Application of an omonasteine ligation strategy for the total chemical synthesis of the BRD7 bromodomain.

نویسندگان

  • Pieter Van de Vijver
  • Liesbeth Scheer
  • Judy van Beijnum
  • Arjan Griffioen
  • Tilman M Hackeng
چکیده

The use of omonasteine (Omo) in sequential peptide ligation strategies extends the scope of homocysteine (Hcy) ligation to longer, methionine-rich proteins. Hcy-to-Omo conversion can be performed on-resin, while the Omo-to-Hcy deprotection can be performed in situ after peptide ligation. This strategy was successfully applied in the synthesis of the BRD7 bromodomain.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor†

The bromodomain-containing proteins BRD9 and BRD7 are part of the human SWI/SNF chromatin-remodeling complexes BAF and PBAF. To date, no selective inhibitor for BRD7/9 has been reported despite its potential value as a biological tool or as a lead for future therapeutics. The quinolone-fused lactam LP99 is now reported as the first potent and selective inhibitor of the BRD7 and BRD9 bromodomain...

متن کامل

Targeting the anaphase-promoting complex/cyclosome (APC/C)- bromodomain containing 7 (BRD7) pathway for human osteosarcoma

Osteosarcoma is the most common primary malignant bone tumor in childhood and adolescence and has a propensity for local invasion and early lung metastasis. However, the current therapies often result in chemoresistance, and a therapeutic target is not available in the clinic for osteosarcoma. Here, we report that BRD7 forms a complex with the anaphase-promoting complex/cyclosome (APC/C) and is...

متن کامل

BRD7 Acts as a Tumor Suppressor Gene in Lung Adenocarcinoma

Lung cancer is one of the most malignant tumors and the leading cause of cancer-related deaths worldwide. Among lung cancers, 40% are diagnosed as adenocarcinoma. Bromodomain containing 7 (BRD7) is a member of bromodomain-containing protein family. It was proved to be downregulated in various cancers. However, the role of BRD7 in lung adenocarcinoma is still unknown. Western blot and qRT-PCR wa...

متن کامل

BRD7: a novel tumor suppressor gene in different cancers.

BRD7 (bromodomain 7), also known as celtix-1, was first identified in nasopharyngeal carcinoma (NPC) cells in 2000. BRD7 is a crucial component of both functional p53 and BRCA1 (breast cancer 1, early onset) pathways. Recently, the BRD7 tumor suppressor status has been fully established. Previous studies demonstrated that BRD7 was downregulated in human breast cancer and the downregulation ofte...

متن کامل

Bromodomain-containing protein 7 (BRD7) as a potential tumor suppressor in hepatocellular carcinoma

Bromodomain-containing protein 7 (BRD7) is a subunit of the PBAF complex, which functions as a transcriptional cofactor for the tumor suppressor protein p53. Down-regulation of BRD7 has been demonstrated in multiple types of cancer. This study aimed to investigate BRD7 expression and its tumor suppressive effect in hepatocellular carcinoma (HCC).The expression of BRD7 was examined in clinical s...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Chemical communications

دوره 48 75  شماره 

صفحات  -

تاریخ انتشار 2012