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JOURNAL ARTICLE
Guowen Ren, Jinghong Chen, Yue Pu, Eun Ju Yang, Shishi Tao, Pui Kei Mou, Li-Jie Chen, Wenli Zhu, Kin Long Chan, Guanghui Luo, Chuxia Deng, Joong Sup Shim
Loss of PTEN tumor suppressor is an important event during colorectal cancer (CRC) development and is a target for therapeutic exploitation. This study reports that bromodomain and extra-terminal motif (BET) is a synthetic lethal partner of PTEN in CRC. BET inhibition (BETi) selectively induced G1 cell cycle arrest and apoptosis in PTEN-/- CRC. Further, BETi selectively and dose-dependently suppressed the growth of PTEN-/- CRC tumor xenografts in mice and patient-derived organoids. Mechanistically, PTEN-deficient CRC cells elevated the level of cytoplasmic p21CIP1/WAF1 that is hyper-phosphorylated at Thr145 by AKT...
2024: International Journal of Biological Sciences
#2
JOURNAL ARTICLE
Do Yeon Kim, Hyeseon Yun, Ji-Eun You, Ji-U Lee, Dong-Hee Kang, Yea Seong Ryu, Dong-In Koh, Dong-Hoon Jin
Ovarian cancer is the leading cause of gynecologic cancer death. Among the most innovative anti-cancer approaches, the genetic concept of synthetic lethality is that mutations in multiple genes work synergistically to effect cell death. Previous studies found that although vaccinia-related kinase-1 (VRK1) associates with DNA damage repair proteins, its underlying mechanisms remain unclear. Here, we found high VRK1 expression in ovarian tumors, and that VRK1 depletion can significantly promote apoptosis and cell cycle arrest...
April 11, 2024: Experimental Cell Research
#3
JOURNAL ARTICLE
Patricia Bezerra, Eduardo F Motti
Breast cancer stands as the most prevalent type of tumor and a significant contributor to cancer-related deaths. Among its various subtypes, triple-negative breast cancer (TNBC) presents the worst prognosis due to its aggressive nature and the absence of effective treatments. Crotoxin, a protein found in the venom of Crotalus genus snakes, has demonstrated notable antitumor activity against aggressive solid tumors. However, its application has been hindered by substantial toxicity in humans. In efforts to address this challenge, Crotoxin B-derived peptides were synthesized and evaluated in vitro for their antitumor potential, leading to the discovery of 3-NAntC...
April 6, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
#4
JOURNAL ARTICLE
Fanjiao Zuo, Boyao Wang, Lizhi Wang, Jun He, Xilong Qiu
Mesoporous titanium nanoparticles (MTN) have always been a concern and are considered to have great potential for overcoming antibiotic-resistant bacteria. In our study, MTN modified with functionalized UV-responsive ethylene imine polymer (PEI) was synthesized. The characterization of all products was performed by different analyses, including SEM, TEM, FT-IR, TGA, XRD, XPS, and N2 adsorption-desorption isotherms. The typical antibacterial drug berberine hydrochloride (BH) was encapsulated in MTN-PEI. The process exhibited a high drug loading capacity (22...
April 3, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
#5
JOURNAL ARTICLE
Janina Gospodarek, Agnieszka Krajewska, Iwona B Paśmionka, Joanna Bruździńska, Gedyon Tamiru
Thuja occidentalis L. essential oil (EOTO) and its compounds, such as terpinyl acetate, bornyl acetate, and β-thujone, are claimed to be highly effective against some storage pests, sanitary insects, or pests of fruit trees, while data about its use in protecting field crops are very scarce. There is also a lack of information in the literature about the insecticidal value of water extracts from T. occidentalis (WETOs). Both essential oils (EOs) and water extracts (WEs) from various plants have advantages and disadvantages in terms of their use as insecticides...
March 24, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
#6
JOURNAL ARTICLE
Priyadharshini Kannan, Hidayah Baskaran, Jemima Balaselvi Juliana Selvaraj, Agnieszka Saeid, Jennifer Michellin Kiruba Nester
A fungal isolate Aspergillus terreus PDB-B (accession number: MT774567.1), which could tolerate up to 500 mg/L of cypermethrin, was isolated from the lake sediments of Kulamangalam tropical lake, Madurai, and identified by internal transcribed spacer (ITS) sequencing followed by phylogenetic analysis. The biotransformation potential of the strain was compared with five other strains (A, J, UN2, M1 and SM108) as a consortium, which were tentatively identified as Aspergillus glaucus , Aspergillus niger , Aspergillus flavus , Aspergillus terreus , and Aspergillus flavus , respectively...
