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  • ||||||||||  Journal:  Activation of polyamine catabolism promotes glutamine metabolism and creates a targetable vulnerability in lung cancer. (Pubmed Central) -  Mar 25, 2024   
    Importantly, pharmacological inhibition of either one of glutamine transport, glutaminase, or GSH biosynthesis in combination with activation of polyamine catabolism synergistically suppresses lung cancer cell growth and xenograft tumor formation. Together, this study unveils a previously unappreciated functional interconnection between polyamine catabolism and glutamine metabolism and establishes cotargeting strategies as potential therapeutics in lung cancer.
  • ||||||||||  Preclinical, Journal:  Immunohistochemical properties of motoneurons supplying the porcine trapezius muscle. (Pubmed Central) -  Mar 25, 2024   
    The retrogradely labelled neurons were closely apposed by nerve fibres expressing immunoreactivity to CHAT, VACHT, CGRP, SP, D?H, VIP, n-NOS, NPY, GAL, Leu-Enk and Met-Enk. Taking into account the clinical relevance of TRAP, the present results may be useful in designing further research aimed at the management of various dysfunctions of the muscle.
  • ||||||||||  NEO2734 / Epigenetix, inobrodib (CCS1477) / CellCentric
    Review, Journal:  Characteristics of anticancer activity of CBP/p300 inhibitors - Features of their classes, intracellular targets and future perspectives of their application in cancer treatment. (Pubmed Central) -  Mar 23, 2024   
    However, none of the described inhibitors is perfectly specific to CBP/p300 since they share similarity of a key functional domains with other enzymes, which are critically associated with cancer progression and their antagonists demonstrate remarkable clinical efficacy in cancer therapy. Therefore, we revise the possible and clinically relevant off-targets of CBP/p300 inhibitors that can be blocked simultaneously with CBP/p300 thereby improving the anticancer potential of CBP/p300 inhibitors and pharmacokinetic predicting data such as absorption, distribution, metabolism, excretion (ADME) and toxicity.
  • ||||||||||  Journal:  The balance between nuclear import and export of NLRC5 regulates MHC class I transactivation. (Pubmed Central) -  Mar 23, 2024   
    In this study, a comprehensive analysis of all domains in NLRC5 revealed that the regulatory mechanisms for nuclear import and export of NLRC5 coexist and counterbalance each other. Moreover, GCN5 (general control non-repressed 5 protein), a member of HATs (histone acetyltransferases), was found to be a key player to retain NLRC5 in the nucleus, thereby contributing to the expression of MHC class I. Therefore, the balance between import and export of NLRC5 has emerged as an additional regulatory mechanism for MHC class I transactivation, which would be a potential therapeutic target for the treatment of cancer and virus-infected diseases.
  • ||||||||||  Journal:  Peripheral neuronal activation shapes the microbiome and alters gut physiology. (Pubmed Central) -  Mar 22, 2024   
    Physiologically, activation of either ChAT+ or TH+ neurons increases fecal output, while only ChAT+ activation results in increased colonic contractility and diarrhea-like fluid secretion. These findings suggest that specific subsets of peripherally activated neurons differentially regulate the gut microbiome and GI physiology in mice without involvement of signals from the brain.
  • ||||||||||  Journal:  Disease-associated astrocyte epigenetic memory promotes CNS pathology. (Pubmed Central) -  Mar 21, 2024   
    In summary, these studies define an epigenetically controlled memory astrocyte subset that promotes CNS pathology in EAE and, potentially, multiple sclerosis. These findings may guide novel therapeutic approaches for multiple sclerosis and other neurologic diseases.
  • ||||||||||  paclitaxel / Generic mfg.
    Journal:  Biosynthesis of the highly oxygenated tetracyclic core skeleton of Taxol. (Pubmed Central) -  Mar 20, 2024   
    After identifying a acetyltransferase catalyzing the formation of C7-OAc, the pathway producing the highly-oxygenated 1?-dehydroxybaccatin VI with the Taxol tetracyclic core skeleton is elucidated and its complete biosynthesis from taxa-4(20),11(12)-diene-5?-ol is achieved in an engineered yeast. These systematic studies lay the foundation for the complete elucidation of the biosynthetic pathway of Taxol.
  • ||||||||||  Journal:  Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain. (Pubmed Central) -  Mar 20, 2024   
    Our study demonstrates that engagement of Cereblon (CRBN) and a sufficiently long linker between the E3 and CBP/EP300 binders (?21 atoms) are required for PROTAC-mediated degradation using CPI-1612 resulting in a new active PROTAC dCE-1. Lessons learned from this campaign, particularly the importance of cell-based assays to understand the reasons underlying PROTAC performance, are likely applicable to other targets to assist the development of degraders.
  • ||||||||||  trichostatin A (VTR-297) / Vanda
    Journal:  NS1-mediated enhancement of MVC transcription and replication promoted by KAT5/H4K12ac. (Pubmed Central) -  Mar 20, 2024   
    In the current study, we found the histone deacetylase (HDAC) inhibitor, trichostatin A (TSA), promoted the replication and transcription of parvovirus minute virus of canines (MVC)...This study illustrated that histone acetylation status is important for MVC replication and transcription and revealed a novel mechanism that the viral nonstructural protein NS1 hijacks the host acetyltransferase KAT5 to enhance histone acetylation of H4K12ac, which relies on a potential tyrosine phosphorylation site, Y44 in KAT5. Other parvoviruses share a similar genome organization and coding potential and may adapt a similar strategy for efficient viral replication and transcription.
