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Journal articles on the topic 'KDMs'

Author: Grafiati

Published: 10 March 2023

Last updated: 31 July 2025

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1

Dorna, Dawid, and Jarosław Paluszczak. "The Emerging Significance of Histone Lysine Demethylases as Prognostic Markers and Therapeutic Targets in Head and Neck Cancers." Cells 11, no. 6 (2022): 1023. http://dx.doi.org/10.3390/cells11061023.

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Epigenetic aberrations, associated with altered DNA methylation profiles and global changes in the level of histone modifications, are commonly detected in head and neck squamous cell carcinomas (HNSCC). Recently, histone lysine demethylases have been implicated in the pathogenesis of HNSCC and emerged as potential molecular targets. Histone lysine demethylases (KDMs) catalyze the removal of methyl groups from lysine residues in histones. By affecting the methylation of H3K4, H3K9, H3K27, or H3K36, these enzymes take part in transcriptional regulation, which may result in changes in the level

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2

Vicioso-Mantis, Marta, Samuel Aguirre, and Marian A. Martínez-Balbás. "JmjC Family of Histone Demethylases Form Nuclear Condensates." International Journal of Molecular Sciences 23, no. 14 (2022): 7664. http://dx.doi.org/10.3390/ijms23147664.

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The Jumonji-C (JmjC) family of lysine demethylases (KDMs) (JMJC-KDMs) plays an essential role in controlling gene expression and chromatin structure. In most cases, their function has been attributed to the demethylase activity. However, accumulating evidence demonstrates that these proteins play roles distinct from histone demethylation. This raises the possibility that they might share domains that contribute to their functional outcome. Here, we show that the JMJC-KDMs contain low-complexity domains and intrinsically disordered regions (IDR), which in some cases reached 70% of the protein.

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3

Wigle, Tim J., Kerren K. Swinger, John E. Campbell, et al. "A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening." Journal of Biomolecular Screening 20, no. 6 (2015): 810–20. http://dx.doi.org/10.1177/1087057115575689.

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Demethylation of histones by lysine demethylases (KDMs) plays a critical role in controlling gene transcription. Aberrant demethylation may play a causal role in diseases such as cancer. Despite the biological significance of these enzymes, there are limited assay technologies for study of KDMs and few quality chemical probes available to interrogate their biology. In this report, we demonstrate the utility of self-assembled monolayer desorption/ionization (SAMDI) mass spectrometry for the investigation of quantitative KDM enzyme kinetics and for high-throughput screening for KDM inhibitors. S

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4

Bonnici, Joanna, Anthony Tumber, Akane Kawamura, and Christopher J. Schofield. "Inhibitors of both the N -methyl lysyl- and arginyl-demethylase activities of the JmjC oxygenases." Philosophical Transactions of the Royal Society B: Biological Sciences 373, no. 1748 (2018): 20170071. http://dx.doi.org/10.1098/rstb.2017.0071.

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The Jumonji C (JmjC) family of 2-oxoglutarate (2OG)-dependent oxygenases have established roles in the regulation of transcription via the catalysis of demethylation of N ε - methylated lysine residues in histone tails, especially the N - terminal tail of histone H3. Most human JmjC N ɛ -methyl lysine demethylases (KDMs) are complex enzymes, with ‘reader domains’ in addition to their catalytic domains. Recent biochemical evidence has shown that some, but not all, JmjC KDMs also have N ω - methyl arginyl demethylase (RDM) activity. JmjC KDM activity has been linked to multiple cancers and some

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5

Kim, Yoon-Jung, Dong Hoon Lee, Yong-Sung Choi, Jin-Hyun Jeong, and So Hee Kwon. "Benzo[b]tellurophenes as a Potential Histone H3 Lysine 9 Demethylase (KDM4) Inhibitor." International Journal of Molecular Sciences 20, no. 23 (2019): 5908. http://dx.doi.org/10.3390/ijms20235908.

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Gene expression and tumor growth can be regulated by methylation levels of lysine residues on histones, which are controlled by histone lysine demethylases (KDMs). Series of benzo[b]tellurophene and benzo[b]selenophene compounds were designed and synthesized and they were evaluated for histone H3 lysine 9 demethylase (KDM4) inhibitory activity. Among the carbamates, alcohol and aromatic derivatives, tert-butyl benzo[b]tellurophen-2-ylmethylcarbamate (compound 1c) revealed KDM4 specific inhibitory activity in cervical cancer HeLa cells, whereas the corresponding selenium or oxygen substitute co

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6

Guo, Xiaoqiang, and Qiaoxia Zhang. "The emerging role of histone demethylases in renal cell carcinoma." Journal of Kidney Cancer and VHL 4, no. 2 (2017): 1–5. http://dx.doi.org/10.15586/jkcvhl.2017.56.

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Renal cell carcinoma (RCC), the most common kidney cancer, is responsible for more than 100,000 deaths per year worldwide. The molecular mechanism of RCC is poorly understood. Many studies have indicated that epigenetic changes such as DNA methylation, noncoding RNAs, and histone modifications are central to the pathogenesis of cancer. Histone demethylases (KDMs) play a central role in histone modifications. There is emerging evidence that KDMs such as KDM3A, KDM5C, KDM6A, and KDM6B play important roles in RCC. The available literature suggests that KDMs could promote RCC development and progr

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7

Wang, Zhanxin, and Dinshaw J. Patel. "Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases." Quarterly Reviews of Biophysics 46, no. 4 (2013): 349–73. http://dx.doi.org/10.1017/s0033583513000085.

