SER100 / Serodus - LARVOL DELTA

A case report of Maturity Onset Diabetes of the young type 3 in a young female and her mother. Implications of genetic diagnosis. (ESPE-ESE 2025) - "She was initially commenced on a long-acting insulin (degludec) and placed on a continues glucose monitor (CGM)...Treatment changed to gliclazide 30mg by mouth once daily and Three months after HbA1c was 6.7%...She was placed on different regimens without improvement most recently she was on metformin plus empagliflozin (5/1000mg daily) and semaglutide (1mg per week)...If a case is suspicious a genetic test is guaranteed as monogenic diabetes has different therapeutic approach. For our patient further genetic evaluation is necessary considering her mother results."

Case report • Clinical • Late-breaking abstract • Diabetes • Diabetic Nephropathy • Genetic Disorders • Gestational Diabetes • Hepatology • Metabolic Disorders • Nephrology • Polycystic Kidney Disease • Renal Disease • Type 1 Diabetes Mellitus • Type 2 Diabetes Mellitus • HNF1A

Dynamics, mechanistic and energetic evaluation of thiazole-thiadiazole compounds in flavin dependent thymidylate synthase of Mycobacterium tuberculosis. (PubMed, Int J Biol Macromol) - "Free energy landscape (FEL) analysis shows rapid stabilization in ligand-bound states. Compound 5l stands out due to its favourable pharmacokinetic properties and safety, making it a promising candidate for anti-tuberculosis drug development."

Journal • Infectious Disease • Pulmonary Disease • Respiratory Diseases • Tuberculosis • TYMS

Calibration in terms of activity per unit volume of the stack monitor at a PET cyclotron centre using Monte Carlo technique (EANM 2024) - "A simple and relatively inexpensive stack monitor may be sufficient in many cyclotron PET centres. Monte Carlo simulation techniques allow the detectors to be calibrated with satisfactory accuracy, even under "bad geometry" conditions."

Application of Pt-M/ZSM-22-PHTS catalyst in n-heptane hydroisomerization (ACS-Fall 2024) - "Figure 1. TEM images of series catalysts: (a) Pt-Co/ZP-120; (b) Pt-Mo/ZP-120; (c) Pt-Zn/ZP-120; (d) Pt-Ni/ZP-120; (e) Pt-Cr/ZP-120; and STEM-EDS elemental analysis photos of Pt-Mo/ZP-120"

Structure of the human outer kinetochore KMN network complex. (PubMed, Nat Struct Mol Biol) - "Ser100 and Ser109 of the N-terminal segment of the MIS12C subunit Dsn1, two key targets of Aurora B kinase, directly stabilize this auto-inhibition. Our study indicates how selectively relieving this auto-inhibition through Ser100 and Ser109 phosphorylation might restrict outer kinetochore assembly to functional centromeres during cell division."

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Studies on the interaction mechanism between xanthine oxidase and osmundacetone: Molecular docking, multi-spectroscopy and dynamical simulation. (PubMed, Spectrochim Acta A Mol Biomol Spectrosc) - "Molecular docking studies showed that osmundacetone was inserted into the Mo-Pt center and interacted with hydrophobic residues of Phe911, Gly913, Phe914, Ser1008, Phe1009, Thr1010, Val1011, and Ala1079 of XO. In summary, these findings suggest that provide theoretical basis for the research and development of XO inhibitors from Inonotus obliquus."