March 23, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
#7
JOURNAL ARTICLE
Aaron R Ashbrook, Jeffrey L Feder, Gary W Bennett, Matthew D Ginzel, Ameya D Gondhalekar
Many gregarious insect species use aggregation and alarm pheromones. The bed bug, Cimex lectularius L., emits an alarm pheromone (AP), a 70/30 blend of (E)-2-hexenal and (E)-2-octenal, when threatened. Bed bugs avoid temperatures above 43 °C, which are lethal to bugs and used commercially as spatial heat treatments to manage infestations. However, the interaction of bed bug AP in heat avoidance has not been investigated. The goal of this research was to: 1) determine if bed bugs emit AP as an alarm response to heat exposure, and 2) quantify the behavioral responses of conspecifics to AP emitted by heat-exposed bed bugs...
April 12, 2024: Scientific Reports
#8
JOURNAL ARTICLE
DOTA-based plectin-1 targeted contrast agent enables detection of pancreatic cancer in human tissue.
Thais Gazzi, Marina Lesina, Qinghua Wang, Alexandra Berninger, Silke Radetzki, Ihsan Ekin Demir, Larissa Heinemann, Waldemar Meiser, Sebastian Wilke, Jens Peter von Kries, Hana Algül, Hai-Yu Hu, Marc Nazaré
Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive and lethal malignancy with extremely poor patient survival rates. A key reason for the poor prognosis is the lack of effective diagnostic tools to detect the disease at curable, premetastatic stages. Tumor surgical resection is PDAC first-line treatment, however distinguishing between cancerous and healthy tissue with current imaging tools remains a challenge. In this work, we report a DOTA-based fluorescent probe targeting plectin-1 for imaging PDAC with high specificity...
April 12, 2024: Angewandte Chemie
#9
JOURNAL ARTICLE
Jiachen Zhang, Hongjuan Yu, Gang Li
Hepatocellular carcinoma (HCC) has become an important public health problem, and there are still challenges to overcome in clinical treatment. The nanodrug delivery system (NDDS) has developed tremendously in recent years, and many researchers have explored NDDS for the treatment of HCC. Engineered cell membrane-coated nanoparticles (ECNPs) have emerged, combining the unique functions of cell membranes with the engineering versatility of synthetic nanoparticles (NPs) to effectively deliver therapeutic drugs...
March 1, 2024: Biointerphases
#10
JOURNAL ARTICLE
Maria Michela Pallotta, Maddalena Di Nardo, Antonio Musio
Cohesin is a highly conserved ring-shaped complex involved in topologically embracing chromatids, gene expression regulation, genome compartmentalization, and genome stability maintenance. Genomic analyses have detected mutations in the cohesin complex in a wide array of human tumors. These findings have led to increased interest in cohesin as a potential target in cancer therapy. Synthetic lethality has been suggested as an approach to exploit genetic differences in cancer cells to influence their selective killing...
March 30, 2024: Cells
#11
JOURNAL ARTICLE
Rita Turpin, Ruixian Liu, Pauliina M Munne, Aino Peura, Jenna H Rannikko, Gino Philips, Bram Boeckx, Natasha Salmelin, Elina Hurskainen, Ilida Suleymanova, July Aung, Elisa M Vuorinen, Laura Lehtinen, Minna Mutka, Panu E Kovanen, Laura Niinikoski, Tuomo J Meretoja, Johanna Mattson, Satu Mustjoki, Päivi Saavalainen, Andrei Goga, Diether Lambrechts, Jeroen Pouwels, Maija Hollmén, Juha Klefström
BACKGROUND: Combining cytotoxic chemotherapy or novel anticancer drugs with T-cell modulators holds great promise in treating advanced cancers. However, the response varies depending on the tumor immune microenvironment (TIME). Therefore, there is a clear need for pharmacologically tractable models of the TIME to dissect its influence on mono- and combination treatment response at the individual level. METHODS: Here we establish a patient-derived explant culture (PDEC) model of breast cancer, which retains the immune contexture of the primary tumor, recapitulating cytokine profiles and CD8+T cell cytotoxic activity...