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AbstractAltered chromatin structures and dynamics are responsible for a range of human malignancies, among which the status of histone lysine methylation remains of paramount importance. Histone lysine methylation is maintained by the relative activities of sequence-specific methyltransferase (KMT) writers and demethylase (KDM) erasers, with aberrant enzymatic activities or expression profiles closely correlated with multiple human diseases. Hence, targeting these epigenetic enzymes should provide a promising avenue for pharmacological intervention of aberrantly marked sites within the epigeno

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8

Hanauske-Abel, Hartmut Martin, Mainul Hoque, Seema Husain, Sukhwinder Singh, Axel R. Hanauske, and Patricia Soteropoulos. "Abstract 2722: An added twist: drug-mediated pan-inhibition of KDM catalysis causes selective reduction of mRNAs that encode a small subset of KDM enzymes." Cancer Research 85, no. 8_Supplement_1 (2025): 2722. https://doi.org/10.1158/1538-7445.am2025-2722.

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Abstract Background: The class of 2-oxoglutarate-requiring mono-iron dioxygenases (MIDOs) that demethylate specific lysine, histidine, or arginine residues of histones is receiving attention for its role in human diseases, in particular cancer (10.1016/j.ejmech.2022.114143). The steric events during MIDO catalysis were resolved at subatomic scale in 1982 by two students at Philipps University, Marburg/Germany (HAG mechanism [10.1016/0022-5193(82)90320-4, 10.1016/0022-5193(82)90320-4]). They presented a classification of all conceivable inhibitors and rapidly reduced their seminal approach to p

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9

Nic-Can, Geovanny I., Beatriz A. Rodas-Junco, Leydi M. Carrillo-Cocom, et al. "Epigenetic Regulation of Adipogenic Differentiation by Histone Lysine Demethylation." International Journal of Molecular Sciences 20, no. 16 (2019): 3918. http://dx.doi.org/10.3390/ijms20163918.

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Obesity is a rising public health problem that contributes to the development of several metabolic diseases and cancer. Adipocyte precursors outside of adipose depots that expand due to overweight and obesity may have a negative impact on human health. Determining how progenitor cells acquire a preadipocyte commitment and become mature adipocytes remains a significant challenge. Over the past several years, we have learned that the establishment of cellular identity is widely influenced by changes in histone marks, which in turn modulate chromatin structure. In this regard, histone lysine deme

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10

Nanduri, Jayasri, Ning Wang, Benjamin L. Wang та Nanduri R. Prabhakar. "Lysine demethylase KDM6B regulates HIF-1α-mediated systemic and cellular responses to intermittent hypoxia". Physiological Genomics 53, № 9 (2021): 385–94. http://dx.doi.org/10.1152/physiolgenomics.00045.2021.

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Intermittent hypoxia (IH) is a hallmark manifestation of obstructive sleep apnea (OSA). Rodents treated with IH exhibit hypertension. Hypoxia-inducible factor (HIF)-1-dependent transcriptional activation of NADPH oxidases ( Nox) and the resulting increase in reactive oxygen species (ROS) levels is a major molecular mechanism underlying IH/OSA-induced hypertension. Jumanji C (JmjC)-containing histone lysine demethylases (JmjC-KDMs) are coactivators of HIF-1-dependent transcriptional activation. In the present study, we tested the hypothesis that JmjC-KDMs are required for IH-evoked HIF-1 transc

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11

Perusini, Maria Agustina, Eleanore Louise Musick, Filza Gul, et al. "Retrospective Evaluation of BCR::ABL Kinase Domain Mutation Profiles and Treatment Outcomes in Patients with Chronic Myeloid Leukemia to Confirm Clinical Relevance of in Vitro Sensitivity-Based Treatment Switch: Real-World Experience." Blood 144, Supplement 1 (2024): 3810. https://doi.org/10.1182/blood-2024-210449.

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Introduction The constitutively active BCR::ABL fusion protein leads to dysregulated tyrosine kinase activity and leukemogenesis in chronic myeloid leukemia (CML). The BCR::ABL kinase domain mutation (KDM) activates signalling pathways, promoting uncontrolled proliferation, evasion of apoptosis, and drug resistance. The emergence of ABL1 KDMs confers resistance to conventional therapeutic agents, including tyrosine kinase inhibitors (TKIs). A strategy to overcome ABL1 KDM involves TKI switch based on the IC50 experiments generated from the BaF3 cell lines harboring ABL1 KDMs. While therapeutic

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12

Karásek, Matej, and Ľubica Kollárová. "The Christian Democratic Youth of Slovakia: Christian Legacy, Post-Socialist Memory and the Present Spirit of Capitalism." Ethnologia Actualis 15, no. 1 (2015): 40–64. http://dx.doi.org/10.1515/eas-2015-0008.

