Abstract：
:This work describes the chemical synthesis, combinatorial selection, and enzymatic evaluation of peptidomimetic fluorescent substrates specific for the trypsin-like (β2) subunit of the 20S human proteasome. After deconvolution of a library comprising nearly 6000 compounds composed of peg substituted diaminopropionic acid DAPEG building blocks, the sequence ABZ-Dap(O2(Cbz))-Dap(GO1)-Dap(O2(Cbz))-Arg-ANB-NH2, where ABZ is 2-aminobenzoic acid, and ANB- 5 amino 2- nitro benzoic acid was selected. Its cleavage followed sigmoidal kinetics, characteristic for allosteric enzymes, with Km = 3.22 ± 0.02 μM, kcat = 245 s-1, and kcat/Km = 7.61 × 107 M-1 s-1. This process was practically halted when a selective inhibitor of the β2 subunit of the 20S human proteasome was supplemented to the reaction system. Titration of the substrate resulting in decreased amounts of proteasome 20S produced a linear signal up to 10-11 M. Using this substrate, we detected human proteasome 20S in human urine samples taken from the bladders of cancer patients. This observation could be useful for the noninvasive diagnosis of this severe disease.
journal_name
Int J Mol Scijournal_title
International journal of molecular sciencesauthors
Wysocka M,Romanowska A,Gruba N,Michalska M,Giełdoń A,Lesner Adoi
10.3390/ijms21072396subject
Has Abstractpub_date
2020-03-31 00:00:00issue
7issn
1422-0067pii
ijms21072396journal_volume
21pub_type
杂志文章abstract：:The rice leaf roller (Cnaphalocrocis medinalis) is one of the most destructive agricultural pests. Due to its migratory behavior, it is difficult to control worldwide. To date, little is known about major genes of C. medinalis involved in chitin metabolism and insecticide detoxification. In order to obtain a comprehen...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms160921873
更新日期：2015-09-10 00:00:00
abstract：:Increased platelet activation and apoptosis are characteristic of diabetic (DM) platelets, where a Parkin-dependent mitophagy serves a major endogenous protective role. We now demonstrate that Parkin is highly expressed in both healthy platelets and diabetic platelets, compared to other mitochondria-enriched tissues s...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21165869
更新日期：2020-08-15 00:00:00
abstract：:Spider silk is self-assembled from water-soluble silk proteins through changes in the environment, including pH, salt concentrations, and shear force. The N-terminal domains of major and minor ampullate silk proteins have been found to play an important role in the assembly process through salt- and pH-dependent dimer...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21124466
更新日期：2020-06-23 00:00:00
abstract：:Prostate cancer (PCa), an epithelial malignant tumor, is the second common cause of cancer death among males in western countries. Thus, the development of new strategies is urgently needed. Tanshinones isolated from Salvia miltiorrhiza and its synthetic analogs show various biological activities including anticancer ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20184459
更新日期：2019-09-10 00:00:00
abstract：:Traumatic brain injury (TBI) represents an important problem of global health. The damage related to TBI is first due to the direct injury and then to a secondary phase in which neuroinflammation plays a key role. NLRP3 inflammasome is a component of the innate immune response and different diseases, such as neurodege...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21176204
更新日期：2020-08-27 00:00:00
abstract：:The purpose of this study is to clinically validate a series of circulating miRNAs that distinguish between the 4 most prevalent tumor types (lung cancer (LC); breast cancer (BC); colorectal cancer (CRC); and prostate cancer (PCa)) and healthy donors (HDs). A total of 18 miRNAs and 3 housekeeping miRNA genes were eval...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21082783
更新日期：2020-04-16 00:00:00
abstract：:Class I and II histone deacetylases (HDAC) are considered important regulators of immunity and inflammation. Modulation of HDAC expression and activity is associated with altered inflammatory responses but reports are controversial and the specific impact of single HDACs is not clear. We examined class I and II HDACs ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21238943
更新日期：2020-11-25 00:00:00
abstract：:One of the most important adaptations of seagrasses during sea colonization was the capacity to grow at the low micromolar nitrate concentrations present in the sea. In contrast to terrestrial plants that use H+ symporters for high-affinity NO3- uptake, seagrasses such as Zostera marina L. use a Na+-dependent high-aff...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20153650