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"Sending some ❤️to some of my favorite women scientists @karynotype @ClaireAldridge2 @joana_damas @cmfraser10000 @eenork @KizzyPhD" (@bcantarel)

Supplementation With Zinc Proteinate Increases the Growth Performance by Reducing the Incidence of Diarrhea and Improving the Immune Function of Dairy Calves During the First Month of Life. (PubMed, Front Vet Sci) - "In Experiment 2, compared with the CON group, ZP increased the ADG (P < 0.01), serum zinc concentration (P < 0.01), and plasma immunoglobulin G (IgG; P < 0.01) and IgM (P < 0.01) concentrations, but reduced the incidence of diarrhea (P < 0.01), serum malondialdehyde (P < 0.01), and plasma interleukin-1β (P < 0.01) concentrations during days 1-28. Overall, ZP supplementation to yield 80 mg zinc/day improves the growth performance and immune function, and decrease the incidence of diarrhea of dairy calves, which was comparable to the same dose of zinc in the form of ZM."

Journal • IL1B

Pancancer Analyses Reveal Genomics and Clinical Characteristics of the SETDB1 in Human Tumors. (PubMed, J Oncol) - "SETDB1 is an important oncogene involved in tumorigenesis and tumor progression through different biological mechanisms. Furthermore, SETDB1 may be a potential therapeutic target for cancer treatment."

IO biomarker • Journal • Pan tumor • Immune Modulation • Inflammation • Oncology • Solid Tumor • SETDB1

CYP2C8-Mediated Formation of a Human Disproportionate Metabolite of the Selective Na1.7 Inhibitor DS-1971a, a Mixed Cytochrome P450 and Aldehyde Oxidase Substrate. (PubMed, Drug Metab Dispos) - "We clearly demonstrate that DS-1971a, a mixed aldehyde oxidase and cytochrome P450 substrate, was predominantly metabolized by CYP2C8 to form M1, a human disproportionate metabolite. Species differences in the formation of M1 highlight the regio- and stereoselective metabolism by CYP2C8, and the proposed interaction between DS-1971a and CYP2C8 provides new knowledge of CYP2C8-mediated metabolism of cyclohexane-containing substrates."

Journal • CYP2C8

Inhibition of multiple SARS-CoV-2 proteins by an antiviral biomolecule, seselin from Aegle marmelos deciphered using molecular docking analysis. (PubMed, J Biomol Struct Dyn) - "The results suggested that the seselin had inhibitory potential over multiple SARS-COV-2 targets and hold a high potential to work effectively as a novel drug for COVID-19 if evaluated in experimental setups in the foreseeable future. Communicated by Ramaswamy H. Sarma."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

The Chk2-PKM2 axis promotes metabolic control of vasculogenic mimicry formation in p53-mutated triple-negative breast cancer. (PubMed, Oncogene) - "Its activation by DNA-damaging agents such as cisplatin, etoposide, and DPT reduces VM formation. P-PKM2 S100 reduces VM formation by decreasing glucose flux, and the PKM2 S100A mutation abolishes the inhibition of glucose flux and VM formation induced by Chk2 activation. Overall, this study proposes a novel strategy of VM suppression through Chk2 induction, which prevents PKM2-mediated glucose flux in p53-mutated TNBC."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CHEK2 • TP53

Sex-specific expression mechanism of hepatic estrogen inactivating enzyme and transporters in diabetic women. (PubMed, Biochem Pharmacol) - "For the sulfotransferase gene, phosphorylated nuclear receptors ERα and RORα, at Ser212 and Ser100, respectively, bind their response elements to activate the SULT1E1 promoter in women. This coordinated increase in estrogen inactivation and excretion, and the phosphorylated nuclear receptor-mediated gene activation could be a defense mechanism against toxicities of estrogens through inactivation and excretion in the livers of women."

Clinical • Journal • Diabetes • Hepatology • Metabolic Disorders • Type 2 Diabetes Mellitus • ABCG2 • SULT1E1

CaMKK2 is inactivated by cAMP-PKA signaling and 14-3-3 adaptor proteins. (PubMed, J Biol Chem) - "We also report the crystal structure of 14-3-3ζ bound to a synthetic diphosphorylated peptide that reveals how the canonical (Ser511) and non-canonical (Ser100) 14-3-3 consensus sites on CaMKK2 co-operate to bind 14-3-3 proteins. Our findings provide detailed molecular insights into how cAMP-PKA signaling inactivates CaMKK2 and reveals a pathway to inhibit CaMKK2 with potential for treating human diseases."

