Binding of the microbial cyclic tetrapeptide trapoxin A to the class I histone deacetylase HDAC8
NJ Porter, DW Christianson - ACS chemical biology, 2017 - ACS Publications
Trapoxin A is a microbial cyclic tetrapeptide that is an essentially irreversible inhibitor of
class I histone deacetylases (HDACs). The inhibitory warhead is the α, β-epoxyketone side …
class I histone deacetylases (HDACs). The inhibitory warhead is the α, β-epoxyketone side …
Potent histone deacetylase inhibitors built from trichostatin A and cyclic tetrapeptide antibiotics including trapoxin
R Furumai, Y Komatsu, N Nishino… - Proceedings of the …, 2001 - National Acad Sciences
Trichostatin A (TSA) and trapoxin (TPX) are potent inhibitors of histone deacetylases
(HDACs). TSA is proposed to block the catalytic reaction by chelating a zinc ion in the active …
(HDACs). TSA is proposed to block the catalytic reaction by chelating a zinc ion in the active …
Trapoxin A analogue as a selective nanomolar inhibitor of HDAC11
Histone deacetylases (HDACs) are enzymes that regulate many important biological
pathways. There is a need for the development of isoform-selective HDAC inhibitors for …
pathways. There is a need for the development of isoform-selective HDAC inhibitors for …
Macrocyclic octapeptide binding and inferences on protein substrate binding to histone deacetylase 6
Histone deacetylases (HDACs) are essential for the regulation of myriad biological
processes, and their aberrant function is implicated in cancer, neurodegeneration, and other …
processes, and their aberrant function is implicated in cancer, neurodegeneration, and other …
Structural basis of the antiproliferative activity of largazole, a depsipeptide inhibitor of the histone deacetylases
KE Cole, DP Dowling, MA Boone… - Journal of the …, 2011 - ACS Publications
Largazole is a macrocyclic depsipeptide originally isolated from the marine cyanobacterium
Symploca sp., which is indigenous to the warm, blue-green waters of Key Largo, Florida …
Symploca sp., which is indigenous to the warm, blue-green waters of Key Largo, Florida …
Design, synthesis, biological evaluation, and structural characterization of potent histone deacetylase inhibitors based on cyclic α/β-tetrapeptide architectures
A Montero, JM Beierle, CA Olsen… - Journal of the American …, 2009 - ACS Publications
Histone deacetylases (HDACs) are a family of enzymes found in bacteria, fungi, plants, and
animals that profoundly affect cellular function by catalyzing the removal of acetyl groups …
animals that profoundly affect cellular function by catalyzing the removal of acetyl groups …
Structural basis for the selective inhibition of HDAC10, the cytosolic polyamine deacetylase
CJ Herbst-Gervasoni, RR Steimbach… - ACS chemical …, 2020 - ACS Publications
The cytosolic class IIb histone deacetylase HDAC10 is an emerging target for drug design.
As an inducer of autophagy, its selective inhibition suppresses the autophagic response that …
As an inducer of autophagy, its selective inhibition suppresses the autophagic response that …
Selective inhibition of histone deacetylase 10: hydrogen bonding to the gatekeeper residue is implicated
M Géraldy, M Morgen, P Sehr… - Journal of medicinal …, 2019 - ACS Publications
The discovery of isozyme-selective histone deacetylase (HDAC) inhibitors is critical for
understanding the biological functions of individual HDACs and for validating HDACs as …
understanding the biological functions of individual HDACs and for validating HDACs as …
Synthesis of natural and modified trapoxins, useful reagents for exploring histone deacetylase function
J Taunton, JL Collins, SL Schreiber - Journal of the American …, 1996 - ACS Publications
Trapoxin, a cyclotetrapeptide isolated from the fungus Helicoma ambiens, profoundly affects
mammalian cell growth and morphology. In this paper, we describe syntheses of …
mammalian cell growth and morphology. In this paper, we describe syntheses of …
Phage‐assisted, active site‐directed ligand evolution of a potent and selective histone deacetylase 8 inhibitor
JS Morse, YJ Sheng, JT Hampton, LD Sylvain… - Protein …, 2022 - Wiley Online Library
Phage‐assisted, active site‐directed ligand evolution (PADLE) is a recently developed
technique that uses an amber codon‐encoded noncanonical amino acid (ncAA) as an …
technique that uses an amber codon‐encoded noncanonical amino acid (ncAA) as an …
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