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Abstract The subject of this case study is the youth political organisation Christian Democratic Youth of Slovakia (KDMS). The first parts of this paper are dedicated to history and the structure of organisation. Latter parts discuss the influence of historical memory on creating the collective discourses of KDMS and its civic engagements, ambitions and activities. The purpose of the paper is also to evaluate the role of religion and secularisation in KDMS agenda and also to discuss the ways how the ´christian heritage´ becames the source for arguments in political debates and opossitely how t

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13

Lee, Jina, Ji-Soo Kim, Hye-In Cho, So-Ra Jo, and Yeun-Kyu Jang. "JIB-04, a Pan-Inhibitor of Histone Demethylases, Targets Histone-Lysine-Demethylase-Dependent AKT Pathway, Leading to Cell Cycle Arrest and Inhibition of Cancer Stem-Like Cell Properties in Hepatocellular Carcinoma Cells." International Journal of Molecular Sciences 23, no. 14 (2022): 7657. http://dx.doi.org/10.3390/ijms23147657.

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JIB-04, a pan-histone lysine demethylase (KDM) inhibitor, targets drug-resistant cells, along with colorectal cancer stem cells (CSCs), which are crucial for cancer recurrence and metastasis. Despite the advances in CSC biology, the effect of JIB-04 on liver CSCs (LCSCs) and the malignancy of hepatocellular carcinoma (HCC) has not been elucidated yet. Here, we showed that JIB-04 targeted KDMs, leading to the growth inhibition and cell cycle arrest of HCC, and abolished the viability of LCSCs. JIB-04 significantly attenuated CSC tumorsphere formation, growth, relapse, migration, and invasion in

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14

Liu, Oscar Hsin-Fu, Miika Kiema, Mustafa Beter, Seppo Ylä-Herttuala, Johanna P. Laakkonen, and Minna U. Kaikkonen. "Hypoxia-Mediated Regulation of Histone Demethylases Affects Angiogenesis-Associated Functions in Endothelial Cells." Arteriosclerosis, Thrombosis, and Vascular Biology 40, no. 11 (2020): 2665–77. http://dx.doi.org/10.1161/atvbaha.120.315214.

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Objective: Previous studies have demonstrated that the expression of several lysine (K)-specific demethylases (KDMs) is induced by hypoxia. Here, we sought to investigate the exact mechanisms underlying this regulation and its functional implications for endothelial cell function, such as angiogenesis. Approach and Results: We analyzed the expression changes of KDMs under hypoxia and modulation of HIF (hypoxia-inducible factor) expression using GRO-Seq and RNA-Seq in endothelial cells. We provide evidence that the majority of the KDMs are induced at the level of nascent transcription mediated

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15

Lee, Song Hee, Emily R. Albright, Jeong-Hee Lee, Derek Jacobs, and Robert F. Kalejta. "Cellular defense against latent colonization foiled by human cytomegalovirus UL138 protein." Science Advances 1, no. 10 (2015): e1501164. http://dx.doi.org/10.1126/sciadv.1501164.

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Intrinsic immune defenses mediated by restriction factors inhibit productive viral infections. Select viruses rapidly establish latent infections and, with gene expression profiles that imply cell-autonomous intrinsic defenses, may be the most effective immune control measure against latent reservoirs. We illustrate that lysine-specific demethylases (KDMs) are restriction factors that prevent human cytomegalovirus from establishing latency by removing repressive epigenetic modifications from histones associated with the viral major immediate early promoter (MIEP), stimulating the expression of

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16

Shobab, Leila, Hui Zheng, Kirk Jensen, et al. "Sex-Specific Expression of Histone Lysine Demethylases (KDMs) in Thyroid Cancer." Cancers 16, no. 7 (2024): 1260. http://dx.doi.org/10.3390/cancers16071260.

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Background: The incidence of thyroid cancer in women is 3–4-fold higher than in men. To characterize sex-specific molecular alterations in thyroid cancer, we examined the expression of sex-biased genes in normal thyroids and thyroid tumors. Methods: Ingenuity pathways analysis was used to define sex-biased gene networks using data from the Cancer Genome Atlas (TCGA). Confirmatory studies were performed through the analysis of histone lysine demethylases (KDMs) expression by real-time PCR and immunostaining. Results: In normal thyroids, 44 sex-biased genes were comparatively upregulated in male

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17

Xu, Ling, Yuhong Lu, Jing Lai, et al. "Characteristics of the TCR Vbeta Repertoire and Identical Clonally Expanded T Cells in Chronic Myeloid Leukemia Patients in Advanced Phase with ABL Mutations." Blood 126, no. 23 (2015): 5136. http://dx.doi.org/10.1182/blood.v126.23.5136.5136.

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Abstract Abstract Tumor specific or related antigen cytotoxic lymphocyte (CTL) have been identified in chronic myeloid leukemia patients, however, whether they are constituted by specific type of T cell receptor chains has not been illustrated so far. Previous studies have reported abnormal TCR repertoires and clonally expanded TCR Vβ T cells in chronic myeloid leukemia in chronic phase (CP-CML). In this study, we investigated the distribution and clonality of the TCR Vβ repertoire in 5 CML patients in blast crisis (BC-CML) and one in acceleration phase (AP-CML) with ABL kinase domain mutation

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18

Park, Hyunsung, and Soojeong Chang. "Abstract 4766: Hypoxia increases the methylated histones to prevent histone clipping during Raf-induced senescence." Cancer Research 83, no. 7_Supplement (2023): 4766. http://dx.doi.org/10.1158/1538-7445.am2023-4766.

