DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors

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

Promiscuous Aggregate-Based Inhibitors Promote Enzyme Unfolding

One of the leading sources of false positives in early drug discovery is the formation of organic small molecule aggregates, which inhibit enzymes nonspecifically at micromolar concentrations in aqueous solution. The molecular basis for this widespread problem remains hazy. To investigate the mechanism of inhibition at a molecular level, we determined changes in solvent accessibility that occur...

متن کامل

Enzyme inhibitors for renin assay in rat plasma.

1. Degradation of 125I-labelled [Ile5]-angiotensin I and unlabelled angiotensin I was studied during incubation of rat plasma treated with disodium ethylenediaminetetra-acetate (disodium EDTA) at 37 degrees C, pH 6.5, for 1 h with 8-hydroxyquinoline, phenylmethylsulphonyl fluoride or di-isopropyl fluorophosphate. 2. Isoelectric focusing showed approximately 100, 59--66 and 10--31% preservation ...

متن کامل

High-throughput assays for promiscuous inhibitors.

High-throughput screening (HTS) searches large libraries of chemical compounds for those that can modulate the activity of a particular biological target; it is the dominant technique used in early-stage drug discovery. A key problem in HTS is the prevalence of nonspecific or 'promiscuous' inhibitors. These molecules have peculiar properties, act on unrelated targets and can dominate the result...

متن کامل

Development of a QPatch automated electrophysiology assay for identifying KCa3.1 inhibitors and activators.

The intermediate-conductance Ca(2+)-activated K(+) channel KCa3.1 (also known as KCNN4, IK1, or the Gárdos channel) plays an important role in the activation of T and B cells, mast cells, macrophages, and microglia by regulating membrane potential, cellular volume, and calcium signaling. KCa3.1 is further involved in the proliferation of dedifferentiated vascular smooth muscle cells and fibrobl...

متن کامل

Anucleate cell blue assay: a useful tool for identifying novel type II topoisomerase inhibitors.

About 95,000 compounds were screened by the anucleate cell blue assay. Fifty-one of the hit compounds had various structures and showed inhibitory activity against DNA gyrase and/or topoisomerase IV. Moreover, the compounds exhibited antibacterial activity against a fluoroquinolone- and novobiocin-resistant strain of Staphylococcus aureus. The anucleate cell blue assay is therefore a useful too...

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: ACS Medicinal Chemistry Letters

سال: 2019

ISSN: 1948-5875,1948-5875

DOI: 10.1021/acsmedchemlett.9b00093