April 11, 2024: Journal for Immunotherapy of Cancer
#12
JOURNAL ARTICLE
Xiao-Hong Ding, Yi Xiao, Fenfang Chen, Cheng-Lin Liu, Tong Fu, Zhi-Ming Shao, Yi-Zhou Jiang
Breast cancer is a highly heterogeneous disease with varied subtypes, prognoses and therapeutic responsiveness. Human leukocyte antigen class I (HLA-I) shapes the immunity and thereby influences the outcome of breast cancer. However, the implications of HLA-I variations in breast cancer remain poorly understood. In this study, we established a multiomics cohort of 1156 Chinese breast cancer patients for HLA-I investigation. We calculated four important HLA-I indicators in each individual, including HLA-I expression level, somatic HLA-I loss of heterozygosity (LOH), HLA-I evolutionary divergence (HED) and peptide-binding promiscuity (Pr)...
March 27, 2024: Briefings in Bioinformatics
#13
JOURNAL ARTICLE
John Alexander, Koen Schipper, Sarah Nash, Rachel Brough, Harriet Kemp, Jacopo Iacovacci, Clare Isacke, Rachael Natrajan, Elinor Sawyer, Christopher J Lord, Syed Haider
BACKGROUND: Invasive Lobular Carcinoma (ILC) is a morphologically distinct breast cancer subtype that represents up to 15% of all breast cancers. Compared to Invasive Breast Carcinoma of No Special Type (IBC-NST), ILCs exhibit poorer long-term outcome and a unique pattern of metastasis. Despite these differences, the systematic discovery of robust prognostic biomarkers and therapeutically actionable molecular pathways in ILC remains limited. METHODS: Pathway-centric multivariable models using statistical machine learning were developed and tested in seven retrospective clinico-genomic cohorts (n = 996)...
April 10, 2024: British Journal of Cancer
#14
JOURNAL ARTICLE
Kevin M Cottrell, Kimberly J Briggs, Douglas A Whittington, Haris Jahic, Janid A Ali, Charles B Davis, Shanzhong Gong, Deepali Gotur, Lina Gu, Patrick McCarren, Matthew R Tonini, Alice Tsai, Erik W Wilker, Hongling Yuan, Minjie Zhang, Wenhai Zhang, Alan Huang, John P Maxwell
It has been shown that PRMT5 inhibition by small molecules can selectively kill cancer cells with homozygous deletion of the MTAP gene if the inhibitors can leverage the consequence of MTAP deletion, namely, accumulation of the MTAP substrate MTA. Herein, we describe the discovery of TNG908, a potent inhibitor that binds the PRMT5·MTA complex, leading to 15-fold-selective killing of MTAP -deleted (MTAP-null) cells compared to MTAP intact (MTAP WT) cells. TNG908 shows selective antitumor activity when dosed orally in mouse xenograft models, and its physicochemical properties are amenable for crossing the blood-brain barrier (BBB), supporting clinical study for the treatment of both CNS and non-CNS tumors with MTAP loss...
April 10, 2024: Journal of Medicinal Chemistry
#15
JOURNAL ARTICLE
Vinod Ravasaheb Shinde, Ajinkya Thanekar, Sajmina Khatun, Hima Sree Buddhiraju, Basu Bhattacharjee, Aravind Kumar Rengan
Melanoma is one of the most aggressive and lethal types of cancer owing to its metastatic propensity and chemoresistance property. An alternative therapeutic option is Photodynamic and Photothermal Therapies (PDT/PTT), which employ near-infrared light to generate heat and Reactive Oxygen Species (ROS). As per previous reports, Melanin and its synthetic analogs (i.e., polydopamine nanoparticles) can induce near-infrared (NIR) light-mediated heat energy, thereby selectively targeting and ameliorating cancer cells...
April 9, 2024: Nanotechnology
#16
JOURNAL ARTICLE
Gabriele Picco, Yanhua Rao, Angham Al Saedi, Yang Lee, Sara F Vieira, Shriram Bhosle, Kieron May, Carmen Herranz-Ors, Samantha J Walker, Raynold Shenje, Cansu Dincer, Freddy Gibson, Ruby Banerjee, Zoe Hewitson, Thilo Werner, Joshua E Cottom, Yang Peng, Nanhua Deng, Philip Landis, Daniela Conticelli, Katrina McCarten, Jacob Bush, Mamta Sharma, Howard Lightfoot, David House, Emma Milford, Emma K Grant, Michal P Glogowski, Craig D Wagner, Marcus Bantscheff, Anna Rutkowska-Klute, Cell Model Network Uk Group, Francesca Zappacosta, Jonathan Pettinger, Syd Barthorpe, H Christian Eberl, Brian T Jones, Jessica L Schneck, Dennis J Murphy, Emile E Voest, Joshua P Taygerly, Michael P DeMartino, Matthew A Coelho, Jonathan Houseley, Geeta Sharma, Benjamin J Schwartz, Mathew J Garnett
Microsatellite-unstable (MSI) cancers require WRN helicase to resolve replication stress due to expanded DNA (TA)n-dinucleotide repeats. WRN is a promising synthetic lethal target for MSI tumours, and WRN inhibitors are in development. Here, we used CRISPR-Cas9 base editing to map WRN residues critical for MSI cells, validating the helicase domain as the primary drug target. Fragment-based screening led to the development of potent and highly selective WRN helicase covalent inhibitors. These compounds selectively suppressed MSI model growth In vitro and In vivo by mimicking WRN loss, inducing DNA double-strand breaks at expanded TA-repeats and DNA damage...
