ArticleNature chemical biology2016
Discovery of LRE1 as a specific and allosteric inhibitor of soluble adenylyl cyclase.
Article in Nature chemical biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
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Who cites it
54 citing papers in PubMed, 87 citations in OpenAlex.
- Targeting Soluble Adenylyl Cyclase for On-Demand Contraception.Physiology (Bethesda, Md.) · 2026Review
- Physiological basis of contraceptive function of a GSK3α-selective inhibitor, manifested during epididymal sperm maturation.Molecular human reproduction · 2026Article
- Assessing efficacy of ADCY10 inhibitors in cervical mucus.Molecular human reproduction · 2026Article
- Soluble adenylyl cyclase in nonmammalian sperm is directly controlled by pH, not by HCOProceedings of the National Academy of Sciences of the United States of America · 2026Article
- Chemical biology approaches to resolve the subcellular GPCR signaling landscape.Nature chemical biology · 2025Review
- Obesity-driven oleoylcarnitine accumulation in tumor microenvironment promotes breast cancer metastasis-like phenotype.Acta pharmaceutica Sinica. B · 2025Article
- Cyclic AMP Rescue of Motility in Sperm Devoid of Soluble Adenylyl Cyclase.International journal of molecular sciences · 2025Article
- David Garbers and the Birth of cAMP Biology in Mammalian Sperm.Molecular reproduction and development · 2024Review
- The compound YK 3-237 promotes pig sperm capacitation-related events.Veterinary research communications · 2024Article
- The role of soluble adenylyl cyclase in sensing and regulating intracellular pH.Pflugers Archiv : European journal of physiology · 2024Review
- Rosmarinic Acid Present inPlants (Basel, Switzerland) · 2024Article
- Two novel heterozygousJournal of genetics · 2024Review
- Article
- Male contraception: narrative review of ongoing research.Basic and clinical andrology · 2023Review
- Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells.Cell reports · 2023Article
- Scaffold Hopping and Optimization of Small Molecule Soluble Adenyl Cyclase Inhibitors Led by Free Energy Perturbation.Journal of chemical information and modeling · 2023Article
- On-demand male contraception via acute inhibition of soluble adenylyl cyclase.Nature communications · 2023Article
- Soluble cyclase-mediated nuclear cAMP synthesis is sufficient for cell proliferation.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Review
- Article
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Authors and funding
16 authors at 5 institutions in 2 countries.
Funding
Abstract
The prototypical second messenger cAMP regulates a wide variety of physiological processes. It can simultaneously mediate diverse functions by acting locally in independently regulated microdomains. In mammalian cells, two types of adenylyl cyclase generate cAMP: G-protein-regulated transmembrane adenylyl cyclases and bicarbonate-, calcium- and ATP-regulated soluble adenylyl cyclase (sAC). Because each type of cyclase regulates distinct microdomains, methods to distinguish between them are needed to understand cAMP signaling. We developed a mass-spectrometry-based adenylyl cyclase assay, which we used to identify a new sAC-specific inhibitor, LRE1. LRE1 bound to the bicarbonate activator binding site and inhibited sAC via a unique allosteric mechanism. LRE1 prevented sAC-dependent processes in cellular and physiological systems, and it will facilitate exploration of the therapeutic potential of sAC inhibition.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.