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Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies
Bioorg Med Chem. 2023 Sep 7;94:117467. doi: 10.1016/j.bmc.2023.117467. Online ahead of print.ABSTRACTSulfonamides constitute an important class of classical carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. Herein we have accomplished the conjugation of biotin with an ample number of sulfonamide motifs with the aim of testing them in vitro as inhibitors of the human carbonic anhydrase (hCA) isoforms I and II (cytosolic isozymes), as well as hCA IX and XII (transmembrane, tumor-associated enzymes). Most of these newly synthesized compounds exhibited interesting inhibition profiles, with activities in the nanomolar range. The ...
Source: Bioorganic and Medicinal Chemistry - September 18, 2023 Category: Chemistry Authors: Paloma Begines Alessandro Bonardi Alessio Nocentini Paola Gratteri Simone Giovannuzzi Roberto Ronca Camilla Tavani Maria Luisa Massardi Óscar López Claudiu T Supuran Source Type: research
Case Report: Case Series of Kocuria palustris Bacteremia among Immunocompromised Patients
We present three cases of bacteremia in immunocompromised patients admitted to our hospital; one patient was receiving chemotherapy for gall bladder carcinoma, the second was on maintenance hemodialysis for chronic kidney disease, and the third was receiving chemotherapy for acute myeloid leukemia. All three patients presented with a fever in the setting of neutropenia during the course of treatment with chemotherapy (in Cases 1 and 3) or hemodialysis (in Case 2). The blood culture samples of all the patients had pure isolates of Kocuria species K. palustris, which was identified by matrix assisted laser desorption ionisat...
Source: The American Journal of Tropical Medicine and Hygiene - September 18, 2023 Category: Tropical Medicine Authors: Gerlin Varghese Ashima Jamwal Deepika Sarawat Chinmoy Sahu Sangram Singh Patel Nidhi Tejan Source Type: research
Chemoresistance Mechanisms in Non-Small Cell Lung Cancer-Opportunities for Drug Repurposing
Appl Biochem Biotechnol. 2023 Sep 18. doi: 10.1007/s12010-023-04595-7. Online ahead of print.ABSTRACTGlobally, lung cancer contributes significantly to the public health burden-associated mortality. As this form of cancer is insidious in nature, there is an inevitable diagnostic delay leading to chronic tumor development. Non-small cell lung cancer (NSCLC) constitutes 80-85% of all lung cancer cases, making this neoplasia form a prevalent subset of lung carcinoma. One of the most vital aspects for proper diagnosis, prognosis, and adequate therapy is the precise classification of non-small cell lung cancer based on biomarke...
Source: Applied Biochemistry and Biotechnology - September 18, 2023 Category: Biochemistry Authors: Rajdeep Kaur P K Suresh Source Type: research
Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies
Bioorg Med Chem. 2023 Sep 7;94:117467. doi: 10.1016/j.bmc.2023.117467. Online ahead of print.ABSTRACTSulfonamides constitute an important class of classical carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. Herein we have accomplished the conjugation of biotin with an ample number of sulfonamide motifs with the aim of testing them in vitro as inhibitors of the human carbonic anhydrase (hCA) isoforms I and II (cytosolic isozymes), as well as hCA IX and XII (transmembrane, tumor-associated enzymes). Most of these newly synthesized compounds exhibited interesting inhibition profiles, with activities in the nanomolar range. The ...
