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Methods of treating cancer by inhibiting setd2

A cancer, inhibitor technology, applied in the field of cancer treatment by inhibiting SETD2

Pending Publication Date: 2020-05-01
EPIZYME
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And, despite the existence of effective cancer therapies, suboptimal response, relapse...

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  • Methods of treating cancer by inhibiting setd2
  • Methods of treating cancer by inhibiting setd2
  • Methods of treating cancer by inhibiting setd2

Examples

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example 1

[0138] Pancreatic ductal adenocarcinoma (PDAC) cell lines depend on SETD2 for proliferation

[0139] CRISPR pooling screen.The 249 cancer cell line and the untransformed MCF10A cell line (control) were infected with pooled lentiviruses containing CRISPR-sgRNA libraries targeting different genes, including human SETD2. Cell lines were obtained from ATCC, DSMZ or JCRB cell banks. Figure 1A with 1B Each bar in the graph represents a cell line. The LogP score on the Y-axis of the graph represents the depletion of a specific target in the population. Therefore, the LogP score indicates the dependence of each cell line on a specific gene. In this case, the survival of each cell line with a LogP score below −2.5 was dependent on SETD2. Table 1 lists all cell lines with their mean LogP and median fold change values.

[0140] Figure 1A Graphs are shown for all 250 cell lines studied. Figure 1B A graph showing cell lines derived from pancreatic ductal adenocarcinoma (PDAC). ...

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Abstract

The present disclosure provides methods and pharmaceutical compositions for treating or slowing the progression of cancer, i.e., pancreatic cancer or esophageal cancer, by administering to a human subject in need thereof a therapeutically effective amount of an inhibitor of the histone methyltransferase, SETD2.

Description

[0001] References to Electronically Submitted Sequence Listings [0002] The contents of the electronically filed sequence listing in the ASCII text file (named 3562.012000_Sequence_listing_ST25.txt; size: 1,142 bytes; and date created: August 14, 2017) filed with this application are hereby incorporated by reference in their entirety . technical field [0003] The present disclosure relates generally to the field of epigenetics-based cancer therapy. More specifically, the present disclosure relates to methods and pharmaceutical compositions for treating cancer by inhibiting the human histone methyltransferase SETD2. Background technique [0004] The selective addition of methyl groups to specific amino acid sites of histones is controlled by the action of a family of enzymes known as histone methyltransferases (HMTs). The expression level of a particular gene is affected by the presence or absence of one or more methyl groups at the relevant histone sites. The specific r...

Claims

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Application Information

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IPC IPC(8): C12N15/113C12Q1/00
CPCC12N15/1137C12N2310/14C12N2310/20C12N2320/11C12N2740/16043C12Q1/00C12Y201/01043C12N9/1007C07K16/18C12N15/102A61P35/00A61P35/02A61K31/713A61K48/00C07K2317/24C07K2317/54C07K2317/55A61K2039/505A61K31/7076A61K31/7088A61K38/465A61K39/3955C07K16/40C07K2317/76C12N9/22C12N15/11C12N2800/80C12N5/0693
Inventor 亚历山德拉·罗斯·格拉西安迈克尔·托梅纽斯詹尼弗·安妮·托特曼
Owner EPIZYME
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