Switch Control Kinase Inhibitor Platform

Our proprietary drug discovery switch-control kinase inhibitor platform is based on our deep insight into the biology of kinases. Our switch-control kinase inhibitors interact at a molecular level that is distinct from other kinase inhibitors and are designed to generate higher and more durable rates of response. Using our switch-control kinase inhibitor platform, we have developed a diverse pipeline of differentiated, wholly-owned, orally administered drug candidates.1

1 Development and commercialization exclusive license with Zai Lab in Greater China.

Deciphera

 

 

Kinase Activation: The process and mechanism of activation kinases

Kinases are molecular signaling proteins located within cells. Kinases direct the activity of other signaling proteins, including other kinases, to orchestrate the function of a variety of essential cellular processes.

A molecular control known as the activation switch governs whether the kinase is in the inactive “off switch” or the active “on switch”; enabling a high-level control of cellular processes. The transformation of a kinase from an inactive to an activated state is dependent upon the interaction of the activation switch with an area called the switch pocket; a mechanism of activation that is common among kinases. By directly targeting the switch pocket, we design inhibitors to be broadly active against the target kinase, covering both wild-type and known mutant or amplified forms.

How Our Switch-Control Kinase Inhibitor Platform Works

While this activation mechanism is common among kinases, the molecular structure of the activation switch and the switch pocket varies among kinases. At Deciphera, we take advantage of this variation to design molecules that inhibit a specific kinase or kinases.

Switch-control Kinase Inhibitors in Immunosuppressive Diseases

Step 1

Step 1

 A tumor appears in the body

Step 2

Step 2

A tumor sends a signal to an immune cell to activate a kinase and turn it to the on position

Step 3

Step 3

Deciphera’s switch-control kinase inhibitor is embedded tightly into the switch pocket of a kinase

Step 4

Step 4

The switch-control inhibitor prevents the tumor from suppressing the immune system, restoring its natural ability to attack the tumor

Switch-control Kinase Inhibitors in Drug Resistant Kinase Mutations

mutation step 1

Step 1

Mutations in kinases cause uncontrolled interaction of the kinase activation switch with the switch pocket

Mutation step 2

Step 2

This activates the kinase and leads to upregulation of kinase signaling, which drives cancer cell proliferation

Mutation step 3

Step 3

Deciphera’s switch-control kinase inhibitor binds both the switch pocket region and the activation loop to lock the kinase in an inactive state

Mutation step 4

Step 4

The switch-control kinase inhibitor secures the kinase into an inactive state, inhibiting downstream signaling and cancer cell proliferation

Yellow tube
Our Discovery Platform
Learn More
Pair of people
Potential Impact
Potential Impact