Scrip is part of Informa PLC

This site is operated by a business or businesses owned by Informa PLC and all copyright resides with them. Informa PLC’s registered office is 5 Howick Place, London SW1P 1WG. Registered in England and Wales. Number 8860726.

This copy is for your personal, non-commercial use. For high-quality copies or electronic reprints for distribution to colleagues or customers, please call +44 (0) 20 3377 3183

Printed By

UsernamePublicRestriction
UsernamePublicRestriction

Teasing Out Mechanisms of Small-Molecule Kinase Inhibition

This article was originally published in Start Up

Executive Summary

Even as kinases remain a popular target in oncology for industry, two recent papers show how much we have yet to learn about how to interfere with these molecules. These most recent laboratory studies help explain the confusing observation that the very act of inhibiting a kinase with a drug can also "prime" phosphorylation of that target, which in some cases can actually enhance tumor activity.

You may also be interested in...



A Study in RAF: On-Target Effects Can be Surprisingly Fickle

Two independent research teams have shown that current RAF inchibitors, a class of experimental targeted cancer drugs, may only work well in patients with one particular mutation - in an enzyme called BRAF. In other people, the drugs can actually contribute to the growth of tumors. The findings echo develoments earlier in the decade with EGFr inhibitors, which proved to be harmful to some patients until the mechanism of action was worked out and their use subsequently restricted.

For Cancer Therapy, Radiation Protection and Delayed Tumor Growth from the Same Mechanism

A group at the National Cancer Institute has shown that blocking the activity of the glycoprotein thrombospondin-1 protects surrounding tissue from the effects of ionizing radiation while, at the same time, sensitizing tumor cells to the effects of the radiation blast. The work could lead to new adjunctive cancer therapies--especially in breast cancer, to ablate residual tumor cells following reconstructive surgery.

Combining Chemical Genetics and Cancer Immunotherapy

Two years ago, a team at Stanford described a new "chemical genetics" technique--a more precise way to use small molecules to perturb gene products and living systems. Now they have published more data on the system. And of acute interest to drug developers, they have linked the work to therapeutic applications in cancer immunotherapy, showing the ability to regulate secreted proteins such as IL-2 and TNF.

Related Content

Topics

Related Companies

Related Deals

UsernamePublicRestriction

Register

SC091817

Ask The Analyst

Please Note: Click here for more information on the Ask the Analyst service.

Your question has been successfully sent to the email address below and we will get back as soon as possible. my@email.address.

All fields are required.

Please make sure all fields are completed.

Please make sure you have filled out all fields

Please make sure you have filled out all fields

Please enter a valid e-mail address

Please enter a valid Phone Number

Ask your question to our analysts

Cancel