Results 61 to 70 of about 212,806 (232)

Potent inhibitors active against HIV reverse transcriptase with K101P, a mutation conferring rilpivirine resistance [PDF]

, 2015
Catechol diether compounds have nanomolar antiviral and enzymatic activity against HIV with reverse transcriptase (RT) variants containing K101P, a mutation that confers high-level resistance to FDA-approved non-nucleoside inhibitors efavirenz and ...
Anderson, Karen S., Bollini, Mariela, Frey, Kathleen M., Gray, William T., Jorgensen, William L., Laskey, Sarah B., Lee, Won Gil, Mislak, Andrea C., Siliciano, Robert F., Spasov, Krasimir A.   +9 more
core   +2 more sources

Tuning Polyacrylate Composition to Recognize and Modulate Fluorescent Proteins

Angewandte Chemie, EarlyView.
Random hetero oligomers (RHOs) of defined compositions are synthesized and fractionated to identify the chemical design criteria (charge, length, hydrophobicity) required to achieve nanomolar binding to green fluorescent protein, resulting in >100% fluorescence increases.
Darwin C. Gomez, Swarnadeep Seth, Ronnie Mondal, Stephen J. Koehler, Jared G. Baker, Charles Plate, Ian C. Anderson, Mikayla R. Smith, Joey Gloriod, Morgan Gunter, Valerie V. Welborn, Sanket A. Deshmukh, C. Adrian Figg   +12 more
wiley   +2 more sources

Potent single-domain antibodies that arrest respiratory syncytial virus fusion protein in its prefusion state [PDF]

, 2017
Human respiratory syncytial virus (RSV) is the main cause of lower respiratory tract infections in young children. The RSV fusion protein (F) is highly conserved and is the only viral membrane protein that is essential for infection.
Chen, Man, Gilman, Morgan SA, Graham, Barney S, Kabeche, Stephanie C, Kanekiyo, Masaru, Mas, Vicente, McLellan, Jason S, Melero, José A, Rossey, Iebe, Saelens, Xavier, Schepens, Bert, Sedeyn, Koen, Spitaels, Jan, Wrapp, Daniel   +13 more
core   +2 more sources

Trypanosoma brucei DHRF-TS revisited:characterisation of a bifunctional and highly unstable recombinant dihydrofolate reductase-thymidylate synthase [PDF]

, 2016
Bifunctional dihydrofolate reductase–thymidylate synthase (DHFR-TS) is a chemically and genetically validated target in African trypanosomes, causative agents of sleeping sickness in humans and nagana in cattle.
A Dawson, A El Fadili, A Khodursky, AJ Wahba, AJ Wahba, AL Jackman, Alan H. Fairlamb, B Nare, BJ Dolnick, C Fraser-Lhostis, C Shih, CJ Allegra, CW Carreras, D Spinks, DC Jones, E Wirtz, EJ Shanks, EL White, F Gamarro, FW Studier, H Zhang, Han B. Ong, HB Ong, J Phan, J Yuvaniyama, JA Frearson, Jayne Raper, JF Morrison, JM Blaney, JR Appleman, K Al Chalabi, KY Han, LM Changchien, LS Torrie, M Berriman, M Hekmat-Nejad, Marc W. Gibson, MM Bradford, N Greig, N Sienkiewicz, N Sienkiewicz, Natasha Sienkiewicz, ND Brunn, P Prapunwattana, P Reche, PH Liang, R Ferone, R Grumont, RA Copeland, RC Jackson, RD Walter, RJ Bonney, RJ Cisneros, S Shallom, SA Margosiak, SE Webber, SF Chowdhury, SI Ahmad, Simon Dewar, SM Lanham, TC Eadsforth, TD Meek, TW Synold, Y Cheng   +63 more
core   +3 more sources

A Novel Family of Acid-Cleavable Linker Based on Cyclic Acetal Motifs for the Production of Antibody-Drug Conjugates with High Potency and Selectivity.

Bioconjugate chemistry, 2022
Cleavable linkers have become the subject of intense study in the field of chemical biology, particularly because of their applications in the construction of antibody-drug conjugates (ADC), where they facilitate lysosomal cleavage and liberation of ...
Tony Rady, Lorenzo Turelli, M. Nothisen, Elisabetta Tobaldi, Stéphane Erb, Fabien Thoreau, Oscar Hernandez-Alba, S. Cianférani, F. Daubeuf, Alain Wagner, Guilhem Chaubet   +10 more
semanticscholar   +1 more source

A potent human neutralizing antibody Fc-dependently reduces established HBV infections

eLife, 2017
Hepatitis B virus (HBV) infection is a major global health problem. Currently-available therapies are ineffective in curing chronic HBV infection. HBV and its satellite hepatitis D virus (HDV) infect hepatocytes via binding of the preS1 domain of its ...
Dan Li, Wenhui He, Ximing Liu, Sanduo Zheng, Yonghe Qi, Huiyu Li, Fengfeng Mao, Juan Liu, Yinyan Sun, Lijing Pan, Kaixin Du, Keqiong Ye, Wenhui Li, Jianhua Sui   +13 more
doaj   +1 more source

Ternatin and improved synthetic variants kill cancer cells by targeting the elongation factor-1A ternary complex. [PDF]

, 2015
Cyclic peptide natural products have evolved to exploit diverse protein targets, many of which control essential cellular processes. Inspired by a series of cyclic peptides with partially elucidated structures, we designed synthetic variants of ternatin,
Carelli, Jordan D, Jain, Rishi K, Merrick, William C, Miller, Howard R, Ross, Nathan T, Sethofer, Steven G, Simard, Jillian L, Smith, Geoffrey A, Taunton, Jack   +8 more
core   +2 more sources

Synthesis, In Silico and In Vitro Characterization of Novel N,N-Substituted Pyrazolopyrimidine Acetamide Derivatives for the 18KDa Translocator Protein (TSPO)

Pharmaceuticals, 2023
The translocator protein (TSPO) is an interesting biological target for molecular imaging and therapy because the overexpression of TSPO is associated with microglial activation caused by neuronal damage or neuroinflammation, and these activated ...
Jaekyung Park, Sobia Wasim, Jae Ho Jung, Mi-hyun Kim, Byung Chul Lee, Mohammad Maqusood Alam, Sang-Yoon Lee   +6 more
doaj   +1 more source

Pharmacological Profile of MP-101, a Novel Non-racemic Mixture of R- and S-dimiracetam with Increased Potency in Rat Models of Cognition, Depression and Neuropathic Pain

Cells, 2022
The racemic mixture dimiracetam negatively modulates NMDA-induced glutamate release in rat spinal cord synaptosomal preparations and is orally effective in models of neuropathic pain.
T. Bonifacino, L. Micheli, Carola Torazza, C. Ghelardini, C. Farina, G. Bonanno, M. Milanese, L. di Cesare Mannelli, M. Scherz   +8 more
semanticscholar   +1 more source

Rice endosperm is cost-effective for the production of recombinant griffithsin with potent activity against HIV [PDF]

, 2015
Protein microbicides containing neutralizing antibodies and antiviral lectins may help to reduce the rate of infection with human immunodeficiency virus (HIV) if it is possible to manufacture the components in large quantities at a cost affordable in HIV‐
Arcalis, E, Capell, T, Christou, P, Evans, A, Medina, V, O'Keefe, BR, Ramessar, K, Shattock, RJ, Stöger, E, Vamvaka, E   +9 more
core   +2 more sources