ArticleBioorganic & medicinal chemistry2020
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.
Article in Bioorganic & medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 24 citations in OpenAlex.
- Effects of selected alkaloids on postnatal neurogenesis - in vivo and in vitro studies - literature review.Psychopharmacology · 2025Review
- Multifaced Nature of Yohimbine-A Promising Therapeutic Potential or a Risk?International journal of molecular sciences · 2024Review
- Article
- Chloroformate-mediated ring cleavage of indole alkaloids leads to re-engineered antiplasmodial agents.Organic & biomolecular chemistry · 2024Article
- A literature perspective on the pharmacological applications of yohimbine.Annals of medicine · 2022Review
- Anticancer potential of yohimbine in drug-resistant oral cancer KB-ChR-8-5 cells.Molecular biology reports · 2022Article
- Review
- Stationed or Relocating: The Seesawing EMT/MET Determinants from Embryonic Development to Cancer Metastasis.Biomedicines · 2021Review
- Ring Distortion of Vincamine Leads to the Identification of Re-Engineered Antiplasmodial Agents.ACS omega · 2021Article
- Synthesis of Conformationally Liberated Yohimbine Analogues and Evaluation of Cytotoxic Activity.ACS omega · 2021Article
- Limonin as a Starting Point for the Construction of Compounds with High Scaffold Diversity.Angewandte Chemie (International ed. in English) · 2021Article
- Yohimbine Ameliorates Temporomandibular Joint Chondrocyte Inflammation with Suppression of NF-κB Pathway.Inflammation · 2021Article
- Re-engineering natural products to engage new biological targets.Natural product reports · 2020Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
G protein-coupled receptors (GPCRs) constitute the largest protein superfamily in the human genome. GPCRs play key roles in mediating a wide variety of physiological events including proliferation and cancer metastasis. Given the major roles that GPCRs play in mediating cancer growth, they present promising targets for small molecule therapeutics. One of the principal goals of our lab is to identify complex natural products (NPs) suitable for ring distortion, or the dramatic altering of the inherently complex architectures of NPs, to rapidly generate an array of compounds with diverse molecular skeletal systems. The overarching goal of our ring distortion approach is to re-program the biological activity of select natural products and identify new compounds of importance to the treatment of disease, such as cancer. Described herein are the results from biological screens of diverse small molecules derived from the indole alkaloid yohimbine against a panel of GPCRs involved in various diseases. Several analogues displayed highly differential antagonistic activities across the GPCRs tested. We highlight the re-programmed profile of one analogue, Y7g, which exhibited selective antagonistic activities against AVPR2 (IC
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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.