Abstract：
:Pepstatin is a low molecular weight, potent inhibitor specific for acid proteases with a Ki value of about 10(-10)M for pepsin. The chemical structure of pepstatin is essentially a hexapeptide which contains two residues of an unusual amino acid, 4-amino-3-hydroxy-6-methylheptanoic acid (statine). The complete structure of pepstatin is isovaleryl-L-valyl-L-valyl-statyl-L-alanyl-statine. To study its mode of inhibition, we prepared several derivatives and measured their kinetics of inhibition. Both N-acetyl-statine and N-acetyl-alanyl-statine are competitive inhibitors for pepsin with Ki values of 1.2 x 10(-4)M and 5.65 x 10(-6)M, respectively. The Ki value for N-acetyl-valyl-statine is 4.8 x 10(-6)M. These statyl derivatives, therefore, are very strong inhibitors. The Ki value for N-acetyl-statine is 600-fold smaller than that of its structural analog N-acetyl-leucine. The derivative which contains two statyl residues in a tetrapeptide exhibits inhibitory properties which approach those of pepstatin itself. Other acid proteases, human pepsin, human gastricsin, renin, cathepsin D, the acid protease from R. chinensis and bovine chymosin, also are inhibited by pepstatin and its derivatives. We suggest that the statyl residue is responsible for the unusual inhibitory capability of pepstatin and that statine is an analog of the previously proposed transition state for catalysis by pepsin and other acid proteases.
journal_name
Adv Exp Med Bioljournal_title
Advances in experimental medicine and biologyauthors
Marciniszyn J Jr,Hartsuck JA,Tang Jdoi
10.1007/978-1-4757-0719-9_12subject
Has Abstractpub_date
1977-01-01 00:00:00pages
199-210eissn
0065-2598issn
2214-8019journal_volume
95pub_type
杂志文章abstract：:Expression levels of five miRNAs (miR-19b, miR-21, miR-126, miR-141, miR-205) were measured in the plasma of healthy donors and prostate cancer patients. It was shown that miR-141 expression level efficiently discriminates early stage prostate cancer patients and correlates with the Gleason score. ...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-3-319-42044-8_2
更新日期：2016-01-01 00:00:00
abstract：:This chapter represents a summary of the findings from the Yersinia enterocolitica strain 8081 whole genome sequence and the associated microarray analysis. Section 1 & 2 provide an introduction to the species and an overview of the general features of the genome. Section 3 identifies important regions within the geno...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-0-387-72124-8_1
更新日期：2007-01-01 00:00:00
abstract：:In summary, we present a list of phage clones we have obtained from rat genomic libraries (from lamba SC1 to lambda SC31, lambda WC1 and lambda WC40) together with cDNA clones we have obtained from a rat brain cDNA library (PRCM1,5,3 and 4). pRCM5 corresponds to 4.0 kb mRNA species observed primarily in skeletal muscl...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4684-5679-0_24
更新日期：1989-01-01 00:00:00
abstract：:The cerebral tissue oxygenation index (TOI) and fractional tissue oxygen extraction (FTOE) reflect the cerebral oxygenation. We studied the effect of glycaemia on the TOI and FTOE, as measured by near-infrared-spectroscopy (NIRS). We continuously measured TOI, glycaemia, mean arterial blood pressure (MABP), saturation...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4419-1241-1_66
更新日期：2010-01-01 00:00:00
abstract：:Olfaction is a unique sensory modality. Odor molecules reach olfactory receptors by inspiration, and odor information projects directly to limbic structures not through the thalamus. Odor stimuli thus induce respiratory changes, and simultaneously induce emotion and memory recognition via stimulation of olfactory-rela...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4419-5692-7_71
更新日期：2010-01-01 00:00:00
abstract：:Immune responses are controlled by the optimal balance between protective immunity and immune tolerance. T-cell receptor (TCR) signals are modulated by co-signaling molecules, which are divided into co-stimulatory and co-inhibitory molecules. By expression at the appropriate time and location, co-signaling molecules p...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-981-32-9717-3_2
更新日期：2019-01-01 00:00:00
abstract：:Cancer development originates in a single mutant cell transformed from a normal cell, including further evolution of pro-tumor cells through additional mutations into malignant cancer tissues. Data from recent studies, however, suggest that most pro-tumor cells do not develop into tumors but remain dormant within or a...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-3-030-23629-8_5
更新日期：2019-01-01 00:00:00
