RU2017113351A - Ингибиторы ezh2 человека и способы их применения - Google Patents

Ингибиторы ezh2 человека и способы их применения Download PDF

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RU2017113351A
RU2017113351A RU2017113351A RU2017113351A RU2017113351A RU 2017113351 A RU2017113351 A RU 2017113351A RU 2017113351 A RU2017113351 A RU 2017113351A RU 2017113351 A RU2017113351 A RU 2017113351A RU 2017113351 A RU2017113351 A RU 2017113351A
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dimethylation
control
trimethylation
ratio
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Роберт Аллен КОУПЛЕНД
Виктория Мари РИЧОН
Маргарет Дэвис СКОТТ
Кристофер Джон СНИРИНГЕР
Кевин Уэйн КУНТЦ
Сара Кейтлин НАТСОН
Рой Макфарлэйн ПОЛЛОК
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Эпизайм, Инк.
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Claims (15)

1. Способ, включающий:
a) получение образца ткани от индивидуума;
b) выявление уровня диметилирования (me2) H3-K27, если оно присутствует в указанном образце ткани, и сравнение указанного уровня диметилирования (me2) с контрольным уровнем диметилирования (me2);
c) необязательно выявление уровня триметилирования (me3) H3-K27, если оно присутствует в указанном образце ткани, и сравнение указанного уровня триметилирования (me3) с контрольным уровнем триметилирования (me3),
где указанный индивидуум является отвечающим на ингибитор EZH2, когда указанный уровень диметилирования (me2) отсутствует или ниже указанного контрольного уровня диметилирования (me2), или когда указанный уровень триметилирования (me3) является таким же или более высоким, чем указанный контрольный уровень триметилирования (me3), и указанный уровень диметилирования (me2) отсутствует или ниже указанного контрольного уровня диметилирования (me2).
2. Способ по п.1, дополнительно включающий:
d) получение соотношения уровня диметилирования (me2) и уровня триметилирования (me3) H3-K27 в указанном образце ткани, для получения тестируемого соотношения, и сравнение тестируемого соотношения с контрольным соотношением;
где указанный индивидуум является отвечающим на ингибитор EZH2, когда указанное тестируемое соотношение является более низким, чем указанное контрольное соотношение.
3. Способ по п.1, где указанный индивидуум имеет рак.
4. Способ по п.1, где указанное выявление проводят с помощью анализа, выбранного из анализа с использованием вестерн-блоттинга, иммуногистохимии (IHC), иммунофлуоресценции (IF) и масс-спектрометрии (МС).
5. Способ по п.1, где указанное выявление включает приведение в контакт указанного образца ткани со средством, которое специфично связывается с диметилированным H3-K27 и/или триметилированным H3-K27.
6. Способ по п.5, где указанное средство представляет собой антитело, полипептид, аптамер или их фрагмент.
7. Способ по п.3, где указанный рак выбран из фолликулярной лимфомы и диффузной крупно-B-клеточной лимфомы (DLBCL).
8. Способ по любому из пп.1-7, где у указанного индивидуума экспрессируется мутантный по Y641 полипептид EZH2.
9. Способ по п.8, где указанный мутант по Y641 выбран из Y641F, Y641H, Y641N и Y641S.
RU2017113351A 2010-09-10 2011-09-12 Ингибиторы ezh2 человека и способы их применения RU2765155C2 (ru)

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RU2765155C2 (ru) 2022-01-26
US20170065628A1 (en) 2017-03-09
JP2019070653A (ja) 2019-05-09
RU2013115928A (ru) 2014-10-20
RU2017113351A3 (ru) 2020-08-26
BR112013005806B1 (pt) 2022-05-10
WO2012034132A2 (en) 2012-03-15
CN103261890A (zh) 2013-08-21
US9333217B2 (en) 2016-05-10
US20120071418A1 (en) 2012-03-22
KR20140019770A (ko) 2014-02-17
CA2810998A1 (en) 2012-03-15
ES2570380T3 (es) 2016-05-18
AU2011298987A1 (en) 2013-03-28

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