Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

نویسندگان
چکیده

برای دانلود باید عضویت طلایی داشته باشید

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

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Irreversible protein kinase inhibitors: balancing the benefits and risks.

■ INTRODUCTION In the relatively young but expanding field of irreversible kinase inhibitor drug discovery, there are two main developments that are of central importance. First, the patients have watched the first wave of low molecular weight protein kinase inhibitors becoming available to them over the past decade. These kinase inhibitors have been approved by the U.S. Food and Drug Administr...

متن کامل

Structural bioinformatics-based design of selective, irreversible kinase inhibitors.

The active sites of 491 human protein kinase domains are highly conserved, which makes the design of selective inhibitors a formidable challenge. We used a structural bioinformatics approach to identify two selectivity filters, a threonine and a cysteine, at defined positions in the active site of p90 ribosomal protein S6 kinase (RSK). A fluoromethylketone inhibitor, designed to exploit both se...

متن کامل

Endogenous Protein Kinase Inhibitors

A thermostable inhibition of ATP:protein phosphotransferase (EC 2.7.1.37) (protein kinase) which is present in crude tissue extracts has been resolved by gel chromatography (Sephadex G-100) into two molecular forms. These two forms will be referred to as type I and type II inhibitor. The type I inhibitor (M, = 24,000) is specific for CAMP-dependent protein kinase and corresponds to the inhibito...

متن کامل

New protein kinase inhibitors.

Background: The stomach is an infrequent site of breast cancer metastasis. It may prove very difficult to distinguish a breast cancer metastasis to the stomach from a primary gastric cancer on the basis of clinical, endoscopic, radiological and histopathological features. It is important to make this distinction as the basis of treatment for breast cancer metastasis to the stomach is usually wi...

متن کامل

Monitoring of protein kinase inhibitors

Several mechanisms may influence the enhanced glucose uptake in cancer cells, including upregulation of glucose transporters, increase in the hexokinase activity and the protein kinase B, also called Akt, which appears to play key role in the control of glucose metabolism together with proteins which are involved in the signal cascade pathway, such as the mammalian target of rapamycin (mTOR). I...

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

ژورنال

عنوان ژورنال: Chemistry & Biology

سال: 2013

ISSN: 1074-5521

DOI: 10.1016/j.chembiol.2012.12.006