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Abstract Hypoxia increases methylated histones by inhibiting O2- and α-ketoglutarate-dependent histone lysine demethylases (KDMs). This study is the first to demonstrate how the hypoxic increment of methylated histones cross-talks with other epigenetic changes, such as histone clipping and heterochromatin redistribution, named senescence-associated heterochromatin foci (SAHF), which are found during oncogene-induced senescence (OIS). Raf-activation in primary human fibroblasts IMR90 increases mature cathepsin L (CTSL)-mediated clipping of histone H3, H2B and H4. Hypoxia protects histones from

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19

Arifuzzaman, Sarder, Mst Reshma Khatun, and Rabeya Khatun. "Emerging of lysine demethylases (KDMs): From pathophysiological insights to novel therapeutic opportunities." Biomedicine & Pharmacotherapy 129 (September 2020): 110392. http://dx.doi.org/10.1016/j.biopha.2020.110392.

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20

Wang, Zhen, and Huadong Liu. "Roles of Lysine Methylation in Glucose and Lipid Metabolism: Functions, Regulatory Mechanisms, and Therapeutic Implications." Biomolecules 14, no. 7 (2024): 862. http://dx.doi.org/10.3390/biom14070862.

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Glucose and lipid metabolism are essential energy sources for the body. Dysregulation in these metabolic pathways is a significant risk factor for numerous acute and chronic diseases, including type 2 diabetes (T2DM), Alzheimer’s disease (AD), obesity, and cancer. Post-translational modifications (PTMs), which regulate protein structure, localization, function, and activity, play a crucial role in managing cellular glucose and lipid metabolism. Among these PTMs, lysine methylation stands out as a key dynamic modification vital for the epigenetic regulation of gene transcription. Emerging evide

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He, Xingrui, Hang Zhang, Yingqian Zhang, et al. "Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present)." European Journal of Medicinal Chemistry 231 (March 2022): 114143. http://dx.doi.org/10.1016/j.ejmech.2022.114143.

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22

Tarhonskaya, Hanna, Anthony Tumber, Akane Kawamura, and Christopher J. Schofield. "In Vitro Enzyme Assays for JmjC-Domain-Containing Lysine Histone Demethylases (JmjC-KDMs)." Current Protocols in Pharmacology 80, no. 1 (2018): 3.15.1–3.15.12. http://dx.doi.org/10.1002/cpph.34.

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23

Carmichael, James, Laure Escoubet, Kate Lines, et al. "RF19 | PSUN349 Histone Eraser and Reader Targeting Epigenetic Inhibitors Are Effective in Pancreatic Neuroendocrine Tumours." Journal of the Endocrine Society 6, Supplement_1 (2022): A897—A898. http://dx.doi.org/10.1210/jendso/bvac150.1859.

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Abstract Background The 5-year survival for metastatic pancreatic neuroendocrine tumours (PNETs) is &lt;50%, and current therapies are not effective. Thus, there is an unmet clinical need for new therapies for patients with PNETs. PNETs frequently have mutations in chromatin remodelling genes, including in Multiple Endocrine Neoplasia type 1 (MEN1), encoding menin, which is mutated in up to 40% of sporadic PNETs, and is part of multiple histone modifying complexes including the SET1/MLL methyltransferases. Aim To examine multiple classes of epigenetic inhibitors and determine which may be

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24

Banelli, Barbara, Antonio Daga, Alessandra Forlani, et al. "Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells." Oncotarget 8, no. 21 (2017): 34896–910. http://dx.doi.org/10.18632/oncotarget.16820.

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25

Koutsioumpa, Marina, Maria Hatziapostolou, Christos Polytarchou, et al. "Lysine methyltransferase 2D regulates pancreatic carcinogenesis through metabolic reprogramming." Gut 68, no. 7 (2018): 1271–86. http://dx.doi.org/10.1136/gutjnl-2017-315690.

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ObjectiveDespite advances in the identification of epigenetic alterations in pancreatic cancer, their biological roles in the pathobiology of this dismal neoplasm remain elusive. Here, we aimed to characterise the functional significance of histone lysine methyltransferases (KMTs) and demethylases (KDMs) in pancreatic tumourigenesis.DesignDNA methylation sequencing and gene expression microarrays were employed to investigate CpG methylation and expression patterns of KMTs and KDMs in pancreatic cancer tissues versus normal tissues. Gene expression was assessed in five cohorts of patients by re

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26

Kindrick, Jessica D., Peter J. Ratcliffe, WIlliam Doug Figg, and David R. Mole. "Abstract 3766: Correlating locus-specific changes in histone trimethylation and gene expression in hypoxia." Cancer Research 82, no. 12_Supplement (2022): 3766. http://dx.doi.org/10.1158/1538-7445.am2022-3766.

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Abstract Low oxygen availability (hypoxia) is a common feature of many solid tumors and is associated with poor prognosis and resistance to therapy. The main regulator of cellular responses to hypoxia is the transcription factor HIF (hypoxia-inducible factor). In addition, several histone lysine demethylases (KDMs) are 2-OG dependent dioxygenases and require oxygen for their activity. When oxygen availability is limited, the activity of these KDMs is inhibited leading to global histone hypermethylation, potentially altering gene expression. However, some KDMs are also known to be direct transc

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Carter, David M., Edgar Specker, Jessica Przygodda, et al. "Identification of a Novel Benzimidazole Pyrazolone Scaffold That Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells." SLAS DISCOVERY: Advancing the Science of Drug Discovery 22, no. 7 (2017): 801–12. http://dx.doi.org/10.1177/2472555217699157.

