Dergiler / Turkish Journal of Biology / 2021 / Cilt: 45 - Sayı: 5

Screening of the small molecule library of Meinox enables the identification of anticancer compounds in pathologically distinct cancers

Sayfa
633–643
Yayın Tarihi
2022-10-17
DOI
—
🏛️Bu makalenin bibliyografik verileri ve tam metin bağlantısı DergiPark üzerinden sağlanmıştır.
DergiPark Kaydı ↗
✨

Yapay Zeka Hızlı Bakış & Çıkarımlar

AI Insight
⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

This study shows that in vitro analysis of different cancers or other phenotypic assays with Meinox small molecule library may generate novel and potent bioassay-specific compounds.

📌 3 Maddede Bu Makale

🎯
Amaç & Hipotez:Small molecules are widely used for the modulation of the molecular basis of diseases.
📊
Temel Bulgular & Veri:We have shown that most small molecules have molecular weights less than 450.
💡
Sonuç & Katkı:This study shows that in vitro analysis of different cancers or other phenotypic assays with Meinox small molecule library may generate novel and potent bioassay-specific compounds.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Alan Parametreleri

Abstract

Small molecules are widely used for the modulation of the molecular basis of diseases. This makes them the perfect tool for discovering and developing new therapeutics. In this work, we have established a library of small molecules in house and characterized its molecular and druglike properties. We have shown that most small molecules have molecular weights less than 450. They have pharmaceutically relevant cLogP, cLogS, and druglikeness value distributions. In addition, Meinox’s small molecule library contained small molecules with polar surface areas that are less than 60 square angstroms, suggesting their potent ability to cross the bloodbrain barrier. Meinox’s small molecule library was also tested in vitro for pathologically distinct forms of cancer, including pancreatic adenocarcinoma PANC1, breast carcinoma MCF7, and lymphoblastic carcinoma RS4-11 cell lines. Analysis of this library at a dose of 1 μM allowed the discovery of potent, specific or broadly active anticancer compounds against pathologically distinct cancers. This study shows that in vitro analysis of different cancers or other phenotypic assays with Meinox small molecule library may generate novel and potent bioassay-specific compounds.

🔖

Bu Makaleye Atıf Yap

MERMER, A., MAMMADOVA, A., KOCABAŞ, F. (2022). Screening of the small molecule library of Meinox enables the identification of anticancer compounds in pathologically distinct cancers. Turkish Journal of Biology, Cilt: 45 - Sayı: 5, 633–643. https://ajindex.com/articles/600102

📄 Tam Metin PDF Okuyucu

📄

PDF görüntüleyici hazırlanıyor...

Kaynakça (9)

  1. Bakhshaliyev N, Uluganyan M, Enhos A, Karacop E, Ozdemir R (2020). The effect of 5-day course of hydroxychloroquine and azithromycin combination on QT interval in non-ICU COVID19(+) patients. Journal of Electrocardiology 62: 59-64.
  2. Barreca M, Spanò V, Montalbano A, Cueto M, Díaz Marrero AR et al. (2020). Marine Anticancer Agents: An Overview with a Particular Focus on Their Chemical Classes. Marine drugs 18: 619. Bayram B, Ozgur A, Tutar L, Tutar Y (2018). Tumor Targeting of Polymeric Nanoparticles Conjugated with Peptides, Saccharides, and Small Molecules for Anticancer Drugs. Current Pharmaceutical Design 23 (35): 5349-5357.
  3. Beksac M, Balli S, Akcora Yildiz D (2020). Drug Targeting of Genomic Instability in Multiple Myeloma. Frontiers in Genetics 9 (11): 228. doi: 10.3389/fgene.2020.00228 Boztas AO, Karakuzu O, Galante G, Ugur Z, Kocabas F et al. (2013). Synergistic Interaction of Paclitaxel and Curcumin with Cyclodextrin Polymer Complexation in Human Cancer Cells. Molecular Pharmaceutics 10 (7): 2676-83. doi: 10.1021/ mp400101k Boztas AO, Karakuzu O, Galante G, Ugur Z, Kocabas F et al. (2013). Synergistic interaction of paclitaxel and curcumin with cyclodextrin polymer complexation in human cancer cells. Molecular Pharmaceutics 10: 2676-2683.
  4. Coussens NP, Braisted JC, Peryea T, Sittampalam GS, Simeonov A et al. (2017). Small-Molecule Screens: A Gateway to Cancer Therapeutic Agents with Case Studies of Food and Drug Administration–Approved Drugs. Pharmacological Reviews 69: 479-496.
  5. Daglioglu C (2017). Enhancing Tumor Cell Response to Multidrug Resistance with pH-Sensitive Quercetin and Doxorubicin Conjugated Multifunctional Nanoparticles. Colloids and Surfaces B: Biointerfaces 156: 175-185.
  6. Demirel HC, Dogan T, Tuncbag N (2018). A Structural Perspective on the Modulation of Protein-Protein Interactions with Small Molecules. Current Topics in Medicinal Chemistry 18: 700- 713. Ersek A, Xu K, Antonopoulos A, Butters TD, Santo AE et al. (2015). Glycosphingolipid synthesis inhibition limits osteoclast activation and myeloma bone disease. Journal of Clinical Investigation 125: 2279-2292.
  7. Gökbulut AA, Yaşar M, Baran Y (2015).
  8. A Novel Natural Product, KL-21, Inhibits Proliferation and Induces Apoptosis in Chronic Lymphocytic Leukemia Cells. Turkish Journal of Hematology 32: 118-126.
  9. Gravina GL, Senapedis W, McCauley D, Baloglu E, Shacham S et al. (2014). Nucleo-cytoplasmic transport as a therapeutic target of cancer. Journal of Hematology & Oncology 7: 85. Kacı