel group of stat3 pathway inhibitors and cancer stem cell pathway inhibitors
WO2012078982A2 (en) * 2010-12-09 2012-06-14 The Ohio State University Xzh-5 inhibits constitutive and interleukin-6-induced stat3 phosphorylation in human hepatocellular carcinoma cells

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE PUBCHEM 21 July 2009 (2009-07-21), "2-[[(2-phenylcarbamoylamino)acetyl]amino]acetic acid", retrieved from http://pubchem.ncbi.nlm.nih.gov/summarylsummary.cgi?cid=43354399&loc=eç rcs accession no. 3354399 *

Also Published As

Publication number Publication date
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