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  1. 19 Cellular and Molecular Biology Letters
  2. 8 Acta Biochimica Polonica
  3. 8 Archivum Immunologiae et Therapiae Experimentalis
  4. 7 Journal of Physiology and Pharmacology
  5. 2 Folia Histochemica et Cytobiologica
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  1. 3 2016
  2. 3 2015
  3. 1 2014
  4. 2 2013
  5. 1 2011
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  1. 2 Funa K.
  2. 2 Ginalski K.
  3. 2 Lesyng B.
  4. 2 Uramoto H.
  5. 1 Ahluwalia A.
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1
Crosstalk between G protein-coupled receptors and tyrosine kinase signalling; Src take centre stage
100%
Ptasznik A. , Gewirtz A. M.
Archivum Immunologiae et Therapiae Experimentalis
|
2000
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tom 48
|
nr 1
2
Content available remote Regulatory mechanisms for the expression and activity of platelet-derived growth factor receptor.
88%
Funa K. , Uramoto H.
Acta Biochimica Polonica
|
2003
|
tom 50
|
nr 3
647-658
EN
PDGF is one of the most potent serum mitogens, and the signalling mechanism by way of its receptor tyrosine-kinase has been extensively studied since its first purification in 1979. The identification of homology between the simian sarcoma virus oncogene, v-sis, and the B-chain of PDGF, as well as the frequent over-expression of both the ligands and receptors in various tumours and stroma led to the proposal of the PDGF-mediated autocrine and paracrine hypothesis. Consistent with the important roles of PDGF in the growth and survival of cells, the expression and activity of PDGF receptors are tightly controlled by both positive and negative feedback mechanisms at different levels. The deregulation of the control system can result in serious pathological conditions such as chronic inflammation and tumours. Understanding the molecular mechanisms for the regulatory system and the signalling pathway of PDGF is essential in order to find effective therapies in the diseases where PDGF is involved.
3
Specific, irreversible inhibitors of the epidermal growth factor receptor [EGFR] family of tyrosine kinases
88%
Fry D. W.
Cellular and Molecular Biology Letters
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1998
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tom 03
|
nr 3
4
Phytoestrogen action in Leydig cells of Bilgoraj ganders (Anser anser)
75%
Opalka M. , Kaminska B. , Puchajda-Skowronska H. , Dusza L.
Reproductive Biology
|
2006
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tom 06
|
nr Suppl.2
5
Content available Tyrosine kinase, Aurora kinase and leucine aminopeptidase as attractive drug targets in anticancer therapy - characterisation of their inhibitors
75%
Ziemska J. , Solecka J.
Roczniki Państwowego Zakładu Higieny
|
2016
|
tom 67
|
nr 4
EN
Cancers are the leading cause of deaths all over the world. Available anticancer agents used in clinics exhibit low therapeutic index and usually high toxicity. Wide spreading drug resistance of cancer cells induce a demanding need to search for new drug targets. Currently, many on-going studies on novel compounds with potent anticancer activity, high selectivity as well as new modes of action are conducted. In this work, we describe in details three enzyme groups, which are at present of extensive interest to medical researchers and pharmaceutical companies. These include receptor tyrosine kinases (e.g. EGFR enzymes) and non-receptor tyrosine kinases (Src enzymes), type A, B and C Aurora kinases and aminopeptidases, especially leucine aminopeptidase. We discuss classification of these enzymes, biochemistry as well as their role in the cell cycle under normal conditions and during cancerogenesis. Further on, the work describes enzyme inhibitors that are under in vitro, preclinical, clinical studies as well as drugs available on the market. Both, chemical structures of discovered inhibitors and the role of chemical moieties in novel drug design are discussed. Described enzymes play essential role in cell cycle, especially in mitosis (Aurora kinases), cell differentiation, growth and apoptosis (tyrosine kinases) as well as G1/S transition (leucine aminopeptidase). In cancer cells, they are overexpressed and only their inhibition may stop tumor progression. This review presents the clinical outcomes of selected inhibitors and argues the safety of drug usage in human volunteers. Clinical studies of EGFR and Src kinase inhibitors in different tumors clearly show the need for molecular selection of patients (to those with mutations in genes coding EGFR and Src) to achieve positive clinical response. Current data indicates the great necessity for new anticancer treatment and actions to limit off-target activity.
