Reference Detail

Ref Type Journal Article
PMID (20509775)
Authors Dai Y
Title Platelet-derived growth factor receptor tyrosine kinase inhibitors: a review of the recent patent literature.
Journal Expert opinion on therapeutic patents
Vol 20
Issue 7
Date 2010 Jul
URL
Abstract Text Platelet-derived growth factor receptor (PDGFR) is a compelling target for developing therapeutic agents to treat diseases associated with overactivated platelet-derived growth factor (PDGF) signaling and has proved to be particularly encouraging for cancer treatment. The efforts in this area have been greatly enhanced by the approval of tyrosine kinase inhibitors with PDGFR inhibitory activity such as imatinib, sunitinib and sorafenib.This review surveys the small molecule PDGFR inhibitors reported in patent literature over the past 5 years (2005 - 2009).The reader will gain an overview of the chemical scaffolds and the activity/selectivity of the newly discovered PDGFR inhibitors.Targeting PDGFR kinase with small molecule inhibitors has remained a very active area. Many new and novel PDGFR inhibitors with different selectivity profiles are being discovered and evaluated. In cancer therapy, the identification of novel and potent PDGFR inhibitors with preferred kinase inhibitory profiles that deliver superior antitumor efficacy, yet have manageable side effects and toxicities, will continue to be the key for success. Additionally, interest in targeting PDGF signaling for intervention of various vascular diseases and fibrotic conditions is expected to continue to grow.

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

Sorting

  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

Molecular Profile Treatment Approach
PDGFRA N659K PDGFR Inhibitor (Pan)
PDGFRA C456_N468del PDGFR Inhibitor (Pan)
PDGFRA R841K PDGFR Inhibitor (Pan)
PDGFRA act mut PDGFR Inhibitor (Pan)
PDGFRA V561_I562insER PDGFR Inhibitor (Pan)
PDGFRA R748G PDGFR Inhibitor (Pan)
PDGFRA D842Y PDGFR Inhibitor (Pan)
PDGFRA V536E PDGFR Inhibitor (Pan)
PDGFRA E311_K312del PDGFR Inhibitor (Pan)
PDGFRA S566_E571delinsR PDGFR Inhibitor (Pan)
PDGFRA P577T PDGFR Inhibitor (Pan)
PDGFRA D846Y PDGFR Inhibitor (Pan)
PDGFRA D842_H845del PDGFR Inhibitor (Pan)
PDGFRA N659S PDGFR Inhibitor (Pan)
PDGFRA C450_K451insMIEWMI PDGFR Inhibitor (Pan)
PDGFRA P577S PDGFR Inhibitor (Pan)
PDGFRA D842_M844del PDGFR Inhibitor (Pan)
PDGFRA Y555C PDGFR Inhibitor (Pan)
PDGFRA H845Y PDGFR Inhibitor (Pan)
PDGFRA I843_M844del PDGFR Inhibitor (Pan)
PDGFRA C456_R481del PDGFR Inhibitor (Pan)
PDGFRA R841_D842delinsKI PDGFR Inhibitor (Pan)
PDGFRA H650Q PDGFR Inhibitor (Pan)
PDGFRA I843_D846del PDGFR Inhibitor (Pan)
PDGFRA D842V PDGFR Inhibitor (Pan)
PDGFRA N848K PDGFR Inhibitor (Pan)
PDGFRA Y849S PDGFR Inhibitor (Pan)
PDGFRA V544_L545insAVLVLLVIVIISLI PDGFR Inhibitor (Pan)
PDGFRA Y849C PDGFR Inhibitor (Pan)
PDGFRA H845_N848delinsP PDGFR Inhibitor (Pan)
PDGFRA V658A PDGFR Inhibitor (Pan)
PDGFRA M844_S847del PDGFR Inhibitor (Pan)
PDGFRA P345S PDGFR Inhibitor (Pan)
PDGFRA D842_D846del PDGFR Inhibitor (Pan)
PDGFRA Y288C PDGFR Inhibitor (Pan)
PDGFRA D842I PDGFR Inhibitor (Pan)
PDGFRA Y375_K455del PDGFR Inhibitor (Pan)
PDGFRA I843del PDGFR Inhibitor (Pan)
PDGFRA D842_I843delinsIM PDGFR Inhibitor (Pan)
PDGFRA V561D PDGFR Inhibitor (Pan)
PDGFRA amp PDGFR Inhibitor (Pan)
PDGFRA G853D PDGFR Inhibitor (Pan)
PDGFRA V561A PDGFR Inhibitor (Pan)
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References