Structure-based design for selective inhibition lowers toxicity

نویسندگان

چکیده

برای دانلود رایگان 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

Structure-guided design of purine-based probes for selective Nek2 inhibition

Nek2 (NIMA-related kinase 2) is a cell cycle-dependent serine/threonine protein kinase that regulates centrosome separation at the onset of mitosis. Overexpression of Nek2 is common in human cancers and suppression can restrict tumor cell growth and promote apoptosis. Nek2 inhibition with small molecules, therefore, offers the prospect of a new therapy for cancer. To achieve this goal, a better...

متن کامل

Structure-Based Design of Potent and Selective LeishmaniaN-Myristoyltransferase Inhibitors

Inhibitors of Leishmania N-myristoyltransferase (NMT), a potential target for the treatment of leishmaniasis, obtained from a high-throughput screen, were resynthesized to validate activity. Crystal structures bound to Leishmania major NMT were obtained, and the active diastereoisomer of one of the inhibitors was identified. On the basis of structural insights, enzyme inhibition was increased 4...

متن کامل

Selective butyrylcholinesterase inhibition elevates brain acetylcholine, augments learning and lowers Alzheimer beta-amyloid peptide in rodent.

Like acetylcholinesterase, butyrylcholinesterase (BChE) inactivates the neurotransmitter acetylcholine (ACh) and is hence a viable therapeutic target in Alzheimer's disease, which is characterized by a cholinergic deficit. Potent, reversible, and brain-targeted BChE inhibitors (cymserine analogs) were developed based on binding domain structures to help elucidate the role of this enzyme in the ...

متن کامل

A Variable Structure Observer Based Control Design for a Class of Large scale MIMO Nonlinear Systems

This paper fully discusses how to design an observer based decentralized fuzzy adaptive controller for a class of large scale multivariable non-canonical nonlinear systems with unknown functions of subsystems’ states. On-line tuning mechanisms to adjust both the parameters of the direct adaptive controller and observer that guarantee the ultimately boundedness of both the tracking error and tha...

متن کامل

Selective Toxicity

The eleven essays cover the following subjects: Inflammation and Tissue Injury, by Ward; Cellular Basis of Immunoglobulin Synthesis, by Mullinax; Immunoglobin Structure and Biological Implications, by Bennett; Molecular Aspects of Antigen-Antibody Binding as Related to the Initiation of Immunological Reactions, by Siskind and Levine; Complement Components, by Stroud; Complement and Its Role in ...

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: Nature Reviews Clinical Oncology

سال: 2013

ISSN: 1759-4774,1759-4782

DOI: 10.1038/nrclinonc.2013.1