PL
Nowotwory stanowią jedną z głównych przyczyn zgonów na świecie. Dostępne w lecznictwie substancje przeciwnowotworowe charakteryzują się niskim indeksem terapeutycznym jak i wysoką toksycznością. Rozwijająca się oporność komórek nowotworowych na dostępne w terapii leki przyczynia się do konieczności poszukiwania nowych punktów uchwytu/miejsc docelowych (z ang. targets) dla potencjalnych substancji przeciwnowotworowych. Obecnie prowadzonych jest również wiele prac nad nowymi związkami przeciwnowotworowymi o wysokim potencjale terapeutycznym, nowym mechanizmie działania i/bądź wyższym indeksie selektywności. W pracy, autorzy skupili uwagę na trzech grupach enzymów, będących obecnie w obszarze zainteresowań współczesnej medycyny. Omówione zostały kinazy tyrozynowe na przykładzie enzymów EGFR i Src, kinazy Aurora typu A, B i C, a także aminopeptydazy na przykładzie aminopeptydazy leucynowej. Scharakteryzowano klasyfikację enzymów, ich rolę w cyklu komórkowym w warunkach fizjologicznych i procesie nowotworowym. Opisano również inhibitory enzymów, substancje będące w trakcie badań in vitro, przedklinicznych i klinicznych jak i leki wprowadzone na rynek farmaceutyczny. Zwrócono uwagę na budowę chemiczną inhibitorów enzymów i tym samym na kierunek poszukiwań nowych leków przeciwnowotworowych. Omówione enzymy w warunkach fizjologicznych odgrywają ważną rolę w cyklu komórkowym, zwłaszcza na etapie podziału mitotycznego. Jednakże w procesie nowotworowym dochodzi do ich nadekspresji. Zjawisko to można zahamować poprzez inhibicję aktywności enzymu. Autorzy omówili wpływ inhibitorów kinaz tyrozynowych, kinaz Aurora czy aminopeptydaz leucynowych na cykl komórkowy i bezpieczeństwo stosowania tych potencjalnych leków u ludzi. Dotychczasowe badania przedkliniczne i kliniczne inhibitorów kinazy tyrozynowej typu EGFR czy Src potwierdziły konieczność selekcji pacjentów, na tych z mutacją w genie kodującym dany enzym. Badania prowadzone na wybranej grupie chorych przynosiły oczekiwany pozytywny wynik. Wiele aspektów dotyczących nowych punktów uchwytu w terapii przeciwnowotworowej wciąż wymaga dalszych prac, aczkolwiek daje również nadzieję na odkrycie skutecznych i selektywnych leków.
6
Content available Identification of potential off-targets of chemotherapeutic agent Sorafenib: a molecular docking approach
75%
Sahrawat T. R. , Chawla P.
