Abstract:
:Due to the obvious advantages of long-acting peptide and protein drugs, strategies to prolong plasma half life time of such compounds are highly on demand. Short plasma half life times are commonly due to fast renal clearance as well as to enzymatic degradation occurring during systemic circulation. Modifications of the peptide/protein can lead to prolonged plasma half life times. By shortening the overall amino acid amount of somatostatin and replacing L: -analogue amino acids with D: -amino acids, plasma half life time of the derivate octreotide was 1.5 hours in comparison to only few minutes of somatostatin. A PEG(2,40 K) conjugate of INF-alpha-2b exhibited a 330-fold prolonged plasma half life time compared to the native protein. It was the aim of this review to provide an overview of possible strategies to prolong plasma half life time such as modification of N- and C-terminus or PEGylation as well as methods to evaluate the effectiveness of drug modifications. Furthermore, fundamental data about most important proteolytic enzymes of human blood, liver and kidney as well as their cleavage specificity and inhibitors for them are provided in order to predict enzymatic cleavage of peptide and protein drugs during systemic circulation.
journal_name
Amino Acidsjournal_title
Amino acidsauthors
Werle M,Bernkop-Schnürch Adoi
10.1007/s00726-005-0289-3subject
Has Abstractpub_date
2006-06-01 00:00:00pages
351-67issue
4eissn
0939-4451issn
1438-2199journal_volume
30pub_type
杂志文章,评审相关文献
AMINO ACIDS文献大全abstract::This study determined whether N-acetylcysteine (NAC) could affect intestinal redox status, proinflammatory cytokines, epidermal growth factor (EGF), EGF receptor (EGFR), Toll-like receptor-4 (TLR4), and aquaporin-8 in a lipopolysaccharide (LPS)-challenged piglet model. Eighteen piglets (35-day-old) were randomly alloc...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-012-1295-x
更新日期:2013-09-01 00:00:00
abstract::Chlamydocin is a powerfulin vitro antitumoral agent, quickly inactivatedin vivo. A series of cyclic tetrapeptides related to chlamydocin or HC toxin and bearing a bioactive alkylating group on anε-amino-lysyl function have been examined for their antitumoral activity on L1210 and P388 murine leukemia cell lines. One a...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00813752
更新日期:1994-10-01 00:00:00
abstract::The extracellular transglutaminases (TGs) in eukaryotes are responsible for the post-translational modification of proteins through different reactions, cross-linking being the best known. In higher plants, extracellular TG appears to be involved in roles similar to those performed by the mammalian counterparties. Sin...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-013-1605-y
更新日期:2014-03-01 00:00:00
abstract::Rats were trained to perform a conditioned avoidance response to white noise in a conventional two-compartment "shuttle-box". The partition between the compartments had two openings, however, and the correct passage (leftor right) was signalled by changes in background illumination. In this situation the psychotomimet...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00806009
更新日期:1992-02-01 00:00:00
abstract::Non-invasive detection of prostate cancer or metastases still remains a challenge in the field of molecular imaging. In our recent work of screening arginine- or lysine-rich peptides for intracellular delivery of a therapeutic agent into prostate cancer cells, an arginine-rich cell permeable peptide (NH(2)GR(11)) was ...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-010-0515-5
更新日期:2011-11-01 00:00:00
abstract::Proline dehydrogenase/oxidase (PRODH/POX) is a mitochondrial protein critical to multiple stress pathways. Because of the roles of PRODH/POX in signaling, and its shared localization to the mitochondrial inner membrane with the electron transport chain (ETC), we investigated whether there was a direct relationship bet...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-015-2134-7
更新日期:2016-03-01 00:00:00
abstract::We recently reported that dietary supplementation with L-proline (proline) during gestation improved embryonic survival in C57BL/6J mice. The objective of the present study was to test the hypothesis that the effect of maternal proline supplementation on embryonic survival can be carried forward to the first generatio...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-019-02717-2
更新日期:2019-05-01 00:00:00
abstract::We studied in vivo production of taurine, hypotaurine and sulfate following subcutaneous administration of L-cysteinesulfinate (CSA) to rats and mice. When 5.0 mmol/kg of body weight of CSA was injected to rats, increased urinary excretions of taurine, hypotaurine and sulfate in 24 h urine were 617, 52 and 1,767 micro...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-005-0277-7
