Results 171 to 180 of about 23,687 (206)

Development And Strategies Of VEGFR-2/KDR Inhibitors

Future Medicinal Chemistry, 2012
VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. As an essential receptor protein tyrosine kinase propagating cellular signal transduction processes, VEGFR-2 is a central target for drug discovery against tumor-associated angiogenesis.
Lingyi, Huang, Zhengui, Huang, Zhiqiang, Bai, Rui, Xie, Liping, Sun, Kejiang, Lin   +5 more
openaire   +2 more sources

Cross resistance to brevetoxin-3 by kdr and super-kdr mutations in house flies

Pesticide Biochemistry and Physiology
The dinoflagellate Karenia brevis is a causative agent of red tides in the Gulf of Mexico and generates a potent family of structurally related brevetoxins that act via the voltage-sensitive Na+ channel. This project was undertaken to better understand the neurotoxicology and kdr cross-resistance to brevetoxins in house flies by comparing the ...
Daniel R, Swale, Jeffrey R, Bloomquist, Sarah E, McComic, Edwin R, Burgess   +3 more
openaire   +2 more sources

Property-Based Design of KDR Kinase Inhibitors

Current Medicinal Chemistry, 2004
Small molecule inhibitors of KDR kinase activity have typically possessed poor intrinsic physical properties including low aqueous solubility and high lipophilicity. These features have often conferred limited cell permeability manifested in low levels of cell-based KDR inhibitory activity and oral bioavailability.
Mark E, Fraley, William F, Hoffman, Kenneth L, Arrington, Randy W, Hungate, George D, Hartman, Rosemary C, McFall, Kathleen E, Coll, Keith, Rickert, Kenneth A, Thomas, Georgia B, McGaughey   +9 more
openaire   +2 more sources

Overcoming super-knock down resistance (super-kdr) mediated resistance: multi-halogenated benzyl pyrethroids are more toxic to super-kdr than kdr house flies.

Insect molecular biology, 2016
Target site insensitivity because of mutations in the voltage-sensitive sodium channel gene (Vssc) is a major mechanism of resistance to pyrethroid insecticides in the house fly, Musca domestica. There are three known Vssc alleles that confer resistance to pyrethroids in the house fly: knock down resistance (kdr; L1014F), super-kdr (M918T + L1014F) and
H, Sun, K P, Tong, S, Kasai, J G, Scott
openaire   +2 more sources

First detection of kdr, kdr-his, and super-kdr type mutations in Musca domestica (Diptera: Muscidae) from Argentina

Journal of Economic Entomology
Abstract The house fly, Musca domestica L. (Diptera: Muscidae), is a cosmopolitan pest that poses health risks to humans and domesticated animals. Pyrethroid insecticides target the insect voltage-sensitive sodium channel (VSSC) and have been widely used to control house flies in poultry farms in Argentina for more than 3 decades.
Romina V Piccinali, Roca-Acevedo Gonzalo, Paredes Viviana, Ariel C Toloza   +3 more
openaire   +2 more sources

Toxicological and molecular characterization of pyrethroid-resistant horn flies, Haematobia irritans: identification of kdr and super-kdr point mutations

Insect Biochemistry and Molecular Biology, 1997
Two pyrethroid-resistant strains of horn flies were found to be 17- and 688-fold more resistant to permethrin and 17- and 11,300-fold more resistant to cyhalothrin than a susceptible control strain. Synergism experiments with piperonyl butoxide showed that both target site insensitivity and metabolic resistance mechanisms were present in the Super ...
F D, Guerrero, R C, Jamroz, D, Kammlah, S E, Kunz   +3 more
openaire   +2 more sources

The Kdr Factor in Pyrethroid Resistance

1983
The pyrethroid and DDT insecticides share several properties: Both groups of chemicals are more toxic at lower temperatures and poison nerves in a superficially similar manner, and their fdr-resistance factors confer cross resistance to both pyrethroids and DDT. It is possible to describe the action of an insecticide as DDT-like or pyrethroid-like, but
T. A. Miller, V. L. Salgado, S. N. Irving   +2 more
openaire   +1 more source

KDR gene polymorphisms and idiopathic recurrent spontaneous abortion

The Journal of Maternal-Fetal & Neonatal Medicine, 2016
Process of angiogenesis is essential for successful gestation. Disruption in this pathway leads to various undesirable consequences in pregnancy such as recurrent spontaneous abortion (RSA). One of the most important genes involved in angiogenesis is kinase-insert domain-containing receptor (KDR).
Negar, Honarvar, Mohammad Hasan, Sheikhha, Ehsan, Farashahi Yazd, Hossein, Pashaiefar, Shirin, Mohtaram, Ali, Sazegari, Zahra, Feizollahi, Nasrin, Ghasemi   +7 more
openaire   +2 more sources

The reliability of endothelial progenitor cells (CD34+, KDR+, and CD34+/KDR+) in the diagnosis of coronary artery disease and its severity

The Egyptian Journal of Haematology, 2012
Background Bone marrow-derived endothelial progenitor cells (EPCs) play an integral role in the regulation and protection of the endothelium, as well as new vessel formation. Changes in EPC number and function during coronary heart disease allow their use as a biomarker.
EmanM. Sewify, Ola Afifi, MonaM. Soliman, AhmadI. Ziada   +3 more
openaire   +1 more source

Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr

Bioorganic & Medicinal Chemistry Letters, 2007
Inhibition of tumor-induced angiogenesis is a promising strategy in anticancer research. Neovascularization is a process required for both tumor growth and metastasis. Enhanced understanding of the underlying molecular mechanisms has led to the discovery of a variety of pharmaceutically attractive targets. Decades of investigation suggest that vascular
Celia, Dominguez, Leon, Smith, Qi, Huang, Chester, Yuan, Xiaohu, Ouyang, Lynn, Cai, Paul, Chen, Joseph, Kim, Timothy, Harvey, Rashid, Syed, Tae-Seong, Kim, Andrew, Tasker, Ling, Wang, Michael, Zhang, Angela, Coxon, James, Bready, Charles, Starnes, Danlin, Chen, Yongmei, Gan, Sesha, Neervannan, Gondi, Kumar, Anthony, Polverino, Richard, Kendall   +22 more
openaire   +2 more sources