International Letters of Natural Sciences
|
2016
|
tom 51
EN
B-Raf is a multi- drug target serine/threonine protein kinase, involved in the transduction of mitogenic signals from the cell membrane to the nucleus. Mutated B-Raf causes overactive downstream signaling via MEK and ERK, leading to excessive cell proliferation and survival, independent of growth factors causing cancers such as Pancreatic carcinoma. A novel bi-aryl urea- Sorafenib, is a potent inhibitor of Raf-1 that has been approved for the treatment of a number of cancers including pancreatic cancer. The present investigation was designed to identify the potential off-targets of Sorafenib which could be responsible for its reported undesirable side effects. Molecular docking was used to test the efficacy of structural analogs of Sorafenib against B-Raf using FlexX and it was found that the analog with CID:10151557 had a high potency with minimum number of clashes, low lipophilic score and high match score, similar to Sorafenib. To identify the potential off-target/s of Sorafenib, macromolecular surface similarity detection software MEDIT SA MED-SuMo was used and the results obtained were validated through literature. The possible off-targets obtained belonged to the family of protein tyrosine kinases i.e. VEGFR-2, VEGFR-3, platelet-derived growth factor receptor beta, Flt-3, and c-KIT, each of which were docked with Sorafenib. Based on high docking scores and similarity with B-Raf for its binding site interacting residues, it was concluded that Vascular endothelial growth factor tyrosine kinase receptor (VEGFR) is a potential off-target of anti-cancer chemotherapeutic agent Sorafenib.
7
Evolving the desired compound profile within an LCK project
75%
Baldwin I. R.
Cellular and Molecular Biology Letters
|
2003
|
tom 08
|
nr 2A
8
Structural basis of oncogenesis caused by point mutations in the kinase domain of the MET proto-oncogene
75%
Miller M. , Zbar B. , Ginalski K. , Lesyng B.
Cellular and Molecular Biology Letters
|
1998
|
tom 03
|
nr 3
9
The transition from a pharmacophore-guided approach to a receptor-guided approach in the design of potent protein kinase C ligands
75%
Marquez V. E. , Nacro K. , Benzaria S. , Lee J. , Milne G. W. , Bienfait B. , Wang S. , Lewin N. , Blumberg P. M.
Cellular and Molecular Biology Letters
|
1998
|
tom 03
|
nr 3
10
WP744, a novel highly apoptotic and antiproliferative agent against STI-571-resistant leukemic cells
75%
Priebe W. , Evrony G. , Fokt I. , Lee S. , Talpaz M. , Donato N. J.
Cellular and Molecular Biology Letters
|
2003
|
tom 08
|
nr 2A
11
Content available remote The role of tyrosine kinase in prostaglandin E2 and vanadate-evoked contractions in rabbit duodenum in vitro
75%
Grasa L. , Arruebo M. P. , Plaza M. A. , Murillo M. D.
Journal of Physiology and Pharmacology
|
2006
|
tom 57
|
nr 2
EN
Prostaglandin E2 (PGE2) can interact with at least four cell surface receptors (EP1-EP4) in smooth muscle, which evokes a variety of intracellular responses depending on the G protein to which the cell surface receptors are coupled. The activation of G protein-coupled receptors and receptor tyrosine kinases can lead to the phosphorylation of tyrosine residues of various cellular proteins. The aim of this study was to examine the role of tyrosine phosphorylation in PGE2, vanadate and carbachol-evoked contractions. PGE2, vanadate, and carbachol induced contractile motor responses in the longitudinal smooth muscle of rabbit duodenum. PGE2-evoked contractions decreased in the presence of genistein or tyrphostin B44. PGE2-evoked contractions increased in the presence of vanadate. Vanadate-evoked contractions decreased in the presence of genistein. In contrast, tyrphostin 47 increased the vanadate-evoked contractions. Vanadate-evoked contractions were reduced in the presence of Ca2+-free solutions, verapamil, or indomethacin. U-73122 decreased PGE2-evoked contractions. Carbachol-evoked contractions decreased in the presence of genistein, tyrphostin B44 or tyrphostin 47. Our results suggest that PGE2, vanadate or carbachol-evoked contractions are mediated by protein tyrosine phosphorylation. Protein tyrosine phosphorylation might cause an increase in calcium influx through voltage-dependent channels and the release of prostaglandins in the longitudinal smooth muscle of the rabbit duodenum.
12
Regulatory mechanisms for the expression and activity of platelet-derived growth factor receptor
75%
Funa K. , Uramoto H.
