Beata Zamlynny

Potent targeted activator of cell kill molecules eliminate cells expressing HIV-1

Carl J. Balibar, Daniel J. Klein, Beata Zamlynny, Tracy L. Diamond et autres

Antiretroviral therapy inhibits HIV-1 replication but is not curative due to establishment of a persistent reservoir after virus integration into the host genome. Reservoir reduction is therefore an important HIV-1 cure strategy. Some HIV-1 nonnucleoside reverse transcriptase inhibitors induce HIV-1 selective cytotoxicity …

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Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing

Derun Li, David L. Sloman, Abdelghani Achab, Hua Zhou et autres

3,3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and cyclobutane functionalities. We report the discovery of a novel class of oxetane indole-amine 2,3-dioxygenase (IDO1) inhibitors suitable for Q3W (once every 3 weeks) oral and parenteral dosing. A diamide class of IDO …

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Structural insights on ligand recognition at the human leukotriene B4 receptor 1

Nairie Michaelian, Anastasiia Sadybekov, Élie Besserer‐Offroy, Gye Won Han et autres

The leukotriene B4 receptor 1 (BLT1) regulates the recruitment and chemotaxis of different cell types and plays a role in the pathophysiology of infectious, allergic, metabolic, and tumorigenic human diseases. Here we present a crystal structure of human BLT1 (hBLT1) in complex …

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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation

Chuan Hong, Noel Byrne, Beata Zamlynny, Srivanya Tummala et autres

Abstract Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain’s ability to control sleep-wake cycles. Current therapies are limited to the management of symptoms with modest effectiveness and substantial adverse effects. Agonists of the orexin receptor 2 (OX2R) …

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Orexin Receptor 2 (OX2R) in Complex with G Protein and Small-Molecule Agonist Compound 1

Chuan Hong, Noel Byrne, Beata Zamlynny, Srivanya Tummala et autres

Orexin Receptor 2 (OX2R) in Complex with G Protein and Natural Peptide-Agonist Orexin B (OxB)

Chun‐Gu Hong, Noel Byrne, Beata Zamlynny, Srivanya Tummala et autres

Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization

Kun Liu, Ravi Kurukulasuriya, Kevin D. Dykstra, Lisa DiMichelle et autres

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Structural basis for selectivity and diversity in angiotensin II receptors

Haitao Zhang, Gye Won Han, A. Batyuk, Andrii Ishchenko et autres

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XFEL structure of human angiotensin II type 2 receptor (Monoclinic form) in complex with compound 1 (N-benzyl-N-(2-ethyl-4-oxo-3-{[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl])

H. Zhang, G.W. Han, A. Batyuk, Andrii Ishchenko et autres

Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder

Jerry Di Salvo, Hiroshi Nagabukuro, L. Alexandra Wickham, Catherine Abbadie et autres

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Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists

Anthony K. Ogawa, Ellen Vande Bunte, Rudrajit Mal, Ping Lan et autres

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CCDC 1421635: Experimental Crystal Structure Determination

Scott D. Edmondson, Cheng Zhu, Nam Fung Kar, Jerry Di Salvo et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …