Got this from a friend (thanks, Mike). Being downstream in the signaling pathway lends greater specificity. On the other hand, Sugen is talking lead optimization, rather than just a patent on the target. That doesn't mean, of course, that REGN hasn't nailed leads for MAP kinase or that it is not desireable to block both the MAP kinase and RAS pathways.
Rick
SUGEN receives patent on the cancer target GRB2
Key target for many pharmaceutical and biotechnology R&D programs
REDWOOD CITY, Calif.--(BW HealthWire)--April 8, 1997-- Sugen Inc today
announced that the United
States Patent and Trademark Office has issued Patent No. 5618619 on SUGEN's
proprietary cancer target
GRB2. SUGEN regards its GRB2 inhibitor program as an important part of its
cancer drug development
pipeline, and therefore intends to enforce vigorously its intellectual
property rights with respect to the GRB2
target, as well as related to claims still in process.
GRB2 is a non-enzymatic protein that bridges the signalling between
Tyrosine Kinase receptors (TKs) and
the RAS signalling cascade. This is accomplished through the interaction of
GRB2 with tyrosine
phosphorylation sites on TKs or other proteins through a domain called the
SH2 domain (src homology 2
domain). GRB2 inhibitors block the ability of oncogenic growth factor
receptors to activate the RAS and
MAP kinase signalling pathways. These pathways are known to be important in
tumor cell transformation
and growth.
Joseph Schlessinger, Ph.D., Chairman of the Department of Pharmacology at
New York University
Medical Center and a scientific co-founder of SUGEN, was the first to
discover the GRB2 protein and
certain other SH2-containing proteins that participate in signal
transduction in mammalian cells. Dr.
Schlessinger's laboratory and studies at SUGEN led by Mikhail Gishizky,
Ph.D., Director of Cell Biology,
have confirmed GRB2 as a key player in signal transduction by using methods
including the use of
dominant-negative mutants of GRB2. These studies have validated this
protein as an important target for
therapeutic intervention in the treatment of cancer.
SUGEN's GRB2 Project
SUGEN has identified small molecule inhibitors that block the binding of
GRB2 to sites of tyrosine
phosphorylation on TKs and other proteins. The Company has found that by
specifically blocking this
interaction, these inhibitors can lead to arrest of the growth of tumor
cells in the G1 phase of the cell cycle,
or apoptosis (programmed cell death), depending upon the system examined.
In addition, the Company has
found that such compounds can inhibit the subcutaneous growth of tumor
cells in animal models.
Currently, SUGEN is in the process of optimizing lead compounds for
potency, safety and pharmacokinetic
characteristics. If this program progresses satisfactorily, SUGEN currently
anticipates that it will select a
GRB2 IND candidate in the second half of 1997.
SUGEN, Inc. is a biopharmaceutical company focusing on the development of
new classes of small
molecule drugs which interact in a specific manner with different members
of the tyrosine kinase, tyrosine
phosphatase and serine-threonine kinase families of signal transduction
molecules, and their signalling
pathways. These pathways are involved in a number of human diseases
including cancer and diabetes, as
well as disorders of the body's immune defenses and neurological systems.
The Company has research and
development collaborations with Zeneca, ASTA Medica and Allergan.
This press release contains, in addition to historical information,
forward-looking statements that involve
risks and uncertainties. The Company's actual results could differ
significantly from the results discussed in
the forward-looking statements. Factors that could cause or contribute to
such differences include the
Company's ability to demonstrate the safety and efficacy of GRB2 in the
time period described in the press
release and other factors more fully discussed in the Company's 1996 Form
10-K. The Company
undertakes no obligation to release the results of any revision to these
forward-looking statements which
may be made to reflect events or circumstances occurring after the date
hereof or to reflect the occurrence of
unanticipated events.
Additional written materials and press releases regarding SUGEN are
available through the SUGEN
Fax-On-Demand Information Service by dialing 1-888-329-4699.
CONTACT: SUGEN, Inc.
Nina W. Ferrari, 415/306-7700
IRDEPT@SUGEN.SF.CA.US |