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Human lysine demethylase (KDM) enzymes (KDM1–7) constitute an emerging class of therapeutic targets, with activities that support growth and development of metastatic disease. By interacting with and co-activating the androgen receptor, the KDM4 subfamily (KDM4A–E) promotes aggressive phenotypes of prostate cancer (PCa). Knockdown of KDM4 expression or inhibition of KDM4 enzyme activity reduces the proliferation of PCa cell lines and highlights inhibition of lysine demethylation as a possible therapeutic method for PCa treatment. To address this possibility, we screened the ChemBioNet small mo

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28

Reis, Linda M., Huban Atilla, Peter Kannu, et al. "Distinct Roles of Histone Lysine Demethylases and Methyltransferases in Developmental Eye Disease." Genes 14, no. 1 (2023): 216. http://dx.doi.org/10.3390/genes14010216.

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Histone lysine methyltransferase and demethylase enzymes play a central role in chromatin organization and gene expression through the dynamic regulation of histone lysine methylation. Consistent with this, genes encoding for histone lysine methyltransferases (KMTs) and demethylases (KDMs) are involved in complex human syndromes, termed congenital regulopathies. In this report, we present several lines of evidence for the involvement of these genes in developmental ocular phenotypes, suggesting that individuals with structural eye defects, especially when accompanied by craniofacial, neurodeve

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Choi, Yong-Ho, Min-Woo Lee, and Kwang-Soo Shin. "The Lysine Demethylases KdmA and KdmB Differently Regulate Asexual Development, Stress Response, and Virulence in Aspergillus fumigatus." Journal of Fungi 8, no. 6 (2022): 590. http://dx.doi.org/10.3390/jof8060590.

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Histone demethylases govern diverse cellular processes, including growth, development, and secondary metabolism. In the present study, we investigated the functions of two lysine demethylases, KdmA and KdmB, in the opportunistic human pathogenic fungus Aspergillus fumigatus. Experiments with mutants harboring deletions of genes encoding KdmA (ΔkdmA) and KdmB (ΔkdmB) showed that KdmA is necessary for normal growth and proper conidiation, whereas KdmB negatively regulates vegetative growth and conidiation. In both mutant strains, tolerance to H2O2 was significantly decreased, and the activities

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Staehle, Hans Felix, Heike Luise Pahl, and Jonas Samuel Jutzi. "The Cross Marks the Spot: The Emerging Role of JmjC Domain-Containing Proteins in Myeloid Malignancies." Biomolecules 11, no. 12 (2021): 1911. http://dx.doi.org/10.3390/biom11121911.

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Histone methylation tightly regulates chromatin accessibility, transcription, proliferation, and cell differentiation, and its perturbation contributes to oncogenic reprogramming of cells. In particular, many myeloid malignancies show evidence of epigenetic dysregulation. Jumonji C (JmjC) domain-containing proteins comprise a large and diverse group of histone demethylases (KDMs), which remove methyl groups from lysines in histone tails and other proteins. Cumulating evidence suggests an emerging role for these demethylases in myeloid malignancies, rendering them attractive targets for drug in

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Benedetti, Rosaria, Carmela Dell’Aversana, Tommaso De Marchi та ін. "Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer". Cancers 11, № 12 (2019): 2027. http://dx.doi.org/10.3390/cancers11122027.

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In breast cancer, Lysine-specific demethylase-1 (LSD1) and other lysine demethylases (KDMs), such as Lysine-specific demethylase 6A also known as Ubiquitously transcribed tetratricopeptide repeat, X chromosome (UTX), are co-expressed and co-localize with estrogen receptors (ERs), suggesting the potential use of hybrid (epi)molecules to target histone methylation and therefore regulate/redirect hormone receptor signaling. Here, we report on the biological activity of a dual-KDM inhibitor (MC3324), obtained by coupling the chemical properties of tranylcypromine, a known LSD1 inhibitor, with the

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32

Tian, Yuzhen, Ruiyi Fan, and Jiwu Zeng. "Comprehensive Analysis of Jumonji Domain C Family from Citrus grandis and Expression Profilings in the Exocarps of “Huajuhong” (Citrus grandis “Tomentosa”) during Various Development Stages." Horticulturae 7, no. 12 (2021): 592. http://dx.doi.org/10.3390/horticulturae7120592.

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Citrus grandis “Tomentosa” (“Huajuhong”) is a famous Traditional Chinese Medicine. In this study, a total of 18 jumonji C (JMJC) domain-containing proteins were identified from C. grandis. The 18 CgJMJCs were unevenly located on six chromosomes of C. grandis. Phylogenetic analysis revealed that they could be classified into five groups, namely KDM3, KDM4, KDM5, JMJC, and JMJD6. The domain structures and motif architectures in the five groups were diversified. Cis-acting elements on the promoters of 18 CgJMJC genes were also investigated, and the abscisic acid-responsive element (ABRE) was dist

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33

Porta, A. Vilarrubí, J. J. Alburquerque Béjar, D. Trastulli, et al. "EP1.14-39 BRG1 Deficient Cells Are Sensitive to the Inhibition of Specific Lysine Demethylases (KDMs) in Lung Cancer." Journal of Thoracic Oncology 14, no. 10 (2019): S1047. http://dx.doi.org/10.1016/j.jtho.2019.08.2324.