abstract：:Dopamine (DA) and noradrenaline (NA) were measured in the rabbit carotid body (CB) in vitro bv HPLC-ED under the following experimental conditions: 1h superfusion in normoxic, hypoxic (10% O2 in N2) or hypercapnic (8% CO2, 20% O2, 72% N2) medium, 5h superfusion in normoxia or hypoxia. The contents of DA and NA were de...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4615-2966-8_26
更新日期：1993-01-01 00:00:00
abstract：:The first step that precedes hematopoietic transplantation is elimination of pathological hematopoiesis by administration of myeloablative doses of radiochemotherapy. This eliminates hematolymphopoietic cells and at the same time damages hematopoietic microenvironment in bone marrow (BM). The damage of BM tissue leads...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4614-4118-2_15
更新日期：2013-01-01 00:00:00
abstract：:EPEC Escherichia coli are an important cause of epidemic diarrhea in infants. The disease is characterized by attaching and effacing (A/E) lesions where the bacteria attach intimately to the enterocyte surface resulting in localized destruction of microvilli. A 35-kb chromosomal locus termed LEE (locus of enterocyte e...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4899-1828-4_36
更新日期：1997-01-01 00:00:00
abstract：:Inositol 1,4,5-trisphosphate receptors (IP3Rs) are ubiquitously expressed intracellular ligand-gated Ca2+ channels present on the endoplasmic reticulum of virtually all eukaryotic cells. These channels mediate the Ca2+ release from intracellular stores in response to activation by the signaling molecule IP3, which fun...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-3-319-55858-5_6
更新日期：2017-01-01 00:00:00
abstract：:To investigate whether altered renal medullary prostaglandin (PG) synthesis is involved in the development of hypertension in spontaneously hypertensive rats (SHR), we compared the capacity of PGE2 synthesis in cultured renal papillary collecting tubule cells from young (4-week-old) and aged (16-week-old) SHR and cont...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4615-9546-5_83
更新日期：1989-01-01 00:00:00
abstract：:Extracellular free sodium (Na+)o and calcium (Ca2+)o concentration changes were measured in the rat motor cortex, using ion-selective microelectrodes. During ionophoretic applications of excitatory amino acids, decreases in (Na2+)o and in (Ca2+)o were observed. Ca2+ signals were not or very little modified by applicat...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4684-7971-3_33
更新日期：1986-01-01 00:00:00
abstract：:This review discusses new developments in Förster resonance energy transfer (FRET) microscopy and its application to cellular receptors. The method is based on the kinetic theory of FRET, which can be used to predict FRET not only in dimers, but also higher order oligomers of donor and acceptor fluorophores. Models ba...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/5584_2018_297
更新日期：2019-01-01 00:00:00
abstract：:The synapse between the inner hair cells (IHCs) and the spiral ganglion neurons (SGNs) in mammalian cochleae is characterized as having presynaptic ribbons and therefore is called ribbon synapse. The special molecular organization is reviewed in this chapter in association with the functional feature of this synapse i...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-981-13-6123-4_3
更新日期：2019-01-01 00:00:00
abstract：:Prostate cancer causes significant morbidity in men and metastatic disease is a major cause of cancer related deaths. Prostate metastasis is controlled by various cellular intrinsic and extrinsic factors, which are often under the regulatory control of various metastasis-associated genes. Given the dynamic nature of m...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-3-319-95693-0_5
更新日期：2018-01-01 00:00:00
abstract：:Arsenic (As) exposure has a toxic effect on the central nervous system, especially on learning and memory. Norepinephrine (NE), dopamine (DA), and serotonin (5-HT) play an important role in learning and memory function of the brain. In the present study, the protective effect of taurine on the disturbed biogenic amine...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4614-6093-0_26
更新日期：2013-01-01 00:00:00
abstract：:Angiogenesis, the process by which new blood vessels are formed from preexisting vessels, is essential for growth and progression of solid tumors. A number of growth factors regulate angiogenesis, but vascular endothelial growth factor (VEGF) is the most important. Activation of the VEGF pathway triggers a range of si...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4020-5133-3_20
更新日期：2006-01-01 00:00:00
abstract：:The effect of caloric intake on tumor growth has been recognized for over 70 years. Inhibition of tumor growth depends primarily on the extent of caloric restriction, but tumor type, animal strain, and dietary composition all exert some influence. Caloric restriction is most effective when maintained during both initi...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4613-1835-4_7
