Glossary

A B C D E F G H I J K L M N O P Q R S T U V W X Y Z

A

ADAM-10

A member of the family of matrix metalloproteases (MMPs) that may play a role in cell migration and tumor metastasis

Akt

Also known as protein kinase B (PKB). Akt is a protein that plays a critical role in regulating cell growth and death, and is implicated in some of the most common human cancers

Angiogenesis

The process of forming new blood vessels

C

Chk Kinase

Chk1 and Chk2 are two kinases that block cell cycle progression in the presence of DNA damage, enabling DNA repair to occur. The signaling pathways activated by Chk1 and Chk2 play an important role in resistance of tumors to chemotherapy

E

EGFR

Epidermal growth factor receptor. EGFR plays an important role in the growth and proliferation of many cancer cells

F

FGFR

Fibroblast growth factor receptor. FGFR plays an important role in cancer cell proliferation and contributes to the development or stabilization of new tumor vasculature.

Flt3

FMS-like tyrosine kinase type 3. Flt3 is an RTK that plays a role in the survival, proliferation and maturation of blood precursor cells

Fungicide

A substance that is toxic to fungi (yeasts and molds); typically used to protect crops from fungal infections

H

HER2

Human epidermal growth factor type 2. HER2 plays an important role in the growth and proliferation of several cancers, including breast, prostate and ovarian cancer

Herbicide

A substance that is toxic to plants; typically used to control the growth of unwanted plant species

I

IGF1R

Insulin-like growth factory type 1 receptor, plays a role in cell growth and proliferation

Investigational New Drug

A new drug, antibiotic drug, or biological drug that is used in a clinical investigation.

Investigational New Drug Application (IND)

An application submitted to the U.S. Food and Drug Administration to request authorization to initiate human
clinical trials.

J

JAK2

Janus kinase 2. JAK2 is activated by a variety of cytokines and growth factors, and plays an important role in cancer cell survival, proliferation, differentiation and migration. Activating mutations of JAK2 occur frequently in a variety of myeloproliferative disorders and JAK2 signaling is upregulated in several types of lymphoma and solid tumors.

K

Kinase

An enzyme that modulates the activity of other proteins through the addition of phosphate groups

KIT

Also known as stem cell factor receptor, An oncogene associated with the growth of certain cancers

KDR

Type 2 vascular endothelial growth factor receptor

M

Matrix Metalloprotease (MMP)

A family of proteins that are activated by binding Zinc, and catalyze the cleavage of a variety of growth factors, cell adhesion molecules and inhibitory proteins. MMPs are implicated in the proliferation, survival and migration of normal and cancer cells.

MEK

Mitogen activated protein kinase (MAPK)/extracellular signal-related kinase (ERK) kinase. MEK is a component of the RAS/RAF/MEK/ERK kinase signaling pathway. This pathway is frequently activated in human tumors and is required for transmission of growth-promoting signals from numerous receptor tyrosine kinases.

Met

An oncogene that also plays a role in blood coagulation and angiogenesis; also known as hepatocyte growth factor.

mTOR

Mammalian target of rapamycin. mTOR is frequently activated in human tumors and plays a central role in tumor cell growth.

O

Oncogene

A gene that normally directs cell growth. If altered, an oncogene can promote or allow the uncontrolled growth of cancer. Alterations can be inherited or caused by an environmental exposure to cancer-causing agents.

P

Pathway

A series of genes or proteins that are activated sequentially to convert a molecular stimulus into a change in cell function or activity

PDGFR

Platelet-derived growth factor receptor. Activation of PDGFR regulates several pathways, including migration and proliferation of fibroblasts, smooth muscle cells and some immune cells, and activation of inflammatory processes.

Pharmacokinetics

The processes (in a living organism) of absorption, distribution, metabolism, and excretion of a drug or vaccine.

Phase I Trials

Initial studies to determine how drugs are circulated, absorbed and cleared from the body in humans, the side effects associated with increasing doses, and to gain early evidence of effectiveness; may include healthy participants and/or patients.

Phase II Trials

Controlled clinical studies conducted to evaluate efficacy of the drug for a particular disease in patients and to determine the common short-term side effects and risks associated with the drug.

Phase III Trials

Expanded controlled and uncontrolled trials intended to generate additional information about overall, efficacy and benefit-risk relationship of the drug and to support product approval and labeling.

PI3K

Phosphoinositide-3-kinase. Activation of the PI3K pathway is a frequent event in human tumors, promoting cell growth, survival and resistance to chemotherapy and radiotherapy.

R

RAF

An oncogene that is activated in one-third of human cancers

RET

The REarranged during Transfection gene is a receptor tyrosine kinase. RET is mutationally activated in hereditary forms of medullary thyroid cancer and in sporadic forms of both medullary and papillary thyroid cancer.

Receptor Tyrosine Kinase (RTK)

A class of cellular receptors that modify the amino acid tyrosine in target proteins, leading to the activation of signaling pathways inside the cell.

S

Spectrum Selective Kinase Inhibitor® (SSKI)

A class of compounds that optimally inhibit the activity of multiple disease-related proteins simultaneously.
Because kinases are important in the growth and spread of cancer cells, SSKIs may help to kill or inhibit the
growth of cancer.

T

Target

A gene or protein whose activity can be modulated for therapeutic effect

T790M mutation

The T790M mutation is an EGFR mutation that is associated with resistance to EGFR inhibitors such as erlotinib and gefitinib. In preclinical studies, XL647 effectively inhibits the activity of the T790M mutant form of EGFR.

V

VEGFR

Vascular endothelial growth factor receptor. VEGFR plays a critical role in the process of new blood vessel formation (angiogenesis)

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For more information on cancer, please visit the National Cancer Institute's web site at: http://www.cancer.gov

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