  • ||||||||||  Journal:  Tau induces inflammasome activation and microgliosis through acetylating NLRP3. (Pubmed Central) -  Mar 19, 2024   
    Other parvoviruses share a similar genome organization and coding potential and may adapt a similar strategy for efficient viral replication and transcription. In conclusion, our findings provide evidence for a novel role of Tau in the regulation of microglia activation through acetylating NLRP3, which has potential implications for early intervention and personalised treatment of AD and related Tauopathies.
  • ||||||||||  Natesto (testosterone) / Acerus, Medac, Aytu BioPharma
    Journal:  Acetylation of transcription factor BpTCP20 by acetyltransferase BpPDCE23 modulates salt tolerance in birch. (Pubmed Central) -  Mar 19, 2024   
    Chromatin immunoprecipitation sequencing showed that BpTCP20 binds to NeuroD1, T-box, and two unknown elements (termed TBS1 and TBS2) to regulate target genes...In addition, we identified dihydrolipoyllysine-residue acetyltransferase component of pyruvate dehydrogenase complex (BpPDCE23), an acetyltransferase that interacts with and acetylates BpTCP20 to enhance its binding to DNA motifs. Together, these results suggest that BpTCP20 is a transcriptional regulator of salt tolerance, whose activity is modulated by BpPDCE23-mediated acetylation.
  • ||||||||||  Journal, IO biomarker, Epigenetic controller:  Electroacupuncture regulates histone acetylation of Bcl-2 and Caspase-3 genes to improve ischemic stroke injury. (Pubmed Central) -  Mar 19, 2024   
    However, the Histone Acetyltransferase inhibitor (HATi) treatment reversed these effects. Our data demonstrated that EA mediated the expression levels of Bcl-2 and caspase-3 in MCAO rats by regulating the occupancy of acetylated H3K9/H3K27 at the promoters of these two genes, thus exerting a cerebral protective effect in ischemic reperfusion (I/R) injury.
  • ||||||||||  Journal:  Polyamine Dysregulation and Nucleolar Disruption in Alzheimer's Disease. (Pubmed Central) -  Mar 15, 2024   
    This Alu competition leads to loss of nucleolar integrity with leaking of nucleolar polyamines that cause aggregation of phosphorylated tau. The hypothesis was developed with key word searches (e.g., PubMed) using relevant terms (e.g., Alzheimer's, lupus, nucleolin) based on a systems biology approach and exploring autoimmune disease tautology, gaining synergistic insights from other diseases.
  • ||||||||||  Review, Journal:  The Protein Acetylation after Traumatic Spinal Cord Injury: Mechanisms and Therapeutic Opportunities. (Pubmed Central) -  Mar 15, 2024   
    Furthermore, we discuss inhibitors and activators targeting acetylation-related enzymes, such as ?-tubulin acetyltransferase 1 (?TAT1), histone deacetylase 6 (HDAC6), and sirtuin 2 (SIRT2), to provide promising opportunities for recovery from SCI. In conclusion, a comprehensive understanding of protein acetylation and deacetylation in SCI may contribute to the development of SCI treatment.
  • ||||||||||  aspirin / Generic mfg.
    Journal:  Aspirin-Mediated Acetylation of SIRT1 Maintains Intestinal Immune Homeostasis. (Pubmed Central) -  Mar 14, 2024   
    Moreover, the knock-in mice of the acetylation-mimic mutant of SIRT1 show the decreased production of pro-inflammatory cytokines and maintain intestinal immune homeostasis. The study indicates the importance of the acetylated internal functional site of SIRT1 in maintaining intestinal immune homeostasis.
  • ||||||||||  Journal:  The autonomic nerves around the vein of Marshall: a (Pubmed Central) -  Mar 12, 2024   
    Interstitial fibrosis increased with age and heart weight was associated with AF and cardiovascular cause of death. This study increases our understanding of the cardiac autonomic innervation in the VOM area in various diseases, offering implications for the development of new therapeutic approaches targeting the autonomic nervous system.
  • ||||||||||  Synthesis of quinoline derivatives as multi-target agents for the treatment of Alzheimer's disease | Poster Board #1726 (In-person; Poster Board #1726; Hall C (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_2974;    
    Our data from the PAMPA assay shows that the presence of an alkyl amino side chain favors the membrane permeability of these compounds. Further research will include testing our most promising PDE5/HAT dual target molecule for the ability to induce biochemical changes including cGMP and HAT acetylation levels in the hippocampus of treated mice.
  • ||||||||||  Review, Journal:  Histone lysine acetyltransferase inhibitors: an emerging class of drugs for cancer therapy. (Pubmed Central) -  Mar 11, 2024   
    Additionally, new chemically induced proximity approaches are presented, offering opportunities for unique target selectivity profiles and tissue-specific targeting of KATs. Emerging clinical data for CREB binding protein (CREBBP)/EP300 BRD inhibitors and KAT6 catalytic inhibitors indicate the promise of this target class in cancer therapeutics.