Acta Biochimica Polonica
|
2003
|
tom 50
|
nr 3
EN
PDGF is one of the most potent serum mitogens, and the signalling mechanism by way of its receptor tyrosine-kinase has been extensively studied since its first purifica­tion in 1979. The identification of homology between the simian sarcoma virus onco­gene, v-sis, and the B-chain of PDGF, as well as the frequent over-expression of both the ligands and receptors in various tumours and stroma led to the proposal of the PDGF-mediated autocrine and paracrine hypothesis. Consistent with the important roles of PDGF in the growth and survival of cells, the expression and activity of PDGF receptors are tightly controlled by both positive and negative feedback mechanisms at different levels. The deregulation of the control system can result in serious pathological conditions such as chronic inflammation and tumours. Understanding the molecular mechanisms for the regulatory system and the signalling pathway of PDGF is essential in order to find effective therapies in the diseases where PDGF is involved.
13
The role of tyrosine kinase in the adhesion and fusion of myoblasts
75%
Wrobel E. , Moraczewski J.
Cellular and Molecular Biology Letters
|
2002
|
tom 07
|
nr Suppl.
14
Structure, regulation and function of PKB-Akt - a major therapeutic target
75%
Hemmings B. A.
Cellular and Molecular Biology Letters
|
2003
|
tom 08
|
nr 2A
15
DNA repair in drug resistance induced by fusion tyrosine kinases
75%
Blasiak J.
Cellular and Molecular Biology Letters
|
2002
|
tom 07
|
nr Suppl.
16
Content available remote Effects of tyrosine kinase inhibitors on voltage-dependent BA2+ currents in the guinea-pig gastric antrum
75%
Zhu H. L. , Ito Y. , Teramoto N.
Journal of Physiology and Pharmacology
|
2006
|
tom 57
|
nr 3
EN
We have investigated whether tyrosine kinases modify the activity of voltage-dependent Ba2+ currents (IBa) recorded from guinea-pig gastric myocytes by use of patch-clamp techniques. All experiments were carried on single smooth muscle cells, dispersed from the circular layer of the guinea-pig gastric antrum. Genistein (10 µM), a specific tyrosine kinase inhibitor, reduced the peak amplitude of IBa in a voltage- and concentration-dependent manner. Daidzein (30 µM), an inactive analog of genistein, also inhibited IBa in a concentration-dependent manner. Similarly, other types of tyrosine kinase inhibitors (lavendustin A and tyrphostin 23) suppressed the peak amplitude of IBa in a concentration-dependent manner. These results indicate that tyrosine kinases may be essential to regulate Ca2+ mobilization through voltage-dependent Ca2+ channels in gastric myocytes.
17
Effect of protein tyrosine kinases on mitochondrial calcium homeostasis in rat hepatocytes treated with thapsigargin
75%
Walajtys-Rode E. , Moehren G. , Hoek J. B.
Cellular and Molecular Biology Letters
|
1998
|
tom 03
|
nr 3
18
Molecular dissection of fertilisation signalling with the aid of tyrosine-kinase-specific inhibitors
75%
Sato K. I. , Iwasaki T. , Fukami Y.
Cellular and Molecular Biology Letters
|
2003
|
tom 08
|
nr 2A
19
Novel small molecule inhibitors of c-terminal Src kinase [Csk]
75%
Kilimnik A. , Kostjukova M. N. , Pyatkin I. H. , Pronin A. M. , Strelnikowa S. R. , Fedotov Y. A. , Kolesnikov A. V.
Cellular and Molecular Biology Letters
|
2003
|
tom 08
|
nr 2A
20
Effects of angiotensin derivatives [Lang] - filled liposomes on isolated rat aorta
75%
Costuleanu M. , Costuleanu N. , Foia L. , Slatineanu S. M. , Costuleanu A. , Petrescu G.
Cellular and Molecular Biology Letters
|
1999
|
tom 04
|
nr 2
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