Wednesday February 16, 10:27 am Eastern Time
Company Press Release
SOURCE: Guilford Pharmaceuticals Inc.
Guilford Licenses Novel Discovery From Johns Hopkins
University
New Biological Target, Serine Racemase, May be Useful for the Treatment of Degenerative
Disorders
BALTIMORE, Feb. 16 /PRNewswire/ -- Guilford Pharmaceuticals Inc. (Nasdaq: GLFD - news) today announced that it has
licensed a discovery from the Johns Hopkins University relating to a unique biological target, serine racemase, that could be
used to develop treatments for neurodegenerative diseases.
``This is an exciting discovery because serine racemase represents a novel way to potentially block the harmful effects of
glutamate over-stimulation,' remarked Dr. Solomon H. Snyder, Director of Neuroscience at the Johns Hopkins University
School of Medicine.
Glutamate's Role in Degenerative Disorders
The overproduction of glutamate has been implicated in a large number of acute and chronic degenerative conditions including
stroke, epilepsy, peripheral neuropathies, chronic pain and Parkinson's, Alzheimer's and Huntington's disease.
Glutamate is one of the most abundant amino acids in the body. It is found both in the peripheral and central nervous system
and controls many important functions. During stroke and other degeneration conditions, however, excessive glutamate is
released, which is highly toxic to neurons. Scientists believe that the harmful effects of excessive glutamate occur principally
through activation of a subtype of the glutamate receptor called the NMDA receptor.
The Role and Activity of Serine Racemase & D-Serine
NMDA receptors have not one, but two sites that must be activated in order for neurotransmission to take place. Scientists
formerly thought that the amino acid, glycine, working in tandem with glutamate, was the sole activator of this site. Recently,
however, scientists at Johns Hopkins, led by Dr. Snyder, discovered that the D-isomer of the amino acid, serine (D-serine),
was the principal activator of this site. Dr. Snyder's lab was responsible for isolating and cloning the enzyme, serine racemase,
which converts the L-isomer to the D-isomer.
``Since glutamate is so abundant in our bodies, nature developed a failsafe mechanism to prevent over-excitation of NMDA
receptors by glutamate. It's very much like a lock that requires two separate keys. We discovered that D-serine, acting in
tandem with glutamate, is required for NMDA activation,' explained Dr. Snyder.
This finding suggested that D-serine plays an important regulatory role in the neurotoxic cascade which contributes to cell injury
and cell death, and that it accomplishes this by acting as a check on glutamate.
``This discovery provides us with an interesting new biological target for drug development, since small molecule inhibitors of
serine racemase could be anticipated to prevent glutamate neurotoxicity in conditions like stroke and other neurodegenerative
conditions,' continued Dr. Snyder.
These findings were recently published in the November 9, 1999 issue of the Proceedings of the National Academy of
Sciences.
Building a Neuroprotectant Franchise
Previous therapeutic approaches have focused on blocking glutamate's ability to bind at the NMDA receptor site, however,
these approaches have been associated with deleterious side effects in clinical studies. In contrast, Guilford's NAALADase
inhibitor program focuses on blocking excessive glutamate pre-synaptically. Similarly, the identification and cloning of serine
racemase expands and complements Guilford's existing neuroprotectant franchise by presenting an additional opportunity to
explore novel ways of blocking glutamate over-stimulation.
As part of the company's agreement with Johns Hopkins, Guilford has obtained an exclusive license covering the rights to this
discovery and its corresponding intellectual property. In addition, Guilford acquired a proprietary screening system to identify
novel inhibitors of serine racemase.
``The over-stimulation of NMDA receptors by glutamate is believed to be an important initial pathologic event in stroke and
several neurodegenerative diseases. Finding an alternative method of blocking glutamate activation of the NMDA receptor --
by selectively blocking the synthesis of D-serine -- could potentially offer new treatment alternatives for conditions like stroke
and chronic degenerative disorders like Parkinson's and Alzheimer's disease,' remarked Dr. Peter Suzdak, Senior Vice
President of Research and Development at Guilford. ``We are excited about pursuing this novel approach as part of our
neuroprotectant research and development program.'
Guilford Pharmaceuticals Inc. is a biopharmaceutical company engaged in the development of polymer-based therapeutics for
cancer, and novel products for the diagnosis and treatment of neurological diseases, including Parkinson's disease, Alzheimer's
disease, stroke, severe head trauma, spinal cord injuries, multiple sclerosis, and peripheral neuropathies.
This press release contains forward-looking statements that involve risks and uncertainties that could cause Guilford's actual
results and experience to differ materially from the anticipated results and expectations expressed in these forward-looking
statements, including those described in the section entitled ``Risk Factors' contained in the Company's Registration Statement
on Form S-3 (file no. 333-8709) filed with the Securities Exchange Commission on September 14, 1999, and in other filings
with the Securities and Exchange Commission. Among other things, there can be no assurance that compounds targeting serine
racemase will successfully complete all the preclinical, clinical, regulatory, manufacturing and other steps necessary to develop
and commercialize them into safe and effective new drugs.
SOURCE: Guilford Pharmaceuticals Inc.
biz.yahoo.com
Sounds good.
Jack |
