Theodore M. Kamenecka

Microtubule Acetylation Regulates the Malignant Phenotype of Glioblastoma and is a Promising Therapeutic Target

This study identifies ATAT1 as a therapeutic target in glioblastoma by showing its role in promoting tumor invasion, proliferation, and resistance, with potential for combination therapies.

Selective Glucocorticoid Receptor Modulators of Immune Checkpoint Function

The paper develops selective glucocorticoid receptor modulators (SGRMs) that modulate immune checkpoint function by altering GR activity states through structural design and machine learning.

Shifting the PPARγ conformational ensemble towards a transcriptionally repressive state improves covalent inhibitor efficacy

The paper investigates how covalent inhibitors of PPARγ shift its conformational state, affecting ligand binding and inhibitor efficacy.

The Endo-GeneScreen Platform Identifies Drug-Like Probes that Regulate Endogenous Protein Levels within Physiological Contexts

The paper introduces Endo-GeneScreen, a platform that identifies small molecules regulating endogenous protein levels, and demonstrates its application in finding probes for Syngap1-related neurodevelopmental disorder.

Structural basis of PPARγ-mediated transcriptional repression by the covalent inverse agonist FX-909

This study compares FX-909 to other covalent PPARγ inverse agonists, showing improved corepressor-selective inverse agonism and stabilization of a repressive conformation.

MT-125 Inhibits Non-Muscle Myosin IIA and IIB, Synergizes with Oncogenic Kinase Inhibitors, and Prolongs Survival in Glioblastoma

Advancing Clinical Response Against Glioblastoma: Evaluating SHP1705 CRY2 Activator Efficacy in Preclinical Models and Safety in Phase I Trials

This paper evaluates the safety and efficacy of SHP1705, a CRY2 activator, in preclinical models and Phase I trials, showing improved efficacy against GBM stem cells and synergistic effects with a REV-ERB agonist.

Towards a unified molecular mechanism for ligand-dependent activation of NR4A-RXR heterodimers

This paper investigates the activation mechanism of NR4A-RXR heterodimers using a diverse RXR ligand set, revealing both classical and non-classical activation pathways.

Ligand efficacy shifts a nuclear receptor conformational ensemble between transcriptionally active and repressive states

This study identifies a PPARγ ligand series that shifts the receptor's conformational ensemble between active and repressive states, revealing how subtle chemical changes influence its function.

Development of novel flavonoid senolytics through phenotypic drug screening and drug design

This study develops two novel flavonoid senolytics through phenotypic drug screening and design, showing enhanced senolytic activity and healthspan extension in a mouse model.

Development of Clinically Viable Non-Muscle Myosin II Small Molecule Inhibitors with Broad Therapeutic Potential

This paper develops a selective non-muscle myosin II inhibitor, MT-228, with high brain penetration and efficacy in preclinical models, offering therapeutic potential for diseases like stimulant use disorder.

Methamphetamine learning induces persistent nonmuscle myosin II-dependent spine motility in the basolateral amygdala

The paper shows that METH learning causes long-lasting NMII-dependent spine motility in BLA neurons, which can be reversed by NMII inhibition.