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Diaz-Hernandez, Martha, Kimihide Murakami, Shizumasa Murata, et al. "Inhibition of KDM2/7 Promotes Notochordal Differentiation of hiPSCs." Cells 13, no. 17 (2024): 1482. http://dx.doi.org/10.3390/cells13171482.

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Intervertebral disc disease (IDD) is a debilitating spine condition that can be caused by intervertebral disc (IVD) damage which progresses towards IVD degeneration and dysfunction. Recently, human pluripotent stem cells (hPSCs) were recognized as a valuable resource for cell-based regenerative medicine in skeletal diseases. Therefore, adult somatic cells reprogrammed into human induced pluripotent stem cells (hiPSCs) represent an attractive cell source for the derivation of notochordal-like cells (NCs) as a first step towards the development of a regenerative therapy for IDD. Utilizing a diff

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35

Lin, Zi-Han, Yen-Fan Chan, Min-Hsiung Pan, Yen-Chen Tung, and Zheng-Yuan Su. "Aged Citrus Peel (Chenpi) Prevents Acetaminophen-Induced Hepatotoxicity by Epigenetically Regulating Nrf2 Pathway." American Journal of Chinese Medicine 47, no. 08 (2019): 1833–51. http://dx.doi.org/10.1142/s0192415x19500939.

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Excessive consumption of analgesic drug acetaminophen (APAP) can cause severe oxidative stress-mediated liver injury. Here, we investigated the protective effect and mechanism of aged citrus peel (Chenpi, CP), a Chinese herb usually used in foods in Asia, against APAP-induced hepatotoxicity. CP water (CP-WE), ethanolic (CP-EE), and water extraction residue ethanolic (CP-WREE) extracts were prepared. We found that CP-WREE contained higher content of bioactive flavonoids, including narirutin, nobiletin, and tangeretin, and more effectively enhanced the Nrf2 pathway in ARE-luciferase reporter gen

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Kim, Yong Yean, Girma Woldemichael, Berkley Gryder, et al. "Abstract 703: Novel histone lysine demethylase inhibitors disrupt PAX3-FOXO1-driven transcriptional output in fusion-positive rhabdomyosarcoma." Cancer Research 82, no. 12_Supplement (2022): 703. http://dx.doi.org/10.1158/1538-7445.am2022-703.

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Abstract BACKGROUND: The PAX3/7-FOXO1 (P3F) fusion transcription factor is the oncogenic driver in fusion-positive rhabdomyosarcoma (FP-RMS). P3F drives oncogenesis in FP-RMS through transcriptional modulation of downstream target genes. Thus, P3F represents a unique vulnerability in FP-RMS. A screen for inhibitors of P3F action identified novel histone lysine demethylase (KDM) inhibitors characterized in this study. MATERIALS/METHODS: A specific luciferase assay which monitors P3F activity was utilized to screen 62,643 compounds. The top candidate with unknown mechanism of action, PFI-63, and

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Xie, Jiang, Jiamin Sun, Jiatai Feng, et al. "Kernel Differential Subgraph Analysis to Reveal the Key Period Affecting Glioblastoma." Biomolecules 10, no. 2 (2020): 318. http://dx.doi.org/10.3390/biom10020318.

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Glioblastoma (GBM) is a fast-growing type of malignant primary brain tumor. To explore the mechanisms in GBM, complex biological networks are used to reveal crucial changes among different biological states, which reflect on the development of living organisms. It is critical to discover the kernel differential subgraph (KDS) that leads to drastic changes. However, identifying the KDS is similar to the Steiner Tree problem that is an NP-hard problem. In this paper, we developed a criterion to explore the KDS (CKDS), which considered the connectivity and scale of KDS, the topological difference

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Maitra, Swati, Nitin Khandelwal, Scherazad Kootar, et al. "Histone Lysine Demethylase JMJD2D/KDM4D and Family Members Mediate Effects of Chronic Social Defeat Stress on Mouse Hippocampal Neurogenesis and Mood Disorders." Brain Sciences 10, no. 11 (2020): 833. http://dx.doi.org/10.3390/brainsci10110833.

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Depression, anxiety and related mood disorders are major psychiatric illnesses worldwide, and chronic stress appears to be one of the primary underlying causes. Therapeutics to treat these debilitating disorders without a relapse are limited due to the incomplete molecular understanding of their etiopathology. In addition to the well-studied genetic component, research in the past two decades has implicated diverse epigenetic mechanisms in mediating the negative effects of chronic stressful events on neural circuits. This includes the cognitive circuitry, where the dynamic hippocampal dentate

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Schütt, Jacqueline, Theresa Nägler, Tino Schenk, and Annamaria Brioli. "Investigating the Interplay between Myeloma Cells and Bone Marrow Stromal Cells in the Development of Drug Resistance: Dissecting the Role of Epigenetic Modifications." Cancers 13, no. 16 (2021): 4069. http://dx.doi.org/10.3390/cancers13164069.

