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Pevonedistat

Context. Pevonedistat (Takeda) is a first-in-class intravenous or subcutaneous NEDD8-activating enzyme (NAE) inhibitor being developed for leukemia and advanced solid tumors. NAE is a pivotal regulator of the NEDD8 conjugation pathway which regulates the activity of the Cullin-RING ligases (CRLs), key proteins involved in the ubiquitin-proteasome system (UPS), controlling important physiological processes such as cell-cycle…

Compound 20

Context. “Compound 20” (Gedeon Richter) is an oral α5-GABAA receptor negative allosteric modulator (NAM) being developed for cognitive disorders. GABA receptor NAMs are known to exert effects opposite to the anxiolytic and anticonvulsant effects of positive allosteric modulators. However, NAM agents targeting α5-GABAA receptors, which have been implicated in learning and memory, have been heavily…

NVP-CLR457

Context. NVP-CLR457 (Novartis Institutes for BioMedical Research) is an oral, non-CNS-penetrating pan-class IA phosphoinositide 3-kinase (PI3K) inhibitor. Due to the key involvement of PI3K in the famed PI3K-Akt−mTOR pathway, whose deregulation has been observed in several cancers, it is no surprise that the last decade has seen over 600 medicinal chemistry-based publications and patents focusing…

TXA6101

Context. TXA6101 (TAXIS Pharmaceuticals) is a filamentous temperature-sensitive mutant Z (FtsZ) protein inhibitor being developed for targeting gram-negative bacteria. Drug resistance continues to be a paramount challenge in antibiotic therapy and there is an ongoing need to explore and develop novel antibacterial drugs. FtsZ has long been considered an attractive antibiotic target due to its…

RLX-33

Context. RLX-33 (Research Triangle Institute) is a nonpeptide relaxin-3/RXFP3 system antagonist. Evidence over the last 2 decades, since the discovery of relaxin‐3 in 2001, suggests that the protein, through its receptor RXFP3, regulates responses to stress, anxiety-related and motivated behaviors, circadian rhythms, learning and memory, and alcohol-seeking behavior, making the relaxin-3/RXFP3 system a desirable target…

INCB13739

Context. INCB13739 (Incyte) is an oral 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) antagonist. Inhibition of the tissue-specific generation of cortisol using agents that antagonize 11β-HSD1, the key metabolic enzyme involved in the conversion of inactive glucocorticoids to active ones, has been considered a desirable therapeutic strategy for type 2 diabetes and metabolic syndrome. Indeed, at least 25…