更新日期：1986-01-01 00:00:00
abstract：:Biomembranes separate a live cell from its environment and keep it in an off-equilibrium, steady state. They contain both phospholipids and nonphospholipids, depending on whether there are phosphate groups in the headgroup regions. Cholesterol (CHOL) is one type of nonphospholipids, and one of the most abundant lipid ...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-3-030-04278-3_8
更新日期：2019-01-01 00:00:00
abstract：:Asthma is a heterogeneous inflammatory disease. Most patients respond to current standard of care, i.e., bronchodilators, inhaled glucocorticosteroids and other anti-inflammatory drugs, but in some adequate asthma control cannot be achieved with standard treatments. These difficult-to-treat patients would be the targe...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/5584_2016_29
更新日期：2016-01-01 00:00:00
abstract：:Fibroblast growth factors (FGFs) and their cognate receptors, FGF receptors (FGFRs), play critical roles in a variety of normal developmental and physiological processes. Numerous reports support a role for deregulation of FGF-FGFR signaling, whether it is at the ligand and/or receptor level, in tumor development and ...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4614-0887-1_12
更新日期：2012-01-01 00:00:00
abstract：:Although mitochondrial dysfunction, endoplasmic reticulum (ER) stress, and disrupted lipid and calcium (Ca2+) homeostasis are classically associated with both insulin resistance and β-cell dysfunction in type 2 diabetes mellitus (T2DM), the interplay between these metabolic stresses is less known. Both organelles inte...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-981-10-4567-7_13
更新日期：2017-01-01 00:00:00
abstract：:One of the key abnormalities of non-insulin-dependent diabetes mellitus (NIDDM) and related diseases of the "Metabolic Syndrome" is impaired insulin action (insulin resistance). Since skeletal muscle plays a major role in insulin-stimulated glucose uptake and whole-body energy expenditure, it is a central player in ca...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4899-1928-1_12
更新日期：1998-01-01 00:00:00
abstract：:Insulin-like growth factor 1 (IGF-1) is a key anabolic growth factor stimulating phosphatidylinositol 3-kinase (PI3K)/Akt signaling which is well known for regulating muscle hypertrophy. However, the role of IGF-1 in muscle atrophy is less clear. This review provides an overview of the mechanisms via which IGF-1 signa...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-981-13-1435-3_6
更新日期：2018-01-01 00:00:00
abstract：:High-field (500 MHz) proton NMR has been used to elucidate the primary and secondary structures of glycosphingolipids (GSLs). Using 2-D J-correlated spectroscopy (2-D SECSY) which establishes scalar couplings of protons, the monosaccharide composition, anomeric configuration and aglycon structures of a GSL can be esta...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4684-1200-0_8
更新日期：1984-01-01 00:00:00
abstract：:cDNA clones mapping within the first 2601 bases of the 3' end of the TGEV genome were sequenced completely or in part by the method of Maxam and Gilbert and open reading frames were examined. One reading frame yielding a protein having properties of the matrix (M) protein was identified. It is positioned at the immedi...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4684-1280-2_13
更新日期：1987-01-01 00:00:00
abstract：:The "silent epidemic" of Chlamydia trachomatis threatens to cause reproductive damage and infertility in many of the 50 million women who acquire it each year. Female reproductive tract infection has more recently been linked to stillbirth and premature delivery. Innate immune cells and mediators appear to be the prim...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-1-4614-4726-9_8
更新日期：2013-01-01 00:00:00
abstract：:The possible molecular conformations of four structurally and biologically different lipoxins derivatives were predicted by a systematic structure tree theoretical analysis. This method takes into account the London-Van der Waals energy of interaction, the electrostatic interaction, the rotation energy of the torsiona...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章
doi：10.1007/978-1-4757-0937-7_8
更新日期：1988-01-01 00:00:00
abstract：:Schizophrenia alters basic brain processes of perception, emotion, and judgment to cause hallucinations, delusions, thought disorder, and cognitive deficits. Unlike neurodegeneration diseases that have irreversible neuronal degeneration and death, schizophrenia lacks agreeable pathological hallmarks, which makes it on...
journal_title：Advances in experimental medicine and biology
pub_type： 杂志文章,评审
doi：10.1007/978-3-7091-0932-8_22
更新日期：2012-01-01 00:00:00
