ACADIA Discovers Novel Small Molecule Leads for the V2 Vasopressin Receptor
Chemical-Genomics Platform Enables Discovery of Small Molecule Activators Of Numerous Peptide GPCRs
2002-09-26 00:01 (New York)
SAN DIEGO and COPENHAGEN, Denmark, Sept. 26 /PRNewswire/ --
ACADIA Pharmaceuticals announced today the discovery of small molecule lead
chemistries for the V2 Vasopressin receptor. The V2 Vasopressin receptor is
the major control mechanism for the production of urine. Activation of this
receptor by ACADIA's lead compounds resulted in a sustained decrease in urine
production in preclinical animal models.
"While V2 peptides that require injection or nasal application have long
been used to treat diabetes insipidus, bleeding disorders, and nocturnal
uresis (bed wetting), an orally active drug may address much broader markets,
potentially including incontinence," said Bo-Ragnar Tolf, Ph.D., ACADIA's Vice
President of Chemistry. "ACADIA's small non-peptide molecules have very
attractive drug characteristics and provide us with the potential to develop
the first oral medication that targets V2."
ACADIA's proprietary V2 chemistry is a product of its chemical-genomics
efforts. ACADIA is using functional assays to broadly screen the members of
the nuclear and G-protein coupled receptor ("GPCR") families, searching for
novel chemistries that act as agonist, antagonists, and inverse agonists.
More than 100 of these targets have been screened, with novel chemistries
identified for more than 70 targets. The V2 small molecule chemistry is an
example of a non-peptide activator of a peptide hormone receptor.
"V2 is just one of the examples where we have found exciting small
molecules that activate peptide GPCRs," said Mark R. Brann, Ph.D., ACADIA's
President and CSO. "In the upcoming issue of the Journal of Medicinal
Chemistry, we report the structure of our small molecule activator of the
Urotensin-II receptor, another peptide hormone receptor. We have also
discovered the first small molecule activators of the PAR-2 receptor. Our
proven ability to consistently discover the first small molecule activators of
peptide receptors runs in the face of the pharmaceutical dogma that holds that
peptide receptors require complex chemistries that mimic the structure of the
natural hormones. The latter are often referred to as peptoids. Our unique
small molecule chemistries have obvious commercial advantages in terms of
bioavailability and future synthetic opportunities relative to the peptides
and peptoids."
ACADIA is a drug discovery and development company that efficiently
discovers small molecule drug candidates using its proprietary
chemical-genomics platform. ACADIA's uniquely productive platform integrates
genomics, chemistry and biology to rapidly identify and validate drug targets
while simultaneously discovering chemistries specific to those targets.
ACADIA has successfully applied its chemical-genomics platform to generate a
broad discovery pipeline that includes advanced programs directed at major
diseases, including psychosis, chronic pain, and glaucoma. ACADIA's corporate
headquarters as well as its genomics and biological research facilities are
located in San Diego, California and its chemistry research facilities are
located in Copenhagen, Denmark.
For further information, please contact: in the United States, Douglas E.
Richards, VP of Business Development of ACADIA Pharmaceuticals,
+1-858-558-2871; or in Europe, Bo-Ragnar Tolf, Ph.D., VP of Chemistry and
Managing Director of ACADIA Pharmaceuticals A/S, +45-4329-3000. |