April 9, 2024: Cancer Discovery
#17
Kyle B Williams, Alex T Larsson, Bryant J Keller, Katherine E Chaney, Rory L Williams, Minu M Bhunia, Garrett M Draper, Tyler A Jubenville, Sue K Rathe, Christopher L Moertel, Nancy Ratner, David A Largaespada
Neurofibromatosis Type 1 (NF1) is a common cancer predisposition syndrome, caused by heterozygous loss of function mutations in the tumor suppressor gene NF1 . Individuals with NF1 develop benign tumors of the peripheral nervous system (neurofibromas), originating from the Schwann cell linage after somatic loss of the wild type NF1 allele, some of which progress further to malignant peripheral nerve sheath tumors (MPNST). There is only one FDA approved targeted therapy for symptomatic plexiform neurofibromas and none approved for MPNST...
March 25, 2024: bioRxiv
#18
JOURNAL ARTICLE
William Fried, Mrityunjay Tyagi, Leonid Minakhin, Gurushankar Chandramouly, Taylor Tredinnick, Mercy Ramanjulu, William Auerbacher, Marissa Calbert, Timur Rusanov, Trung Hoang, Nikita Borisonnik, Robert Betsch, John J Krais, Yifan Wang, Umeshkumar M Vekariya, John Gordon, George Morton, Tatiana Kent, Tomasz Skorski, Neil Johnson, Wayne Childers, Xiaojiang S Chen, Richard T Pomerantz
The DNA damage response (DDR) protein DNA Polymerase θ (Polθ) is synthetic lethal with homologous recombination (HR) factors and is therefore a promising drug target in BRCA1/2 mutant cancers. We discover an allosteric Polθ inhibitor (Polθi) class with 4-6 nM IC50 that selectively kills HR-deficient cells and acts synergistically with PARP inhibitors (PARPi) in multiple genetic backgrounds. X-ray crystallography and biochemistry reveal that Polθi selectively inhibits Polθ polymerase (Polθ-pol) in the closed conformation on B-form DNA/DNA via an induced fit mechanism...
April 5, 2024: Nature Communications
#19
JOURNAL ARTICLE
D Lucas Kane, Brendan Burke, Monica Diaz, Christian Wolf, William A Fonzi
The destructive impact of fungi in agriculture and animal and human health, coincident with increases in antifungal resistance, underscores the need for new and alternative drug targets to counteract these trends. Cellular metabolism relies on many intermediates with intrinsic toxicity and promiscuous enzymatic activity generates others. Fuller knowledge of these toxic entities and their generation may offer opportunities of antifungal development. From this perspective our observation of media-conditional lethal metabolism in respiratory mutants of the opportunistic fungal pathogen Candida albicans was of interest...
2024: PloS One
#20
REVIEW
Kyle D Reichl, Esther C Y Lee, Ariamala Gopalsamy
INTRODUCTION: The multi-subunit SWI/SNF chromatin remodeling complex is a key epigenetic regulator for many cellular processes, and several subunits are found to be mutated in human cancers. The inactivating mutations of SMARCA4, the ATPase subunit of the complex, result in cellular dependency on the paralog SMARCA2 for survival. This observed synthetic lethal relationship posits targeting SMARCA2 in SMARCA4-deficient settings as an attractive therapeutic target in oncology. AREAS COVERED: This review covers patent literature disclosed during the 2019-30 June 2023 period which claim ATPase inhibitors and PROTAC degraders that bind to the ATPase domain of SMARCA2 and/or SMARCA4...
April 5, 2024: Expert Opinion on Therapeutic Patents
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