Delving into the Latest Updates on Mycosynthetix, Inc. with Synapse

概览

关联

1

项与 Mycosynthetix, Inc. 相关的药物

F-5446

靶点-

作用机制

Histone methyltransferases 抑制剂

在研机构-

原研机构

Mycosynthetix, Inc.

在研适应症-

非在研适应症

结肠癌

最高研发阶段无进展

首次获批国家/地区-

首次获批日期-

100 项与 Mycosynthetix, Inc. 相关的临床结果

登录后查看更多信息

0 项与 Mycosynthetix, Inc. 相关的专利（医药）

登录后查看更多信息

51

项与 Mycosynthetix, Inc. 相关的文献（医药）

2024-09-01·Bioorganic & Medicinal Chemistry Letters

Semisynthetic derivatives of the fungal metabolite eupenifeldin via targeting the tropolone hydroxy groups

Article

作者: Bockbrader, Ross H ; Pierre, Herma C ; Fuchs, James R ; Oberlies, Nicholas H ; Burdette, Joanna E ; Al Subeh, Zeinab Y ; Haughan, Monica A ; Pearce, Cedric J ; Tokarski, Robert J ; Maldonado, Amanda C ; Rangel-Grimaldo, Manuel E

Eupenifeldin (1) is a fungal secondary metabolite possessing bis-tropolone moieties that demonstrates nanomolar cytotoxic activity against a number of cancer cell types. As a potential anticancer lead, this meroterpenoid was used to access 29 semisynthetic analogues via functionalization of the reactive hydroxy groups of the bis-tropolones. A series of ester (2-6), carbonate (7-8), sulfonate (9-16), carbamate (17-20), and ether (21-30) analogues of 1 were generated via 22 reactions. Most of these compounds were disubstituted, produced via functionalization of both of the tropolonic hydroxy moieties, although three mono-functionalized analogues (6, 8, and 24) and one tri-functionalized analogue (3) were also obtained. The cytotoxic activities of 1-30 were evaluated against human melanoma and ovarian cancer cell lines (i.e., MDA-MB-435 and OVCAR3, respectively). Ester and carbonate analogues of 1 (i.e., 2-8) maintained cytotoxicity at the nanomolar level, and the greatest improvement in aqueous solubility came from the monosuccinate analogue (6), which was acylated on the secondary hydroxy at the 11 position.

2024-02-01·Experimental Cell Research

Exploring the in vivo anti-cancer potential of Neosetophomone B in leukemic cells using a zebrafish xenograft model

Article

作者: Kuttikrishnan, Shilpa ; Pearce, Cedric J ; Uddin, Shahab ; El-Elimat, Tamam ; Ahmad, Aamir ; Hasan, Maram ; Alali, Feras Q ; Prabhu, Kirti S ; Yalcin, Huseyin C ; Pourkarimi, Ehsan ; Oberlies, Nicholas H ; Bhat, Ajaz A

Neosetophomone B (NSP-B) is a unique meroterpenoid fungal secondary metabolite that has previously demonstrated promising anti-cancer properties against various cancer cell lines in vitro. However, its in vivo anti-cancer potential remaines unexplored. To fill this gap in our knowledge, we tested NSP-B's in vivo anti-cancer activity using a zebrafish model, an organism that has gained significant traction in biomedical research due to its genetic similarities with humans and its transparent nature, allowing real-time tumor growth observation. For our experiments, we employed the K562-injected zebrafish xenograft model. Upon treating these zebrafish with NSP-B, we observed a marked reduction in the size and number of tumor xenografts. Delving deeper, our analyses indicated that NSP-B curtailed tumor growth and proliferation of leukemic grafted xenograft within the zebrafish. These results show that NSP-B possesses potent in vivo anti-cancer properties, making it a potential novel therapeutic agent for addressing hematological malignancies.

2024-02-01·Cell Biology International

Neosetophomone B induces apoptosis in multiple myeloma cells via targeting of AKT/SKP2 signaling pathway

Article

作者: El-Elimat, Tamam ; Kuttikrishnan, Shilpa ; Ahmad, Fareed ; Mateo, Jericha M ; Prabhu, Kirti S ; Pearce, Cedric J ; Akil, Ammira S Alshabeeb ; Bhat, Ajaz A ; Alali, Feras Q ; Oberlies, Nicholas H ; Uddin, Shahab

AbstractMultiple myeloma (MM) is a hematologic malignancy associated with malignant plasma cell proliferation in the bone marrow. Despite the available treatments, drug resistance and adverse side effects pose significant challenges, underscoring the need for alternative therapeutic strategies. Natural products, like the fungal metabolite neosetophomone B (NSP‐B), have emerged as potential therapeutic agents due to their bioactive properties. Our study investigated NSP‐B's antitumor effects on MM cell lines (U266 and RPMI8226) and the involved molecular mechanisms. NSP‐B demonstrated significant growth inhibition and apoptotic induction, triggered by reduced AKT activation and downregulation of the inhibitors of apoptotic proteins and S‐phase kinase protein. This was accompanied by an upregulation of p21Kip1 and p27Cip1 and an elevated Bax/BCL2 ratio, culminating in caspase‐dependent apoptosis. Interestingly, NSP‐B also enhanced the cytotoxicity of bortezomib (BTZ), an existing MM treatment. Overall, our findings demonstrated that NSP‐B induces caspase‐dependent apoptosis, increases cell damage, and suppresses MM cell proliferation while improving the cytotoxic impact of BTZ. These findings suggest that NSP‐B can be used alone or in combination with other medicines to treat MM, highlighting its importance as a promising phytoconstituent in cancer therapy.

100 项与 Mycosynthetix, Inc. 相关的药物交易

登录后查看更多信息

100 项与 Mycosynthetix, Inc. 相关的转化医学

登录后查看更多信息