更新日期:2006-07-01 00:00:00
abstract::Pseudomonas aeruginosa is particularly difficult to treat because it possesses a variety of resistance mechanisms and because it often forms biofilms. Antimicrobial peptides represent promising candidates for future templates of antibiotic-resistant bacterial infections due to their unique mechanism of antimicrobial a...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2625-4
更新日期:2018-10-01 00:00:00
abstract::Prophylactic supplementation of N-acetyl-cysteine (NAC) and epigallocatechin gallate (EGCG) was studied for physiological and cellular changes in skeletal muscle after eccentric muscle contractions. Thirty healthy, active males (20.0 +/- 1.8 years, 160 +/- 7.1 cm, 76.1 +/- 17.0 kg) ingested for 14 days either 1,800 mg...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-009-0432-7
更新日期:2010-06-01 00:00:00
abstract::Both 1,4-benzoquinones and 1,4-naphthoquinones were attached to the non-proteinogenic amino acid taurine to form N-quinonyl taurine derivatives. The products were formed via the direct Michael-like addition or by substitution of a good leaving group. An attempt to bridge the two moieties via an ureido spacer resulted ...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-002-0407-4
更新日期:2003-04-01 00:00:00
abstract::Recently, crystalized mouse ketimine reductase/CRYM complexed with NADPH was found to have pyruvate bound in its active site. We demonstrate that the enzyme binds α-keto acids, such as pyruvate, in solution, and catalyzes the formation of N-alkyl-amino acids from alkylamines and α-keto acids (via reduction of imine in...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-015-2044-8
更新日期:2015-11-01 00:00:00
abstract::Knowing the key features of the structure and the biochemistry of proteins is crucial to improving enzymes of industrial interest like β-fructofuranosidase. Gene sacA from Bacillus licheniformis ATCC 14580 codifies a sucrose-6-phosphate hydrolase, a β-fructofuranosidase (E.C. 3.1.2.26, protein BlsacA), which has no cr...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-02690-2
更新日期:2019-04-01 00:00:00
abstract::Among many actions assigned to taurine (Tau), the most abundant amino acid in numerous mammalian tissues, it prevents high-fat diet-induced obesity with increasing resting energy expenditure. To sustain this Tau action, the goal of the present study was to explore the acute effects of Tau on baseline and on adrenaline...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-011-0919-x
更新日期:2012-05-01 00:00:00
abstract::The sulfur-containing amino acid, taurine (Tau), regulates glucose and lipid homeostasis under normal, pre- and diabetic conditions. Here, we aimed to verify whether Tau supplementation exerts its beneficial effects against obesity, hyperglycemia and alterations in islet functions, in leptin-deficient obese (ob/ob), o...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2553-3
更新日期:2018-06-01 00:00:00
abstract::Cu(I)-mediated [3+2]cycloaddition between azides and alkynes has evolved into a valuable bioconjugation tool in radiopharmaceutical chemistry. We have developed a simple, convenient and reliable radiosynthesis of 4-[18F]fluoro-N-methyl-N-(propyl-2-yn-1-yl)benzenesulfonamide ([18F]F-SA) as a novel aromatic sulfonamide-...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-012-1450-4
更新日期:2013-04-01 00:00:00
abstract::Some of the chemistry of amino acids going on in our laboratory (Laboratoire des Amino acides Peptides et Protéines) is described as well as some mass spectrometry methodology for their characterization particularly on solid supports. Several aspects are presented including: (i) the stereoselective synthesis of natura...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/BF01388176
更新日期:1999-01-01 00:00:00
abstract::The present research has been carried out to elicit the mechanism of antiangiogenic activity of a fusion peptide P2. Peptide P2 was designed by the connection of a heptapeptide MMP inhibitor to ES-2, a fragment of Endostatin. In a previous study, P2 demonstrated strong antiangiogenic and antitumor effect, and the curr...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2589-4
更新日期:2018-08-01 00:00:00
abstract::Lung cancer is still difficult to treat by current chemotherapeutic procedures. We recently found that MVL, an anti-HIV lectin from blue-green algae Microcystis viridis, also has antitumor activity. The objective of this study was to investigate apoptosis-inducing activity of recombinant MVL (R-MVL) and proteomic chan...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-010-0791-0
