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Jonathan D Macdonald

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Citations 214
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Recent Articles
1.
Maw J, Coker J, Arya T, Goins C, Sonawane D, Han S, et al.
J Med Chem . 2024 Feb; 67(4):2631-2666. PMID: 38330278
Citron kinase (CITK) is an AGC-family serine/threonine kinase that regulates cytokinesis. Despite knockdown experiments implicating CITK as an anticancer target, no selective CITK inhibitors exist. We transformed a previously reported...
2.
Rawat C, Ben-Salem S, Singh N, Chauhan G, Rabljenovic A, Vaghela V, et al.
Cancer Res . 2023 Oct; 83(24):4142-4160. PMID: 37801613
Significance: The poorly characterized protein kinase citron kinase is a therapeutic target in prostate cancer that drives tumor growth by regulating diverse substrates, which control several hallmarks of aggressive prostate...
3.
Hooper A, Macdonald J, Reilly B, Maw J, Wirrick A, Han S, et al.
Res Sq . 2023 May; PMID: 37214977
Starting from compound (CCF0058981), a structure-based optimization of the P1 subsite was performed against the severe acute respiratory syndrome coronavirus (SARS-CoV-2) main protease (3CL). Inhibitor and the compounds disclosed bind...
4.
Papay R, Macdonald J, Stauffer S, Perez D
Curr Res Pharmacol Drug Discov . 2022 Dec; 4:100142. PMID: 36544813
α-Adrenergic Receptors (ARs) are G-protein Coupled Receptors (GPCRs) that regulate the sympathetic nervous system via the binding and activation of norepinephrine (NE) and epinephrine (Epi). α-ARs control various aspects of...
5.
Han S, Goins C, Arya T, Shin W, Maw J, Hooper A, et al.
J Med Chem . 2021 Aug; 65(4):2880-2904. PMID: 34347470
Starting from the MLPCN probe compound ML300, a structure-based optimization campaign was initiated against the recent severe acute respiratory syndrome coronavirus (SARS-CoV-2) main protease (3CL). X-ray structures of SARS-CoV-1 and...
6.
Chacon Simon S, Wang F, Thomas L, Phan J, Zhao B, Olejniczak E, et al.
J Med Chem . 2020 Apr; 63(8):4315-4333. PMID: 32223236
The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to a tumorigenic state. Indeed, MYC is overexpressed in up to ∼50% of human cancers and...
7.
Tian J, Teuscher K, Aho E, Alvarado J, Mills J, Meyers K, et al.
J Med Chem . 2019 Dec; 63(2):656-675. PMID: 31858797
WD repeat domain 5 (WDR5) is a member of the WD40-repeat protein family that plays a critical role in multiple chromatin-centric processes. Overexpression of WDR5 correlates with a poor clinical...
8.
Macdonald J, Chacon Simon S, Han C, Wang F, Shaw J, Howes J, et al.
J Med Chem . 2019 Nov; 62(24):11232-11259. PMID: 31724864
The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy toward the inhibition of MYC...
9.
Aho E, Wang J, Gogliotti R, Howard G, Phan J, Acharya P, et al.
Cell Rep . 2019 Mar; 26(11):2916-2928.e13. PMID: 30865883
The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer. Drug discovery efforts center on the blockade of the "WIN site" of WDR5, a well-defined pocket that...
10.
Wang F, Jeon K, Salovich J, Macdonald J, Alvarado J, Gogliotti R, et al.
J Med Chem . 2018 Jun; 61(13):5623-5642. PMID: 29889518
WDR5 is a chromatin-regulatory scaffold protein overexpressed in various cancers and a potential epigenetic drug target for the treatment of mixed-lineage leukemia. Here, we describe the discovery of potent and...