Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Small molecule somatostatin receptor subtype-2 antagonists.

B A Hay1, B M Cole, F M DiCapua

  • 1Global Research and Development, Groton Laboratories, Pfizer Inc, Eastern Pt. Road, Groton, CT 06340-5146, USA. bruce_a_hay@groton.pfizer.com

Bioorganic & Medicinal Chemistry Letters
|October 10, 2001
PubMed
Summary

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Montreal Veterinary Medical Association.

The Journal of comparative medicine and veterinary archives·2022
Same author

Occupational asthma in office workers.

Occupational medicine (Oxford, England)·2022
Same author

Occupational asthma caused by peracetic acid-hydrogen peroxide mixture.

Occupational medicine (Oxford, England)·2019
Same author

Periungual thumb papule on a 62-year-old man.

Clinical and experimental dermatology·2019
Same author

Cleaning agent occupational asthma in the West Midlands, UK: 2000-16.

Occupational medicine (Oxford, England)·2018
Same author

Asbestosis is prevalent in a variety of construction industry trades.

NPJ primary care respiratory medicine·2018

Researchers developed the first potent small molecule somatostatin receptor type 2 (sst2) antagonists. These novel compounds exhibit high binding affinity and full antagonist activity, offering new therapeutic possibilities.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry

Background:

  • Somatostatin receptor type 2 (sst2) plays a crucial role in various physiological processes.
  • Development of selective sst2 antagonists is of therapeutic interest.

Purpose of the Study:

  • To report the discovery of the first potent small molecule antagonists targeting the sst2 receptor.
  • To characterize the binding affinity and functional activity of novel sst2 antagonist compounds.

Main Methods:

  • Structure-activity relationship studies were performed on known sst2 agonist molecules.
  • Binding affinity was assessed by measuring the displacement of radiolabeled somatostatin.
  • Functional antagonist activity was determined by measuring the inhibition of somatostatin-induced signaling.

Related Experiment Videos

Main Results:

  • Novel small molecules with high binding affinity for the sst2 receptor were synthesized.
  • Compounds demonstrated full antagonist activity, effectively blocking somatostatin's action.
  • Compound 7a showed potent sst2 receptor antagonism with an IC(50) of 2.9 nM for binding and 29 nM for functional activity.

Conclusions:

  • The first potent small molecule sst2 antagonists have been successfully developed.
  • These antagonists represent promising new chemical entities for further investigation in sst2-related conditions.
  • The findings open avenues for novel therapeutic strategies targeting the sst2 receptor pathway.