Journal • Gastrointestinal Cancer • Genito-urinary Cancer • Hepatocellular Cancer • Hepatology • Metabolic Disorders • Oncology • Prostate Cancer • Solid Tumor

RORα Phosphorylation by Casein Kinase 1α as Glucose Signal to Regulate Estrogen Sulfation in Human Liver Cells. (PubMed, Biochem J) - "During these dynamic processes, both RORα and HNF4α remain on the enhancer. Thus, RORα utilizes phosphorylation to integrate HNF4α and transduces the glucose signal to regulate the SULT1E1 gene in HepG2 cells and this phosphorylation-mediated mechanism may also regulate SULT1E1 expressions in the human liver."

Journal • Diabetes • Gastrointestinal Cancer • Hepatocellular Cancer • Liver Cancer • Solid Tumor • SULT1E1

Exome sequence analysis in consanguineous Pakistani families inheriting Bardet-Biedle syndrome determined founder effect of mutation c.299delC (p.Ser100Leufs*24) in BBS9 gene. (PubMed, Mol Genet Genomic Med) - "We speculate the evolutionary significance of this mutation and assume its strong founder effect in the Khaisoori tribe of D.I.Khan. Based on these findings, we suggest developing a molecular diagnostic test that may be used for premarital and prenatal screening of families at risk of BBS."

Journal • Bardet–Biedl Syndrome • Developmental Disorders • Genetic Disorders • Inherited Retinal Dystrophy • Mental Retardation • Obesity • Ophthalmology • Renal Disease • Retinal Disorders

The genetic profile of dysferlinopathy in a cohort of 209 cases: genotype-phenotype relationship and a hotspot on the inner DysF domain. (PubMed, Hum Mutat) - "In the analysis of missense variants, p.Trp992Arg, p.Trp999Arg, p.Trp999Cys, p.Ser1000Phe, p.Arg1040Trp and p.Arg1046His were located in the inner DysF domain, representing in 113/160 missense variants (70.6%). This large cohort highlighted the frequent missense variants located in the inner DysF domain as a hotspot for missense variants among our cohort of 209 cases (>95%, Japanese) and hinted at their potential as targets for future therapeutic strategies."

Clinical • Journal • Genetic Disorders • Muscular Dystrophy

Ser 100 phosphorylated RORα orchestrates CAR and HNF4α to form active chromatin complex in response to phenobarbital to regulate induction of CYP2B6. (PubMed, Mol Pharmacol) - "Here, we show that RORα, through phosphorylated S100 residue, orchestrated CAR-HNF4α interaction on the CYP2B6 promoter in human primary hepatocyte cultures. These results signify not only the role RORα in the molecular process of CYP2B6 induction, but it also reveals the importance of conserved phosphorylation site within the DBD of the receptor."

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Molecular Docking and Molecular Dynamics (MD) Simulation of Human Anti-Complement Factor H (CFH) Antibody Ab42 and CFH Polypeptide. (PubMed, Int J Mol Sci) - "In conclusion, this study has explored the mechanism of interaction between Ab42 antibody and its targeted antigen by both theoretical and experimental analysis. Our results have important theoretical significance for the design and development of relevant antibody drugs."

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NOP-Targeted Peptide Ligands. (PubMed, Handb Exp Pharmacol) - "Moreover, recent findings suggest the possibility to apply different multimerization strategies for the realization of multi-target NOP/opioid receptor ligands or tetrabranched N/OFQ derivatives with extraordinarily prolonged duration of action in vivo. The diverse approaches led to the identification of important pharmacological tools along with drug candidates currently in clinical development such as Rec 0438 (aka UFP-112) for the treatment of overactive bladder and SER 100 (aka ZP120) for the clinical management of systolic hypertension."

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