Institution
ACADIA Pharmaceuticals Inc.
Company•San Diego, California, United States•
About: ACADIA Pharmaceuticals Inc. is a company organization based out in San Diego, California, United States. It is known for research contribution in the topics: Pimavanserin & Receptor. The organization has 260 authors who have published 276 publications receiving 8418 citations.
Papers published on a yearly basis
Papers
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TL;DR: The synthesis of optically active piperidines by enantioselective addition of aryl Grignard reagents to pyridine N-oxides and lithium binolate followed by reduction is reported for the first time.
25 citations
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TL;DR: It is shown that the human angiotensin AT(1) receptor signals directly through G protein-independent pathways and supports NIH3T3 cellular proliferation, which has clear pharmacological implications for development of drugs with pathway-specific actions and defined biological outcomes.
25 citations
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TL;DR: Allosteric agonists differ from orthosteric ligands and among each other in their ability to induce different regulatory pathways are ligand specific, indicating that signaling and regulatory pathways induced by different allostericligands areligand specific.
Abstract: Background
Activation of muscarinic M1 receptors is mediated via interaction of orthosteric agonists with the acetylcholine binding site or via interaction of allosteric agonists with different site(s) on the receptor. The focus of the present study was to determine if M1 receptors activated by allosteric agonists undergo the same regulatory fate as M1 receptors activated by orthosteric agonists.
25 citations
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TL;DR: The synthesized compounds seem to be selective for the UII receptor as no activities were observed at the closely related SSTR3 and 5 receptors.
24 citations
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TL;DR: Low-molecular-weight compounds that specifically and with high potency inhibit the interaction between CD80 and CD28 are identified and serve as promising starting points for further development of CD80 inhibitors as potential immunomodulatory drugs.
Abstract: Protein-protein interactions are widely found in biological systems controlling diverse cellular events. Because these interactions are implicated in many diseases such as autoimmunity and cancer, regulation of protein-protein interactions provides ideal targets for drug intervention. The CD80-CD28 costimulatory pathway plays a critical role in regulation of the immune response and thus constitutes an attractive target for therapeutic manipulation of autoimmune diseases. The objective of this study is to identify small compounds disrupting these pivotal protein-protein interactions. Compounds that specifically blocked binding of CD80 to CD28 were identified using a strategy involving a cell-based scintillation proximity assay as the initial step. Secondary screening (e.g., by analyzing the direct binding of these compounds to the target immobilized on a biosensor surface) revealed that these compounds are highly selective CD80 binders. Screening of structurally related derivatives led to the identification of the chemical features required for inhibition of the CD80-CD28 interaction. In addition, the optimization process led to a 10-fold increase in binding affinity of the CD80 inhibitors. Using this approach, the authors identify low-molecular-weight compounds that specifically and with high potency inhibit the interaction between CD80 and CD28. These compounds serve as promising starting points for further development of CD80 inhibitors as potential immunomodulatory drugs.
24 citations
Authors
Showing all 261 results
Name | H-index | Papers | Citations |
---|---|---|---|
Michael Bachmann | 63 | 360 | 14388 |
Daniel P. van Kammen | 47 | 168 | 6957 |
Kristina Luthman | 39 | 158 | 7344 |
Fredrik Almqvist | 37 | 170 | 4219 |
Mark R. Brann | 35 | 77 | 5579 |
Roger Olsson | 30 | 138 | 2752 |
Uli Hacksell | 29 | 99 | 2954 |
Torbjörn Frejd | 29 | 165 | 2889 |
Petrine Wellendorph | 27 | 83 | 2573 |
Ethan S. Burstein | 27 | 70 | 2255 |
David M. Weiner | 26 | 45 | 3230 |
Kimberly E. Vanover | 25 | 70 | 1955 |
Uli Hacksell | 25 | 129 | 2879 |
Magnus Gustafsson | 25 | 94 | 1546 |
Mark R. Brann | 24 | 39 | 2576 |