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Multiple Myeloma (MM) is a malignancy of plasma cells infiltrating the bone marrow (BM). Many studies have demonstrated the crucial involvement of bone marrow stromal cells in MM progression and drug resistance. Together with the BM microenvironment (BMME), epigenetics also plays a crucial role in MM development. A variety of epigenetic regulators, including histone acetyltransferases (HATs), histone methyltransferases (HMTs) and lysine demethylases (KDMs), are altered in MM, contributing to the disease progression and prognosis. In addition to histone modifications, DNA methylation also plays

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Johnston, Alexis, and Adegboyega K. Oyelere. "Abstract 3092: Optimization of deferiprone for the treatment of triple-negative breast cancer." Cancer Research 83, no. 7_Supplement (2023): 3092. http://dx.doi.org/10.1158/1538-7445.am2023-3092.

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Abstract Triple-negative breast cancer (TNBC) is the leading cause of new cancer cases and the second leading cause of cancer deaths in American women. TNBC is one of the most difficult cancers to treat due to the lack of three receptors, estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor (HER2), found in regular forms of breast cancer (BCa). Currently, there is no targeted therapy for TNBC and treatment options to manage this lethal disease include surgery, adjuvant chemotherapy and radiotherapy. A better understanding of TNBC etiology has aided in

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Kuo, Mei-Tsan, Isabelle Weber, Christa Fittschen, Luc Vereecken, and Jim Jr-Min Lin. "Kinetics of dimethyl sulfide (DMS) reactions with isoprene-derived Criegee intermediates studied with direct UV absorption." Atmospheric Chemistry and Physics 20, no. 21 (2020): 12983–93. http://dx.doi.org/10.5194/acp-20-12983-2020.

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Abstract. Criegee intermediates (CIs) are formed in the ozonolysis of unsaturated hydrocarbons and play a role in atmospheric chemistry as a non-photolytic OH source or a strong oxidant. Using a relative rate method in an ozonolysis experiment, Newland et al. (2015) reported high reactivity of isoprene-derived Criegee intermediates towards dimethyl sulfide (DMS) relative to that towards SO2 with the ratio of the rate coefficients kDMS+CI/kSO2+CI = 3.5 ± 1.8. Here we reinvestigated the kinetics of DMS reactions with two major Criegee intermediates formed in isoprene ozonolysis, CH2OO, and methy

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Liu, Mengshi, Jiacan Jiang, Yapeng Han, et al. "Functional Characterization of the Lysine-Specific Histone Demethylases Family in Soybean." Plants 11, no. 11 (2022): 1398. http://dx.doi.org/10.3390/plants11111398.

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Histone modifications, such as methylation and demethylation, have crucial roles in regulating chromatin structure and gene expression. Lysine-specific histone demethylases (LSDs) belong to the amine oxidase family, which is an important family of histone lysine demethylases (KDMs), and functions in maintaining homeostasis of histone methylation. Here, we identified six LSD-like (LDL) genes from the important leguminous soybean. Phylogenetic analyses divided the six GmLDLs into four clusters with two highly conserved SWRIM and amine oxidase domains. Indeed, demethylase activity assay using rec

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जोगदंड, रमेश बापूराव. "मराठवाड्यातील पर्यटन उद्योगपुढील समस्या आणि उपाय योजना". Journal of Research & Development' 14, № 7 (2022): 1–2. https://doi.org/10.5281/zenodo.6984905.

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<strong>izLrkouk</strong>       vusd ns’kkr i;ZVu m|ksxkpk fodkl eksB~;k izek.kkr >kysyk fnlwu ;srks ,o<sp ukgh rj R;kaph vFkZO;oLFkk iw.kZi.ks i;ZVdkaojp vk/kkjhr vkgs] rlsp Hkkjrkrhy dkgh jkT;kph vFkZO;oLFkk v’kkp izdkjph vkgs- i;ZVu gk vk/kqfud txkrhy ,d izxr m|ksx vkgs- gtkjks yksd ;k O;olk;k’kh fuxMhr vkgsr- vusdkaP;k gkrkyk jkstxkj ns.;kps dke ;k i;ZVu m|ksxkus dsysys fnlwu ;srs- R;keqGs ejkBokM~;kus ;k i;ZVu m|ksxkpk vaxhdkj d:u vkfFkZd ifjorZu ?kMowu vk.kys ikfgts- R;klkBh ik;kHkwr lks;h lqfo/kk mHkkj.khdMs tk.khoiwoZd y{k fnys ikfgts- e

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जोगदंड, रमेश बापूराव. "मराठवाड्यातील पर्यटन उद्योगपुढील समस्या आणि उपाय योजना". Journal of Research & Development' 14, № 8 (2022): 1–2. https://doi.org/10.5281/zenodo.6988511.

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<strong>izLrkouk</strong>    vusd ns’kkr i;ZVu m|ksxkpk fodkl eksB~;k izek.kkr >kysyk fnlwu ;srks ,o<sp ukgh rj R;kaph vFkZO;oLFkk iw.kZi.ks i;ZVdkaojp vk/kkjhr vkgs] rlsp Hkkjrkrhy dkgh jkT;kph vFkZO;oLFkk v’kkp izdkjph vkgs- i;ZVu gk vk/kqfud txkrhy ,d izxr m|ksx vkgs- gtkjks yksd ;k O;olk;k’kh fuxMhr vkgsr- vusdkaP;k gkrkyk jkstxkj ns.;kps dke ;k i;ZVu m|ksxkus dsysys fnlwu ;srs- R;keqGs ejkBokM~;kus ;k i;ZVu m|ksxkpk vaxhdkj d:u vkfFkZd ifjorZu ?kMowu vk.kys ikfgts- R;klkBh ik;kHkwr lks;h lqfo/kk mHkkj.khdMs tk.khoiwoZd y{k fnys ikfgts- ejkBokM~;krhy

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Xie, Jiang, Dongfang Lu, Jiaxin Li, et al. "Kernel differential subgraph reveals dynamic changes in biomolecular networks." Journal of Bioinformatics and Computational Biology 16, no. 01 (2018): 1750027. http://dx.doi.org/10.1142/s0219720017500275.

