CN108137550A - 对bet溴结构域抑制剂的抗性的机理 - Google Patents

对bet溴结构域抑制剂的抗性的机理 Download PDF

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Publication number
CN108137550A
CN108137550A CN201680058347.9A CN201680058347A CN108137550A CN 108137550 A CN108137550 A CN 108137550A CN 201680058347 A CN201680058347 A CN 201680058347A CN 108137550 A CN108137550 A CN 108137550A
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inhibitor
cancer
bet
bcl
brd4
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CN201680058347.9A
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Chinese (zh)
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K·波利亚克
S·舒
J·E·布拉德内尔
C·Y·林
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
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    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57515—Immunoassay; Biospecific binding assay; Materials therefor for cancer of the breast
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • 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
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    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
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CN201680058347.9A 2015-08-10 2016-08-10 对bet溴结构域抑制剂的抗性的机理 Pending CN108137550A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562203128P 2015-08-10 2015-08-10
US62/203,128 2015-08-10
PCT/US2016/046318 WO2017027571A1 (en) 2015-08-10 2016-08-10 Mechanism of resistance to bet bromodomain inhibitors

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CN108137550A true CN108137550A (zh) 2018-06-08

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US (1) US11666580B2 (enExample)
EP (2) EP4585273A3 (enExample)
JP (1) JP2018531891A (enExample)
KR (1) KR20180035905A (enExample)
CN (1) CN108137550A (enExample)
AU (2) AU2016304856B8 (enExample)
BR (1) BR112018002550A2 (enExample)
CA (1) CA2995374A1 (enExample)
CL (1) CL2018000377A1 (enExample)
HK (1) HK1254201A1 (enExample)
IL (1) IL257386A (enExample)
MX (1) MX2018001737A (enExample)
PE (1) PE20181088A1 (enExample)
RU (1) RU2018108165A (enExample)
WO (1) WO2017027571A1 (enExample)
ZA (1) ZA201800969B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114617878A (zh) * 2022-05-16 2022-06-14 深圳大学 Ck2抑制剂在制备抗衰药物中的应用
CN115894678A (zh) * 2022-07-15 2023-04-04 北京顺元天生物制品有限公司 一种干细胞细胞因子的制备方法及其在制备药品中的用途

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180035905A (ko) 2015-08-10 2018-04-06 다나-파버 캔서 인스티튜트 인크. Bet 브로모도메인 억제제에 대한 저항성의 메카니즘
GB201704536D0 (en) * 2017-03-22 2017-05-03 Univ Malta Method
US11712439B2 (en) 2017-08-09 2023-08-01 Mayo Foundation For Medical Education And Research Methods and materials for identifying and treating bet inhibitor-resistant cancers
CN109503618A (zh) * 2017-09-14 2019-03-22 成都海创药业有限公司 一种brd4抑制剂
CN108084193A (zh) * 2017-12-19 2018-05-29 郭守东 一种brd4蛋白抑制剂
WO2020023768A1 (en) 2018-07-25 2020-01-30 Mayo Foundation For Medical Education And Research Methods and materials for identifying and treating bet inhibitor-resistant cancers
US20220062291A1 (en) * 2018-12-21 2022-03-03 Dana-Farber Cancer Institute, Inc. Compositions and methods of treating cancers by administering a phenothiazine-related drug that activates protein phosphatase 2a (pp2a) with reduced inhibitory activity targeted to the dopamine d2 receptor and accompanying toxicity
PT116050B (pt) * 2020-01-09 2022-06-15 Hovione Farm S A Conjugados fármaco-ligando e inibidores das proteínas da família bromodomínio e domínio extraterminal -(bet) modificados
AU2021298154A1 (en) * 2020-06-25 2023-02-23 Tolremo Therapeutics Ag Combination of a CBP/p300 bromodomain inhibitor and a KRAS inhibitor for the treatment of cancer
WO2023041744A1 (en) 2021-09-17 2023-03-23 Institut Curie Bet inhibitors for treating pab1 deficient cancer
EP4480494A4 (en) * 2022-02-16 2026-03-11 Univ Nat Corp Tokyo Medical & Dental COMPOSITION INTENDED FOR USE IN THE TREATMENT OF CANCER, INFLAMMATORY DISEASES OR OBESITY, AND ITS USE