更新日期：2019-07-26 00:00:00
abstract：:Chitooligosaccharide (COS), which is acknowledged for possessing multiple functions, is a kind of low-molecular-weight polymer prepared by degrading chitosan via enzymatic, chemical methods, etc. COS has comprehensive applications in various fields including food, agriculture, pharmacy, clinical therapy, and environme...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms19082197
更新日期：2018-07-27 00:00:00
abstract：:Colorectal cancer (CRC) remains a serious health problem worldwide. Approximately half of patients will develop distant metastasis after CRC resection, usually with very poor prognosis afterwards. Because patient performance after distant metastasis surgery remains very heterogeneous, ranging from death within 2 years...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,评审
doi：10.3390/ijms21155255
更新日期：2020-07-24 00:00:00
abstract：:Recent studies have shown that plumbagin has anti-inflammatory, anti-allergic, antibacterial, and anti-cancer activities; however, it has not yet been shown whether plumbagin suppresses alpha-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis to prevent hyperpigmentation. In this study, we demonstrated t...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms18020320
更新日期：2017-02-03 00:00:00
abstract：:Hibernation is an effective energy conservation strategy that has been widely adopted by animals to cope with unpredictable environmental conditions. The liver, in particular, plays an important role in adaptive metabolic adjustment during hibernation. Mammalian studies have revealed that many genes involved in metabo...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms19082363
更新日期：2018-08-10 00:00:00
abstract：:Stable five-coordinate Pt(II) complexes have been highlighted as a promising and original platform for the development of new cytotoxic drugs. Their interaction with proteins has been scarcely studied. Here, the reactivity of the five-coordinate Pt(II) compound [Pt(I)(Me) (dmphen)(olefin)] (Me = methyl, dmphen = 2,9-d...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20030520
更新日期：2019-01-26 00:00:00
abstract：:Alzheimer's disease (AD), characterized by cognitive impairments, is considered to be one of the most widespread chronic neurodegenerative diseases worldwide. We recently introduced a novel therapeutic agent for AD treatment, the T-type calcium channel enhancer ethyl-8-methyl-2,4-dioxo-2-(piperidin-1-yl)-2H-spiro[cycl...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms22020741
更新日期：2021-01-13 00:00:00
abstract：:Sugars, which are important signaling molecules, regulate diverse biological processes in plants. However, the convergent regulatory mechanisms governing these physiological activities have not been fully elucidated. MODIFIER OF snc1-1 (MOS1), a modulator of plant immunity, also regulates floral transition, cell cycle...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21197095
更新日期：2020-09-26 00:00:00
abstract：:The treatment of metastatic breast cancer remained a challenge despite the recent breakthrough in the immunotherapy regimens. Here, we addressed the multidimensional immunophenotyping of 4T1 metastatic breast cancer by the state-of-the-art single cell mass cytometry (CyTOF). We determined the dose and time dependent c...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21010170
更新日期：2019-12-25 00:00:00
abstract：:Little is known of the adaptive immune response to subarachnoid hemorrhage (SAH). This study was the first to investigate whether T cell receptor (TCR) immune repertoire may provide a better understanding of T cell immunology in delayed cerebral ischemia (DCI). We serially collected peripheral blood in five SAH patien...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21093149
更新日期：2020-04-29 00:00:00
abstract：:In general, a drug candidate is evaluated using 2D-cultured cancer cells followed by an animal model. Despite successful preclinical testing, however, most drugs that enter human clinical trials fail. The high failure rates are mainly caused by incompatibility between the responses of the current models and humans. He...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms18112348
更新日期：2017-11-07 00:00:00
abstract：:Acetylation of nuclear apurinic/apyrimidinic endonuclease-1/redox factor-1 (APE1/Ref-1) is associated with its extracellular secretion, despite the lack of an N-terminal protein secretion signal. In this study, we investigated plasma membrane targeting and translocation of APE1/Ref-1 in HEK293T cells with enhanced ace...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20133178
更新日期：2019-06-28 00:00:00
