Results 61 to 70 of about 48,162 (258)

Structure–activity relationship of the allosteric effects of ivermectin at human P2X4 and GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Positive allosteric modulation of the P2X4 receptor is a potential route to providing cardiovascular benefit through enhancing flow‐dependent arterial vasodilation and providing cardioprotection. However, ligands that selectively enhance P2X4 activity are absent.
Jessica L. Meades, Marcella Bassetto, Marius C. Staiculescu, Gayathri Swaminath, Samuel J. Fountain   +4 more
wiley   +1 more source

Genetic and genomic approaches for the discovery of parasite genes involved in antimalarial drug resistance [PDF]

, 2013
The biggest threat to the war on malaria is the continued evolution of drug resistance by the parasite. Resistance to almost all currently available antimalarials now exists in Plasmodium falciparum which causes the most suffering among all human malaria
Mwangi, J.M., Ranford-Cartwright, L.C.
core   +1 more source

Anti‐inflammatory effects of physical stimuli: The central role of networks in shaping the future of pharmacological research

British Journal of Pharmacology, EarlyView.
Addressing complexity in the study of life sciences through Systems Biology and Systems Medicine has been transformative, making Systems Pharmacology the next logical step. In this review, we focus on physical stimuli, whose potential in pharmacology has been neglected, despite demonstrated therapeutic properties.
Veronica Paparozzi, Reyhaneh Hooshmandabbasi, Alessandro Ravoni, Ying Ma, Luigi Manni, Timothy J. Koh, Caroline Maake, Tiziana Guarnieri, Darong Lai, Vitalii Zablotskii, Christine Nardini   +10 more
wiley   +1 more source

Interactions between inhibitors of dihydrofolate reductase [PDF]

Biochemical Journal, 1989
The binding of substrates and inhibitors to dihydrofolate reductase was studied by steady-state kinetics and high-field 1H-n.m.r. spectroscopy. A series of 5-substituted 2,4-diaminopyrimidines were examined and were found to be ‘tightly binding’ inhibitors of the enzyme (Ki less than 10(-9) M).
James Feeney, A D Hall, K Bowden, Gordon C. K. Roberts, Berry Birdsall   +4 more
openaire   +3 more sources

Antimalarial flavonoid glycoside from Carica papaya with inhibitory potential against Plasmodium falciparum dihydrofolate reductase thymidylate synthase: an in-silico study

Universa Medicina
BACKGROUND Carica papaya is traditionally used to treat malaria. The mechanism of action of the active constituents may be determined by molecular docking.
Dewa Ayu Agus Sri Laksemi, I Dewa Ayu Inten Dwi Primayanti, I Wayan Surudarma, Putu Ayu Asri Damayanti, Ni Made Pitri Susanti   +4 more
doaj   +1 more source

Dihydrofolate reductase of Streptococcus faecium II. Purification and some properties of two dihydrofolate reductases from the Amethopterin-resistant mutant, Streptococcus Faecium Var. Durans Strain A [PDF]

, 1968
From a single amethopterin-resistant organism, Streptococcus faecium var. durans strain A, two different dihydrofolate reductases have been obtained as essentially homogeneous proteins in good yield.
Blakley, R. L., Nixon, P. F.
core  

The Plasmodium falciparum, Nima-related kinase Pfnek-4: a marker for asexual parasites committed to sexual differentiation [PDF]

, 2012
<b>Background</b> Malaria parasites undergo, in the vertebrate host, a developmental switch from asexual replication to sexual differentiation leading to the formation of gametocytes, the only form able to survive in the mosquito vector ...
AG Maier, AM Talman, Andrew Tomlins, C Aurrecoechea, Christian Doerig, CJ Tonkin, EK De Silva, F Silvestrini, J Miao, JA Braks, KG Le Roch, L O’Regan, L Reininger, L Reininger, L Reininger, LM Quarmby, Luc Reininger, M Dyer, MC Bruce, Miguel Garcia, N Hall, P Alano, R Carter, RE Sinden, S Eksi, S Singh, SM Khan, Sylke Müller   +27 more
core   +5 more sources

Tumour Cell Size Control and Its Impact on Tumour Cell Function

Cell Proliferation, EarlyView.
The regulatory mechanism of the size of tumour cells and its impact on the functions of tumour cells, as well as a summary of potential therapeutic targets for the corresponding mechanisms. ABSTRACT Cell size is an important component of cell morphological characteristics.
Min Zhou, Mei Zhou, Yang Jin
wiley   +1 more source

Tracing the evolutionary pathway: on the origin of mitochondria and eukaryogenesis

The FEBS Journal, EarlyView.
This study examines the stepwise transition from archaeal–bacterial associations to the emergence of eukaryotic cells. Metabolic cooperation and endosymbiosis fostered ecological and genetic integration, with extensive gene transfer reshaping host biology.
J. Ernesto Bravo‐Arévalo
wiley   +1 more source

Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1 [PDF]

, 2014
The treatment of Human African Trypanosomiasis remains a major unmet health need in sub-Saharan Africa. Approaches involving new molecular targets are important and pteridine reductase 1 (PTR1), an enzyme that reduces dihydrobiopterin in Trypanosoma spp.
Abedawn I. Khalaf, Addie M., Arcari J. T., Baker N., Barrett M. P., Barrett M. P., Bridges D. J., Brun R., Bursavich M. G., Carter N. S., Cavazzuti A., Colin J. Suckling, Colin L. Gibson, Creek D. J., Dawson A., Dincer S., Federica Giordani, Gangjee A., Gibson C. L., Gourley D. G., Judith K. Huggan, Kaspersen S. J., Keri L. Barrack, Kirsten Stewart, Le Brazidec J.-Y., Matovu E., Michael P. Barrett, Mohamed M. S., Mpamhanga C. P., Pui Ee Wong, Raz B., Sienkiewicz N., Simarro P. P., Spinks D., Tari L. W., Taylor E. C., Tessier P. R., Trzoss M., Tulloch L. B., William N. Hunter, Xie H., Zhu G.   +41 more
core   +4 more sources