更新日期:2011-10-01 00:00:00
abstract::This study investigated the effect of different sampling environments on hemolymph amino acid content of individual Drosophila melanogaster larvae. Hemolymph was collected from individual third instar larvae under cold-anesthetized, awake, and stress conditions. Qualitative and quantitative hemolymph amino acid analys...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-009-0284-1
更新日期:2010-03-01 00:00:00
abstract::The objective of this study was to determine the dose as well as duration of exposure-dependent effects of L-alanyl-L-glutamine, arginine or taurine on polymorphonuclear neutrophil (PMN) free alpha-keto acid profiles and, in a parallel study, on PMN immune functions. Exogenous L-alanyl-L-glutamine significantly increa...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-005-0223-8
更新日期:2005-11-01 00:00:00
abstract::One pathogenic mechanism of ethanol-induced liver injury is the excessive production of reactive oxygen species (ROS), which may result in alcoholic liver disease (ALD) characterized by cell death due to necrosis and apoptosis. Taurine was proved to protect against liver damage. However, whether taurine attenuates eth...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2561-3
更新日期:2018-07-01 00:00:00
abstract::The supplementation of creatine has shown a marked neuroprotective effect in mouse models of neurodegenerative diseases (Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis). This has been assigned to the known bioenergetic, anti-apoptotic, anti-excitotoxic and anti-oxidant properties of creatine....
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-011-0850-1
更新日期:2011-05-01 00:00:00
abstract::This work is an extension of our previous work (Hall et al., 1993) on the synthesis and cytotoxic activity of boronated peptides. The aim of this work was to carry out structural modifications of the amine terminal in compounds1 and2, to increase water solubility, and its effect on the cytotoxicity to tumor cell lines...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF00806550
更新日期:1995-12-01 00:00:00
abstract::This paper analyses the presence of and changes in free amino acids and biogenic amines in red and white muscle of bigeye tuna during storage in controlled atmospheres with 2 gas mixes containing different concentrations of CO(2) and O(2). Levels of amines were generally higher in white than in red muscle, with the ex...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-003-0054-4
更新日期:2004-03-01 00:00:00
abstract::Extracellular peptide ligand binding sites, which bind the N-termini of angiotensin II (AngII) and bradykinin (BK) peptides, are located on the N-terminal and extracellular loop 3 regions of the AT(1)R and BKRB(1) or BKRB(2) G-protein-coupled receptors (GPCRs). Here we synthesized peptides P15 and P13 corresponding to...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-012-1405-9
更新日期:2013-03-01 00:00:00
abstract::Breast cancer epidemic in the early twenty-first century results in around two million new cases and half-a-million of the disease-related deaths registered annually worldwide. A particularly dramatic situation is attributed to some specific patient subgroups such as the triple-negative breast cancer (TNBC). TNBC is a...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-017-2524-0
更新日期:2018-04-01 00:00:00
abstract::Anticancer peptides (ACPs) are biologically anticancer active molecules that are produced by mammals, plants, insects and microorganisms. Here, a new peptide (TC22) with the amino acid sequence MTVVLLLIVLPLLGGVHSSGIL was identified and characterized from the beetle Tribolium castaneum. We found it inhibited the growth...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/s00726-018-2666-8
更新日期:2019-02-01 00:00:00
abstract::This mini review deals with the modern aspects of the spectroscopy and structural elucidation of amino acid derivatives and small biologically active compounds. Free peptide bond rotation in these systems yields various conformers, which possess differing biological activities. Another phenomenon is the intermolecular...
journal_title:Amino acids
pub_type: 杂志文章,评审
doi:10.1007/s00726-008-0220-9
更新日期:2010-01-01 00:00:00
abstract::The regulation of the expression of indoleamine 2,3-dioxygenase (IDO) was studied in cloned murine macrophages (MT2) and microglial (N11) cells. Both cell lines express IDO and inducible nitric oxide synthase activity after interferon-gamma (IFN-gamma) stimulation. The regulation of IDO expression appears to differ in...
journal_title:Amino acids
pub_type: 杂志文章
doi:10.1007/BF01345271
更新日期:1998-01-01 00:00:00