Search Results - "Huerta, Fidel"
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Tuning site-specific dynamics to drive allosteric activation in a pneumococcal zinc uptake regulator
Published in eLife (17-10-2018)“…MarR (multiple antibiotic resistance repressor) family proteins are bacterial repressors that regulate transcription in response to a wide range of chemical…”
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Journal Article -
2
Conserved residues of the Pro103-Arg115 loop are involved in triggering the allosteric response of the Escherichia coli ADP-glucose pyrophosphorylase
Published in Protein science (01-05-2015)“…The synthesis of glycogen in bacteria and starch in plants is allosterically controlled by the production of ADP-glucose by ADP-glucose pyrophosphorylase…”
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Journal Article -
3
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions
Published in Journal of medicinal chemistry (27-04-2023)“…Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs), theoretically possess a catalytic mode-of-action, yet few studies have either…”
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Journal Article -
4
Biophysical Chemistry of Zinc Homeostasis in the Human Pathogen Streptococcus pneumoniae
Published 01-01-2020“…ZnII homeostasis is important for S. pneumoniae colonization of the upper respiratory tract and migration to sites of infection as zinc availability changes as…”
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Dissertation -
5
HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development
Published in ACS chemical biology (21-04-2023)“…The ability to rapidly and selectively modulate cellular protein levels using small molecules is essential for studying complex biological systems. Degradation…”
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Journal Article -
6
Tracing an Allosteric Pathway in Escherichia coli ADP‐glucose Pyrophosphorylase
Published in The FASEB journal (01-04-2015)“…Abstract only…”
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Journal Article -
7
The Agrobacterium tumefaciens ADP‐Glucose Pyrophosphorylase G329D Mutant Exists in a Pre‐Activated State
Published in The FASEB journal (01-04-2016)“…Allosteric regulation of ADP‐glucose (ADP‐Glc PPase, EC 2.7.7.27) is critical for determining the amount of glycogen and starch that gets synthesized in…”
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Journal Article -
8
Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
Published in RSC chemical biology (01-11-2023)“…Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras (PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We…”
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Journal Article -
9
Cereblon covalent modulation through structure-based design of histidine targeting chemical probes
Published in RSC chemical biology (31-08-2022)“…Electrophilic biocompatible warheads, particularly cysteine-reactive acrylamides, have enabled the development of covalent inhibitor drugs and chemical biology…”
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Journal Article -
10
Advancing targeted protein degrader discovery by measuring cereblon engagement in cells
Published in Methods in enzymology (2023)“…Measurement of target engagement in cells is critical to understand the molecular pharmacology of drugs and chemical probes. Many targeted protein degraders…”
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Journal Article -
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Abstract 3426: Catalytic degraders effectively address kinase site mutations in EML-ALK oncogenic fusions
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs), is an emerging modality for drug discovery, and theoretically possess…”
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Journal Article