Source: Bioorganic and Medicinal Chemistry - September 18, 2023 Category: Chemistry Authors: Paloma Begines Alessandro Bonardi Alessio Nocentini Paola Gratteri Simone Giovannuzzi Roberto Ronca Camilla Tavani Maria Luisa Massardi Óscar López Claudiu T Supuran Source Type: research
Role of organic cation transporter 3 (OCT3) in the response of hepatocellular carcinoma to tyrosine kinase inhibitors
In conclusion, analysis by immunohistochemistry of OCT3 in the PM of tumor cells may help to predict the response of HCC patients to sorafenib and potentially to other TKIs.PMID:37722628 | DOI:10.1016/j.bcp.2023.115812
Source: Biochemical Pharmacology - September 18, 2023 Category: Drugs & Pharmacology Authors: Elisa Herraez Ruba Al-Abdulla Meraris Soto Oscar Briz Dominik Bettinger Heike Bantel Sofia Del Carmen Maria A Serrano Andreas Geier Jose J G Marin Rocio I R Macias Source Type: research
NADPH oxidase 4 facilitates progression of chondrosarcoma via generation of reactive oxygen species
Acta Biochim Pol. 2023 Sep 18;70(3):685-692. doi: 10.18388/abp.2020_6580.ABSTRACTNicotinamide adenine dinucleotide phosphate oxidase 4 (NOX4) is an enzyme that regulates reactive oxygen species (ROS) generation, and its function in the development of chondrosarcoma remains unclear. In the present study, we studied NOX4 expression in chondrosarcoma by immunochemical examination, and analyzed the role of NOX4 in viability and apoptosis of human chondrosarcoma cell line SW1353 using NOX4 siRNA or NOX4 inhibitor GKT137831. NOX4 level significantly increased in tumor compared to that in para-carcinoma sample. The levels of NOX4...
Source: Acta Biochim Pol - September 18, 2023 Category: Biochemistry Authors: Zheng Jun Wang Lei Fang Ce Ren Wen Tao Meng Xiang Hui Qing Ci Nan Source Type: research
Circ-PGPEP1 augments renal cell carcinoma proliferation, Warburg effect, and distant metastasis
This study probed the molecular mechanism of circPGPEP1 regulating RCC proliferation, Warburg effect, and distant metastasis by targeting the miR-378a-3p/JPT1 axis. Here identified higher circPGPEP1 expression in RCC tissues and cells by RT-qPCR, and high levels of circPGPEP1 were positively correlated with high histological grade and distant metastasis in RCC patients. Furthermore, patients with high levels of circPGPEP1 had a worse survival prognosis. Functional assays presented that knockdown of circPGPEP1 inhibited RCC proliferation, invasion, migration, EMT, and Warburg effect. Dual-luciferase reporter assay, RNA immu...
Source: Acta Biochim Pol - September 18, 2023 Category: Biochemistry Authors: PeiRui Wang Jin Chen Xin Ye RuYi Wang Lin Chen HanChao Zhang Source Type: research
Circular RNA CSPP1 motivates renal cell carcinoma carcinogenesis and the Warburg effect by targeting RAC1 through microRNA-493-5p
Acta Biochim Pol. 2023 Sep 18;70(3):693-701. doi: 10.18388/abp.2020_6299.ABSTRACTCircular RNAs (circRNAs) take on regulatory roles in renal cell carcinoma (RCC). The research's goal was to figure out circ-CSPP1's role and molecular mechanism in RCC. The results clarified that circ-CSPP1 expression was enhanced in RCC. Down-regulating circ-CSPP1 refrained the proliferation, migration, invasion, and Warburg effect (aerobic glycolysis), but accelerated apoptosis of RCC cells. The luciferase activity assay exhibited that circ-CSPP1 could perform as an endogenous sponge for miR-493-5p. Elevating miR-493-5p repressed RCC progres...
Source: Acta Biochim Pol - September 18, 2023 Category: Biochemistry Authors: Dong Zhang XiaoJie Yang QiDong Luo DeLia Fu HongLiang Li Peng Zhang Chong Tie Source Type: research
Real-world clinical outcomes of patients with metastatic renal cell carcinoma receiving pembrolizumab + axitinib vs. ipilimumab + nivolumab
CONCLUSIONS: Our study provides insight into newer mccRCC treatment tolerability and effectiveness in the real-world US community setting. Our real-world results were comparable to data from clinical trials, which is encouraging for mccRCC patients.PMID:37722984 | DOI:10.1016/j.urolonc.2023.08.009
Source: Urologic Oncology - September 18, 2023 Category: Urology & Nephrology Authors: Neil J Shah Sneha D Sura Reshma Shinde Junxin Shi Puneet Singhal Rodolfo F Perini Robert J Motzer Source Type: research
Chemoresistance Mechanisms in Non-Small Cell Lung Cancer-Opportunities for Drug Repurposing
Appl Biochem Biotechnol. 2023 Sep 18. doi: 10.1007/s12010-023-04595-7. Online ahead of print.ABSTRACTGlobally, lung cancer contributes significantly to the public health burden-associated mortality. As this form of cancer is insidious in nature, there is an inevitable diagnostic delay leading to chronic tumor development. Non-small cell lung cancer (NSCLC) constitutes 80-85% of all lung cancer cases, making this neoplasia form a prevalent subset of lung carcinoma. One of the most vital aspects for proper diagnosis, prognosis, and adequate therapy is the precise classification of non-small cell lung cancer based on biomarke...
