Results 71 to 80 of about 8,600 (184)

Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients.

PLoS ONE, 2013
UnlabelledBelinostat is a hydroxamate class HDAC inhibitor that has demonstrated activity in peripheral T-cell lymphoma and is undergoing clinical trials for non-hematologic malignancies.
Ling-Zhi Wang, Jacqueline Ramírez, Winnie Yeo, Mei-Yi Michelle Chan, Win-Lwin Thuya, Jie-Ying Amelia Lau, Seow-Ching Wan, Andrea Li-Ann Wong, Ying-Kiat Zee, Robert Lim, Soo-Chin Lee, Paul C Ho, How-Sung Lee, Anthony Chan, Sherry Ansher, Mark J Ratain, Boon-Cher Goh   +16 more
doaj   +1 more source

Making Blank Faces Expressive: Chemical Approaches to the Modification of Chemically Inert Peptides

Journal of Peptide Science, Volume 32, Issue 3, March 2026.
As an alternative to the conventional approach, which combines amino acid monomers in a one‐by‐one fashion to peptide derivatives, the chemical modification of existing peptides has attracted significant attention in recent years. However, such approaches generally target the reactive functional groups in cysteine and lysine residues, particularly in ...
Yoshitaka Moriyama, Hikari Sada, Takeshi Nanjo   +2 more
wiley   +1 more source

The Diverse Binding Modes Explain the Nanomolar Levels of Inhibitory Activities Against 1-Deoxy-d-Xylulose 5-Phosphate Reductoisomerase from Plasmodium falciparum Exhibited by Reverse Hydroxamate Analogs of Fosmidomycin with Varying N-Substituents

Molecules
It is established that reverse hydroxamate analogs of fosmidomycin inhibit the growth of Plasmodium falciparum by inhibiting 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR), the second enzyme of the non-mevalonate pathway, which is absent in humans.
Sana Takada, Mona A. Abdullaziz, Stefan Höfmann, Talea Knak, Shin-ichiro Ozawa, Yasumitsu Sakamoto, Thomas Kurz, Nobutada Tanaka   +7 more
doaj   +1 more source

Leveraging the ADAM10 prodomain for selective inhibition to enhance recovery after myocardial infarction

British Journal of Pharmacology, Volume 183, Issue 5, Page 990-1008, March 2026.
Background and Purpose Inflammation plays a crucial role in the development and progression of numerous acute and chronic diseases such as myocardial infarction (MI) and heart failure. Targeting ADAM proteases, particularly ADAM10, holds promise for fine‐tuning inflammatory responses.
Erik Klapproth, Johanna Marks, Patrick Diaba‐Nuhoho, Sören Grell, Paul Leubauer, Susanne Kämmerer, Johannes R. Soltwedel, Fred Rasmussen, Felix Mejia, Marcia L. Moss, Christopher Prince, Peter Mirtschink, Ben Wielockx, Paul Saftig, Michael Wagner, Kristina Lorenz, Ali El‐Armouche   +16 more
wiley   +1 more source

Development of Matrix Metalloproteinase-2 Inhibitors for Cardioprotection [PDF]

, 2018
The objective of our present study is to develop novel inhibitors for MMP-2 for acute cardioprotection. In a series of pilot studies, novel substituted carboxylic acid derivatives were synthesized based on imidazole and thiazole scaffolds and then tested
Adhikari, Agamennone, Ali, Almstead, Alwan, Ammazzalorso, Andreadou, Baig, Bencsik, Bencsik, Bencsik, Bencsik, Cheung, D'Annunzio, DeCoux, Dhanaraj, Di Pizio, Dormán, Duan, Durrant, Fekete, Feng, Ferdinandy, Ferdinandy, Fisher, Galardy, Giricz, Gorbe, Hausenloy, Hudson, Johnson, Jones, Jun, Kalászi, Kupai, Li, Lipinski, Papp, Roth, Sawicki, Sung, Turan, Wang, Willett, Willett, Yamamoto   +45 more
core   +4 more sources

Evolution of lysine and arginine biosynthesis revealed by substrate specificity of lysine biosynthetic enzymes in Thermus thermophilus

The FEBS Journal, Volume 293, Issue 6, Page 1727-1740, March 2026.
Two enzymes from the Thermus thermophilus lysine biosynthetic pathway, LysZ and LysY, unexpectedly exhibit substrate promiscuity. They are able to recognize the LysW intermediates utilized by the ArgW‐mediated arginine route, even though the bacterium already possesses the canonical arginine biosynthetic pathway.
Wenyuan Shi, Ayako Yoshida, Saori Kosono, Makoto Nishiyama   +3 more
wiley   +1 more source

Neurogenesis and the Epigenetic Landscape: Role of Histone Modifications and Chromatin Remodeling

Brain and Behavior, Volume 16, Issue 2, February 2026.
Histone methylation and acetylation modulate gene expression by inducing chromatin condensation or relaxation, which in turn regulates transcriptional activity and impacts neurogenesis. ABSTRACT Aims The purpose of this review is to examine how epigenetic regulation particularly chromatin modification and histone methylation controls gene expression ...
Degisew Yinur Mengistu, Biniam Moges Eskeziyaw   +1 more
wiley   +1 more source

Angiotensin-converting enzyme secretase is inhibited by zinc metalloprotease inhibitors and requires its substrate to be inserted in a lipid bilayer [PDF]

, 1997
Mammalian angiotensin-converting enzyme (ACE; EC 3.4.15.1) is one of several proteins that exist in both membrane-bound and soluble forms as a result of a post-translational proteolytic processing event.
S. PARVATHY, Sylvester Y. OPPONG, Eric H. KARRAN, Derek R. BUCKLE, Anthony J. TURNER, Nigel M. HOOPER   +5 more
core   +1 more source

Characterization of Ru(II) Polypyridyl Photosensitizers Bound to TiO2 Supports Through a New Covalent Metal‐Ester Bonding Motif

ChemCatChem, Volume 18, Issue 2, 28 January 2026.
ABSTRACT The development of photoelectrochemical (PEC) devices involves the attachment of molecular photosensitizers onto solid supports. Particularly significant to this work are PECs that rely on ruthenium‐based photosensitizers on high band gap metal oxide (MOx) supports.
D. M. S. C. Dissanayake, Christopher T. LeBarron, Laura C. Maybach, Joseph J. Kuchta III, Seyyedamirhossein Hosseini, Aaron K. Vannucci   +5 more
wiley   +1 more source

Glyoxalase‐1 Inhibition Leads to Ferroptosis Induction in Lung Cancer Cells: A Dual Mechanism of Action of Hydroxamic Acids Derived from Cysteine

ChemMedChem, Volume 21, Issue 1, January 2026.
A set of three cysteine‐derived hydroxamic acids were synthesized and evaluated for human gloxalase‐1 inhibition and ferroptosis induction activities. Among them, compound 2 exhibited a potent inhibitory effect against human glyoxalase‐1 and induced ferroptosis in non‐small cell lung cancer cell lines, increasing reactive oxygen species production and ...
Josué Martínez‐Miranda, Dolores Aguilar‐Cázares, Angélica Flores–Flores, Miguel Ángel Santos‐Contreras, José S. López‐González, Rodrigo Aguayo‐Ortiz, Rogélio Hernández‐Pando, Francisco Hernández‐Luis   +7 more
wiley   +1 more source