A Two Arm, Randomized, Multicenter, Single blind, Prospective, Clinical study to evaluate efficacy & safety of PS/MAR/HO-1 oil and a marketed formulation in mild to moderate Hair loss in females - NIL

开始日期2015-05-16

申办/合作机构

Marico Ltd.

100 项与 HO-1(Metabomed) 相关的临床结果

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100 项与 HO-1(Metabomed) 相关的转化医学

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100 项与 HO-1(Metabomed) 相关的专利（医药）

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209

项与 HO-1(Metabomed) 相关的文献（医药）

2024-12-31·Journal of Enzyme Inhibition and Medicinal Chemistry

Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells

Article

作者: Affranchi, Federica ; Intagliata, Sebastiano ; Vanella, Luca ; Salerno, Loredana ; Giuliano, Michela ; Consoli, Valeria ; Sorrenti, Valeria ; Pittalà, Valeria ; Notaro, Antonietta

Colon cancer remains a clinical challenge in industrialised countries. Its treatment with 5-Flurouracil (5-FU) develops many side effects and resistance. Thus, several strategies have been undertaken so far, including the use of drug cocktails and polypharmacology. Heme oxygenase-1 (HO-1) is an emerging molecular target in the treatment of various cancers. We recently demonstrated that a combination of HO-1 inhibitors with 5-FU and the corresponding hybrids SI1/17, SI1/20, and SI1/22, possessed anticancer activity against prostate and lung cancer cells. In this work, we evaluated these hybrids in a model of colon cancer and found that SI1/22 and the respective combo have greater potency than 5-FU. Particularly, compounds inhibit HO-1 activity in cell lysates, increase ROS and the expression of HO-1, SOD, and Nrf2. Moreover, we observed a decrease of pro-caspase and an increase in cleaved PARP-1 and p62, suggesting apoptotic and autophagic cell death and potential application of these drugs as anticancer agents.

2024-11-04·ChemMedChem

CORRIGENDUM: Discovery of SI 1/20 and SI 1/22 as Mutual Prodrugs of 5‐Fluorouracil and Imidazole‐Based Heme Oxygenase 1 Inhibitor with Improved Cytotoxicity in DU145 Prostate Cancer Cells

2024-09-12·ACS Medicinal Chemistry Letters

Highly Selective Novel Heme Oxygenase-1 Hits Found by DNA-Encoded Library Machine Learning beyond the DEL Chemical Space

Article

作者: Cui, Weiren ; Hsueh, Kuang-Lung ; He, Yunyun ; Liu, Huan ; Su, Wenji ; Deng, Jason ; Kuai, Letian ; Han, Shuai ; Song, Yidan ; Guo, Xinyun ; Wang, Min

DNA-encoded library (DEL) technology, especially when combined with machine learning (ML), is a powerful method to discover novel inhibitors. DEL-ML can expand a larger chemical space and boost cost-effectiveness during hit finding. Heme oxygenase-1 (HO-1), a heme-degrading enzyme, is linked to diseases such as cancer and neurodegenerative disorders. The discovery of five series of new scaffold HO-1 hits is reported here, using a DEL-ML workflow, which emphasizes the model's uncertainty quantification and domain of applicability. This model exhibits a strong extrapolation ability, identifying new structures beyond the DEL chemical space. About 37% of predicted molecules showed a binding affinity of K _D < 20 μM, with the strongest being 141 nM, amd 14 of those molecules displayed >100-fold selectivity for HO-1 over heme oxygenase-2 (HO-2). These molecules also showed structural novelty compared to existing HO-1 inhibitors. Docking simulations provided insights into possible selectivity rationale.

100 项与 HO-1(Metabomed) 相关的药物交易

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