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Many major diseases, including various types of cancer, are increasingly threatening human health. However, the mechanisms of the dynamic processes underlying these diseases remain ambiguous. From the holistic perspective of systems science, complex biological networks can reveal biological phenomena. Changes among networks in different states influence the direction of living organisms. The identification of the kernel differential subgraph (KDS) that leads to drastic changes is critical. The existing studies contribute to the identification of a KDS in networks with the same nodes; however,

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46

Johnston, Alexis, and Adegboyega K. Oyelere. "Abstract 4492: Deferiprone optimization for the treatment of triple-negative breast cancer." Cancer Research 84, no. 6_Supplement (2024): 4492. http://dx.doi.org/10.1158/1538-7445.am2024-4492.

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Abstract Triple-negative breast cancer (TNBC) is the leading cause of new cancer cases and the second leading cause of cancer deaths in American women disproportionately affecting Black and Hispanic women under 40. Currently, there is no targeted therapy for TNBC and treatment options to manage this lethal disease include surgery, adjuvant chemotherapy and radiotherapy. Among the chemotherapy agents, combination of the PARP inhibitors with DNA-damaging results in a more promising anti-tumor effect. A better understanding of TNBC etiology has aided in unraveling the roles of two additional cell

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47

Marandino, C. A., W. J. De Bruyn, S. D. Miller, and E. S. Saltzman. "Open ocean DMS air/sea fluxes over the eastern South Pacific Ocean." Atmospheric Chemistry and Physics Discussions 8, no. 3 (2008): 12081–114. http://dx.doi.org/10.5194/acpd-8-12081-2008.

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Abstract. Air/sea fluxes of dimethylsulfide (DMS) were measured by eddy correlation over the Eastern South Pacific Ocean during January 2006. The cruise track extended from Manzanillo, Mexico, along 110° W, to Punta Arenas, Chile. Bulk air and surface ocean DMS levels were also measured and gas transfer coefficients (kDMS) were computed. Air and seawater DMS measurements were made using chemical ionization mass spectrometry (API-CIMS) and a gas/liquid membrane equilibrator. Mean surface seawater DMS concentrations were 3.8±2.2 nM and atmospheric mixing ratios were 340±370 ppt. The air/sea flux

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Shen, Zhenhua, Lin Huang, Suyu Jin, and Yucai Zheng. "Cloning and Expression Analysis of Two Kdm Lysine Demethylases in the Testes of Mature Yaks and Their Sterile Hybrids." Animals 10, no. 3 (2020): 521. http://dx.doi.org/10.3390/ani10030521.

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The objective of this study was to explore the molecular mechanism for male sterility of yak hybrids based on two demethylases. Total RNA was extracted from the testes of adult yaks (n = 10) and yak hybrids (cattle–yaks, n = 10). The coding sequences (CDS) of two lysine demethylases (KDMs), KDM1A and KDM4B, were cloned by RT-PCR. The levels of KDM1A and KDM4B in yaks and cattle–yaks testes were detected using Real-time PCR and Western blotting for mRNA and protein, respectively. In addition, the histone methylation modifications of H3K36me3 and H3K27me3 were compared between testes of yaks and

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Pullen, J. K., M. D. Tallquist, R. W. Melvold, and L. R. Pease. "Recognition of a single amino acid change on the surface of a major transplantation antigen is in the context of self peptide." Journal of Immunology 152, no. 7 (1994): 3445–52. http://dx.doi.org/10.4049/jimmunol.152.7.3445.

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Abstract The transcripts encoding two strongly alloantigenic class I mutant molecules, Kdm4 and Kdm5, were characterized and found to encode products that differ from the parental Kd glycoprotein by single amino acid substitutions. The Kdm4 molecule has an amino acid change at position 114, an integral component of a beta-sheet associated with pockets D and E of the peptide binding site. The basis for strong alloantigenicity of the variant molecule can be attributed to differences in peptide binding that were visualized by HPLC analysis of eluted peptides. In contrast, the Kdm5 molecule differ

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Paoli, Antonio, Antonino Bianco, Tatiana Moro, Joao Felipe Mota, and Christianne de Faria Coelho-Ravagnani. "The Effects of Ketogenic Diet on Insulin Sensitivity and Weight Loss, Which Came First: The Chicken or the Egg?" Nutrients 15, no. 14 (2023): 3120. http://dx.doi.org/10.3390/nu15143120.

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The ketogenic diet (KD) is, nowadays, considered an interesting nutritional approach for weight loss and improvement in insulin resistance. Nevertheless, most of the studies available in the literature do not allow a clear distinction between its effects on insulin sensitivity per se, and the effects of weight loss induced by KDs on insulin sensitivity. In this review, we discuss the scientific evidence on the direct and weight loss mediated effects of KDs on glycemic status in humans, describing the KD’s biochemical background and the underlying mechanisms.

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