abstract：BACKGROUND:This study aims to investigate: (a) the putative association between the presence of microcalcifications and the expression of both epithelial-to-mesenchymal transition and bone biomarkers, (b) the role of microcalcifications in the breast osteoblast-like cells (BOLCs) formation, and (c) the association betw...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20225633
更新日期：2019-11-11 00:00:00
abstract：:Detergent-resistant membranes (DRMs) microdomains, or "raft lipids", are key components of the plasma membrane (PM), being involved in membrane trafficking, signal transduction, cell wall metabolism or endocytosis. Proteins imbibed in these domains play important roles in these cellular functions, but there are few st...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21207694
更新日期：2020-10-17 00:00:00
abstract：:donor⁻acceptorDonor⁻acceptor⁻π⁻acceptor⁻donor (D1-A1-π-A2/A3-D2)-type small molecules, such TPA-MC-2 and TPA-MC-3, were designed and synthesized starting from donor-substituted alkynes (TPA-MC-1) via [2 + 2] cycloaddition-retroelectrocyclization reaction with tetracyanoethylene (TCNE) and 7,7,8,8-tetracyanoquinodimeth...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20071621
更新日期：2019-04-01 00:00:00
abstract：:Vascular cell adhesion molecule-1 (VCAM-1) is closely associated with tumor progression and metastasis. However, the relevance and role of VCAM-1 in lung cancer have not been clearly elucidated. In this study, we found that VCAM-1 was highly overexpressed in lung cancer tissue compared with that of normal lung tissue,...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms18030566
更新日期：2017-03-06 00:00:00
abstract：:Cyclin-dependent kinase 5 regulatory subunit 1 (CDK5R1) gene encodes for p35, the main activator of Cyclin-dependent kinase 5 (CDK5). The active p35/CDK5 complex is involved in numerous aspects of brain development and function, and its deregulation is closely associated to Alzheimer's disease (AD) onset and progressi...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms19072022
更新日期：2018-07-11 00:00:00
abstract：BACKGROUND:The peroxisome proliferator-activated receptors (PPARA, PPARG, PPARD) and their transcriptional coactivators' (PPARGC1A, PPARGC1B) gene polymorphisms have been associated with muscle morphology, oxygen uptake, power output and endurance performance. The purpose of this review is to determine whether the PPAR...
journal_title：International journal of molecular sciences
pub_type： 杂志文章,meta分析,评审
doi：10.3390/ijms19051472
更新日期：2018-05-15 00:00:00
abstract：:Treatment with 1-methylcyclopropylene (1-MCP) is an effective technique to preserve fruits, but inappropriate treatment with 1-MCP causes a ripening disorder (rubbery texture) in papaya fruit. In this study, a combined metabolomic and transcriptomic analysis was conducted to reveal the possible mechanism of the ripeni...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms22020916
更新日期：2021-01-18 00:00:00
abstract：:The renal cortex drives renal function. Hypoxia/reoxygenation are primary factors in ischemia-reperfusion (IR) injuries, but renal oxygenation per se is complex and awaits full elucidation. Few mathematical models address this issue: none captures cortical tissue heterogeneity. Using agent-based modeling, we develop t...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20246246
更新日期：2019-12-11 00:00:00
abstract：:Lupus nephritis (LN) is one of the most common and severe complications of lupus. However, the mechanisms for renal damage have not been well elucidated. There are evidences show that glomerular endothelial cells (GECs) are damaged in LN. Immune complexes can deposit in subendothelial area and could affect GEC functio...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms20215281
更新日期：2019-10-24 00:00:00
abstract：OBJECTIVES:Data on pregnancy long-term effects on multiple sclerosis (MS) course are still controversial; whether experiencing more than one pregnancy exposes one to risk of the disability's accrual is still unknown. We investigated differences existing in terms of disability progression among women with MS (wwMS) who ...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms17020234
更新日期：2016-02-12 00:00:00
abstract：:The applications of ZnO nanoparticles in agriculture have largely contributed to crop growth regulation, quality enhancement, and induction of stress tolerance, while the underlying mechanisms remain elusive. Herein, the involvement of melatonin synthesis and metabolism in the process of nano-ZnO induced drought toler...
journal_title：International journal of molecular sciences
pub_type： 杂志文章
doi：10.3390/ijms21030782
更新日期：2020-01-25 00:00:00