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140005169A1 (en) * 2010-12-02 2014-01-02 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA103867A (en) 1907-02-01 1907-03-05 Charles M. Thrasher Nut lock
CA120184A (en) 1908-09-08 1909-08-24 George Albert Thornhill Bottle labelling machine
CA168504A (en) 1915-01-09 1916-03-28 Carl Lorentz Nilson Locomotive
AU6854098A (en) 1997-04-18 1998-11-13 Chugai Research Institute For Molecular Medicine, Inc. Transcriptional regulator
EP1077219A4 (en) 1998-04-30 2005-02-23 Chugai Pharmaceutical Co Ltd Transcriptional, regulatory factor
US20120028912A1 (en) 2000-02-22 2012-02-02 J.David Gladstone Institute Methods of modulating bromodomains
US6607916B2 (en) 2001-02-08 2003-08-19 Isis Pharmaceuticals, Inc. Antisense inhibition of Casein kinase 2-alpha expression
US8522267B2 (en) 2002-03-08 2013-08-27 Caption Colorado Llc Method and apparatus for control of closed captioning
US8557812B2 (en) 2004-08-20 2013-10-15 The Regents Of The University Of Michigan Small molecule inhibitors of anti-apoptotic BCL-2 family members and the uses thereof
WO2006065724A2 (en) 2004-12-14 2006-06-22 Regents Of The University Of Minnesota Casein kinase 2 antisense therapy
WO2006069186A2 (en) 2004-12-22 2006-06-29 The Ohio State Research Foundation Small molecule bcl-xl/bcl-2 binding inhibitors
WO2008060695A2 (en) 2006-05-22 2008-05-22 The Trustees Of The University Of Pennsylvania Antiviral inhibition of casein kinase ii
WO2007143081A2 (en) 2006-06-02 2007-12-13 The Ohio State University Research Foundation Therapeutic agents for the treatment of lymphoid malignancies
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
WO2008119109A1 (en) 2007-03-29 2008-10-09 Velacor Therapeutics Pty Ltd Treatment of neurological disorders
ES2529790T3 (es) 2007-04-13 2015-02-25 Dana-Farber Cancer Institute, Inc. Métodos de tratamiento de cáncer resistente a agentes terapéuticos de ERBB
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
WO2009117769A1 (en) * 2008-03-25 2009-10-01 Newcastle Innovation Limited Inhibition of c-kit cancers
JP2012523458A (ja) 2009-04-13 2012-10-04 ザ オハイオ ステート ユニバーシティー リサーチ ファウンデーション タンパク質ホスファターゼ２ａ活性化剤
US9307184B2 (en) 2009-07-31 2016-04-05 Echostar Technologies L.L.C. Multi-user recording allocation
US8865901B2 (en) 2009-10-02 2014-10-21 Fred Hutchinson Cancer Research Center Gain-of-function Bcl-2 inhibitors
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US9360482B2 (en) 2009-11-05 2016-06-07 Glaxosmithkline Llc Process for the identification of a compound which inhibits the binding of the second bromodomain of each of human BRD-2, BRD-3, and BRD-4
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US8862173B2 (en) 2009-12-10 2014-10-14 Motorola Solutions, Inc. Method for selecting media for delivery to users at an incident
US20110207789A1 (en) 2010-02-19 2011-08-25 Ye Fang Methods related to casein kinase ii (ck2) inhibitors and the use of purinosome-disrupting ck2 inhibitors for anti-cancer therapy agents
MX373121B (es) 2010-05-14 2020-04-30 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
MX384074B (es) 2010-05-14 2025-03-12 Dana Farber Cancer Inst Inc Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
MY165884A (en) 2010-11-23 2018-05-18 Abbvie Ireland Unlimited Co Methods of treatment using selective bcl-2 inhibitors
JP5998152B2 (ja) 2011-01-25 2016-09-28 ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン Ｂｃｌ−２／ｂｃｌ−ｘｌ阻害剤およびそれを使用する治療方法
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US9220706B2 (en) 2012-06-01 2015-12-29 National Institutes Of Health (Nih) Inhibition of leukemic stem cells by PP2A activating agents
EP2861255B1 (en) * 2012-06-19 2019-10-09 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
DE102012212436B4 (de) 2012-07-16 2022-07-14 Coretronic Corporation Lichtmodul für eine Projektionsvorrichtung und Verfahren zur Generierung des Blauanteils in einem Lichtmodul für eine Projektionsvorrichtung
WO2014039994A2 (en) 2012-09-07 2014-03-13 Carlos Cordon-Cardo Targeting chemotherapy agent resistance in cancer
US20140296218A1 (en) * 2012-10-25 2014-10-02 Whitehead Institute For Biomedical Research Super-enhancers and methods of use thereof
US9073878B2 (en) * 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2015018522A1 (en) 2013-08-06 2015-02-12 Oncoethix Sa Bet-bromodomain inhibitor shows synergism with several anti-cancer agents in pre-clinical models of diffuse large b-cell lymphoma (dlbcl)
EP3066101B1 (en) * 2013-11-08 2020-07-29 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors
CN105960239A (zh) 2013-11-27 2016-09-21 翁科埃斯克斯有限公司 利用含有噻吩并三唑并二氮杂*化合物的药物制剂治疗白血病的方法
WO2015109286A1 (en) * 2014-01-20 2015-07-23 Gilead Sciences, Inc. Therapies for treating cancers
WO2016203335A1 (en) * 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
KR20180035905A (ko) 2015-08-10 2018-04-06 다나-파버 캔서 인스티튜트 인크. Bet 브로모도메인 억제제에 대한 저항성의 메카니즘

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140005169A1 (en) * 2010-12-02 2014-01-02 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DHONG HYUN LEE等: "Synergistic effect of JQ1 and rapamycin for treatment of human osteosarcoma", 《INTERNATIONAL JOURNAL OF CANCER》 *
KRISHAN KUMAR等: "GLI2-dependent c-MYC upregulation mediates resistance of pancreatic cancer cells to the BET bromodomain inhibitor JQ1", 《SCIENFITIC REPORTS》 *
TEERU BIHANI等: "Resistance to everolimus driven by epigenetic regulation of MYC in ER+ breast cancers", 《ONCOTARGET》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114617878A (zh) * 2022-05-16 2022-06-14 深圳大学 Ck2抑制剂在制备抗衰药物中的应用
CN115894678A (zh) * 2022-07-15 2023-04-04 北京顺元天生物制品有限公司 一种干细胞细胞因子的制备方法及其在制备药品中的用途
CN115894678B (zh) * 2022-07-15 2023-10-20 新疆赛尔托马斯生物科技有限公司 一种干细胞细胞因子的制备方法及其在制备药品中的用途

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