Results 91 to 100 of about 212,806 (232)

The role of endothelin-1 in pulmonary arterial hypertension. [PDF]

, 2014
Pulmonary arterial hypertension (PAH) is a rare but debilitating disease, which if left untreated rapidly progresses to right ventricular failure and eventually death. In the quest to understand the pathogenesis of this disease differences in the profile,
Chester, AH, Yacoub, MH
core   +1 more source

TR1801‐ADC: a highly potent cMet antibody–drug conjugate with high activity in patient‐derived xenograft models of solid tumors

Molecular Oncology, 2020
cMet is a well‐characterized oncogene that is the target of many drugs including small molecule and biologic pathway inhibitors, and, more recently, antibody–drug conjugates (ADCs).
Marco Gymnopoulos, Oscar Betancourt, Vincent Blot, Ryo Fujita, Diana Galvan, Vincent Lieuw, Sophie Nguyen, Jeanette Snedden, Christine Stewart, Jose Villicana, Jon Wojciak, Eley Wong, Raul Pardo, Neki Patel, Francois D’Hooge, Balakumar Vijayakrishnan, Conor Barry, John A. Hartley, Philip W. Howard, Roland Newman, Julia Coronella   +20 more
doaj   +1 more source

Tonantzitlolone is a Nanomolar Potency Activator of TRPC1/4/5 Channels. [PDF]

, 2018
BACKGROUND AND PURPOSE The diterpene ester tonantzitlonone (TZL) is a natural product which displays cytotoxicity towards certain types of cancer cell such as renal cell carcinoma cells.
Abramowitz, Akbulut, Alexander, Alexander, Alexander, Beech, Busch, Busch, Camacho Londono, Caropreso, Carson, Curtis, Dietrich, Fan, Gaunt, Harding, Jasper, Just, Ludlow, Muraki, Naylor, Pfeffer, Ratnayake, Rubaiy, Rubaiy, Rubaiy, Rubaiy, Sourbier, Sourbier, Storch, Vinayagam, Westlund, Wu   +32 more
core   +1 more source

Analysis of Single Particles of Amyloid Beta and α‐Synuclein With Seeded Amplification for the Diagnosis of Alzheimer's and Parkinson's Disease

Biotechnology and Applied Biochemistry, EarlyView.
ABSTRACT Neurodegenerative diseases, including Alzheimer's disease (AD) and Parkinson's disease (PD), are characterized by the pathological aggregation of specific proteins such as amyloid beta (Aβ) and α‐synuclein, respectively. Early detection of these protein aggregates in biological fluids could facilitate timely diagnosis and therapeutic ...
Alexandra Dybala, Marlene Pils, Oliver Bannach, Gültekin Tamgüney, Detlev Riesner   +4 more
wiley   +1 more source

Comparative Binding Studies of the Chelators Methylolanthanin and Rhodopetrobactin B to Lanthanides and Ferric Iron

ChemBioChem, EarlyView.
The synthesis and the investigation of the lanthanide (Ln) and Fe‐binding properties of the putative lanthanophore methylolanthanin (MLL) and the siderophore rhodopetrobactin B (RPB B) are reported. While both chelators bind Lns, they unexpectedly precipitate with Lns under biologically relevant conditions and thereby challenge the proposed classic ...
Sophie M. Gutenthaler‐Tietze, Michael Mertens, Manh Tri Phi, Patrick Weis, Björn Drobot, Alexander Köhrer, Robin Steudtner, Uwe Karst, N. Cecilia Martinez‐Gomez, Lena J. Daumann   +9 more
wiley   +1 more source

Nanomolar Affinity Host‐Dye Reporter Pairs from Fluorescently Labeled Oligoarginine Peptides and p‐Sulfonatocalix[4]arene

ChemBioChem, EarlyView.
The dependence of the binding affinity of oligoarginine peptides to p‐sulfonatocalix[4]arene (CX4) on peptide length, C‐terminal functionality, and fluorescent labeling is reported. The fluorescent peptides can be excited in the visible range with common lasers and show nanomolar affinity and efficient quenching upon CX4 binding, which enables their ...
Aparna Pramanik, Mohammad A. Alnajjar, Tristan Wegner, Andreas Hennig   +3 more
wiley   +1 more source

Analysis of transition state mimicry by tight binding aminothiazoline inhibitors provides insight into catalysis by human : O-GlcNAcase [PDF]

, 2016
The modification of nucleocytoplasmic proteins with O-linked N-Acetylglucosamine (O-GlcNAc) plays diverse roles in multicellular organisms. Inhibitors of O-GlcNAc hydrolase (OGA), the enzyme that removes O-GlcNAc from proteins, lead to increased O-GlcNAc
Avalos Gonzalez, Bartlett, Beer, Borghgraef, Cetinbas, Copeland, Dennis, Dorfmueller, Dorfmueller, Dorfmueller, Ferrer, Gao, Graham, Greig, Haltiwanger, Hart, Khidekel, Kim, Kim, Kreppel, Kuntz, Kuzmic, Liu, Liu, Lombard, Lubas, Ma, Macauley, Macauley, Macauley, Macauley, Macauley, Mader, Mark, Mehdy, Morrison, Mosi, Murphy, Ortiz-Meoz, Ozcan, Perrin, Ranuncolo, Rao, Roeser, Ruan, Stubbs, Torres, Trinidad, Wang, Whelan, Whitworth, Yi, Yuzwa, Yuzwa, Yuzwa, Yuzwa, Zhu   +56 more
core   +1 more source

High‐Affinity Peptide‐Drug Conjugate Ligands for the TRIM24 PHD and Bromodomain

Chemistry – A European Journal, EarlyView.
We report a series of bivalent peptide‐drug conjugate (PDC) ligands for tripartite motif‐containing protein 24 (TRIM24). These ligands simultaneously engage the PHD and BRD of TRIM24 through an intramolecular (in cis) binding mode, resulting in high affinity binding.
Michael A. Platt, Ekaterina Kot, Louise A. W. Martin, Antoine L. D. Wallabrègue, Liwen Song, Alistair M. Boyd, Lizbé Koekemoer, Ester M. Hammond, Stuart J. Conway   +8 more
wiley   +1 more source

Nanobodies as tools to understand, diagnose, and treat African trypanosomiasis [PDF]

, 2017
African trypanosomes are strictly extracellular protozoan parasites that cause diseases in humans and livestock and significantly affect the economic development of sub-Saharan Africa.
Caljon, Guy, De Baetselier, Patrick, Magez, Stefan, Stijlemans, Benoit, Van Den Abbeele, Jan, Van Ginderachter, Jo A   +5 more
core   +1 more source

Characterizing the Lanthanide‐Binding Tag Grafted at Calmodulin Site 1: Affinity, Selectivity, and Coordination Properties

European Journal of Inorganic Chemistry, EarlyView.
Lanthanide affinity and selectivity in proteins remain poorly understood. Engineering calmodulin with a lanthanide‐binding tag at Site 1 boosts affinity from nanomolar (isolated LBTs) to picomolar dissociation constants, comparable to lanmodulin but with distinct selectivity.
Catherine Berthomieu, Manon Martin, Jean Aupiais, Tiffanie Barré, Loïc Daronnat, Jérémy Pansier, Nicolas Brémond, David Lemaire, Atul Thawari, Martin Levier, Laurence Berthon, Sandrine Sauge‐Merle   +11 more
wiley   +1 more source