Source: Applied Biochemistry and Biotechnology - September 18, 2023 Category: Biochemistry Authors: Rajdeep Kaur P K Suresh Source Type: research
A nomogram based on the risk factors of cervical lymph node metastasis in papillary thyroid carcinoma coexistent with Hashimoto's thyroiditis
CONCLUSION: Based on the risk factors above, a relevant nomogram prediction model was established. The model verification showed that the C-index of the modeling set was 0.814, indicating that the nomogram model had good predicted accuracy. The nomogram based on the risk factors above had good prediction ability, which could optimize thyroidectomy and cervical lymph node dissection and improving prognosis.PMID:37718783 | DOI:10.3233/CH-221673
Source: Clinical Hemorheology and Microcirculation - September 18, 2023 Category: Hematology Authors: Huanhuan Miao Jingwen Zhong Xuesha Xing Jiawei Sun Jiaqi Wu Chengwei Wu Yan Yuan Xianli Zhou Hongbo Wang Source Type: research
Assessing the prognostic value of IMDC risk score for nivolumab-treated patients with renal cancer and malignant melanoma
CONCLUSION: In our study, the IMDC was confirmed to be a prognostic factor for MM. The IMDC groups were similar, except for the favorable RCC and MM groups. Different metastatic sites were prognostic, similar to the IMDC risk group in the MM group.PMID:37718781 | DOI:10.3233/CBM-230159
Source: Cancer Biomarkers : Section A of Disease Markers - September 18, 2023 Category: Cancer & Oncology Authors: Ismail Beyp ınar Y ıldız Sözel Arif Hakan Önder Source Type: research
Machine-learning based integrating bulk and single-cell RNA sequencing reveals the SLC38A5-CCL5 signaling as a promising target for clear cell renal cell carcinoma treatment
In conclusion, our communication signature and its derived model enabled a more precise selection of ccRCC patients who were potential beneficiaries of ICIs. Besides, the SLC38A5-CCL5 axis may serve as a promising target for ccRCC treatment.PMID:37722291 | DOI:10.1016/j.tranon.2023.101790
Source: Translational Oncology - September 18, 2023 Category: Cancer & Oncology Authors: Hualin Chen Wenjie Yang Lin Ma Yingjie Li Zhigang Ji Source Type: research
Integration of palliative care in the management of oral squamous cell carcinoma
Bioinformation. 2023 Jan 31;19(1):1-4. doi: 10.6026/97320630019001. eCollection 2023.ABSTRACTOral Squamous cell Cancers (OSCC) is strongly associated with tobacco consumption. We here in present a case study of a OSCC patient who refused standard oncological care (SOC), to highlight the importance of integrating palliative care (PC) for improved patient outcomes. A 61 years male patient, with history of chewing tobacco for more than 20 years and diagnosed to have OSCC for 1.5 years presented with severe anaemia and a cauliflower-like growth (12 x 10 cm) in the left oral cavity and cheek with greenish-yellow discharge. Pus ...
Source: Bioinformation - September 18, 2023 Category: Bioinformatics Authors: Republica Sridhar Huwait Etimad Peter Natesan Pushparaj Gauthaman Kalamegam Source Type: research
Real-world clinical outcomes of patients with metastatic renal cell carcinoma receiving pembrolizumab + axitinib vs. ipilimumab + nivolumab
CONCLUSIONS: Our study provides insight into newer mccRCC treatment tolerability and effectiveness in the real-world US community setting. Our real-world results were comparable to data from clinical trials, which is encouraging for mccRCC patients.PMID:37722984 | DOI:10.1016/j.urolonc.2023.08.009
Source: Urologic Oncology - September 18, 2023 Category: Urology & Nephrology Authors: Neil J Shah Sneha D Sura Reshma Shinde Junxin Shi Puneet Singhal Rodolfo F Perini Robert J Motzer Source Type: research
