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Paul Tawa

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Articles 24
Citations 258
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Recent Articles
1.
Metwally E, Mak V, Soriano A, Zebisch M, Leonardo Silvestre H, McEwan P, et al.
Commun Biol . 2023 Jul; 6(1):798. PMID: 37524852
cGMP-dependent protein kinase I-α (PKG1α) is a target for pulmonary arterial hypertension due to its role in the regulation of smooth muscle function. While most work has focused on regulation...
2.
Trowbridge A, Seath C, Rodriguez-Rivera F, Li B, Dul B, Schwaid A, et al.
Proc Natl Acad Sci U S A . 2022 Aug; 119(34):e2208077119. PMID: 35969791
Over half of new therapeutic approaches fail in clinical trials due to a lack of target validation. As such, the development of new methods to improve and accelerate the identification...
3.
Tawa P, Zhang L, Metwally E, Hou Y, McCoy M, Seganish W, et al.
J Biol Chem . 2022 Jul; 298(9):102284. PMID: 35868561
cGMP-dependent protein kinase (PKG) represents a compelling drug target for treatment of cardiovascular diseases. PKG1 is the major effector of beneficial cGMP signaling which is involved in smooth muscle relaxation...
4.
Hanisak J, Soriano A, Adam G, Basso A, Bauman D, Bell D, et al.
ACS Med Chem Lett . 2021 Aug; 12(8):1275-1282. PMID: 34413956
PKG1α is a central node in cGMP signaling. Current therapeutics that look to activate this pathway rely on elevation of cGMP levels and subsequent activation of PKG1α. Direct activation of...
5.
Daurio N, Zhou H, Chen Y, Sheth P, Imbriglio J, McLaren D, et al.
ACS Chem Biol . 2020 Sep; 15(10):2623-2635. PMID: 32930572
The ability to target specific proteins for degradation may open a new door toward developing therapeutics. Although effort in chemistry is essential for advancing this modality, i.e., one needs to...
6.
Bennett F, Buevich A, Huang H, Girijavallabhan V, Kerekes A, Huang Y, et al.
Bioorg Med Chem Lett . 2017 Oct; 27(23):5349-5352. PMID: 29056248
(2'R)-Ethynyl uridine 3, and its (2'S)-diastereomer 10, are synthesised in a divergent fashion from the inexpensive parent nucleoside. Both nucleoside analogues are obtained from a total of 5 simple synthetic...
7.
Lai M, Tawa P, Auger A, Wang D, Su H, Yan Y, et al.
J Antimicrob Chemother . 2017 Oct; 73(1):109-117. PMID: 29029095
Objectives: The increasing prevalence of mutations in HIV-1 reverse transcriptase (RT) that confer resistance to existing NRTIs and NNRTIs underscores the need to develop RT inhibitors with novel mode-of-inhibition and...
8.
Mandal M, Tan Z, Madsen-Duggan C, Buevich A, Caldwell J, Dejesus R, et al.
J Med Chem . 2017 Mar; 60(9):3851-3865. PMID: 28322556
We describe our optimization efforts to improve the physicochemical properties, solubility, and off-target profile of 1, an inhibitor of TarO, an early stage enzyme in the biosynthetic pathway for wall...
9.
Lee S, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, et al.
Sci Transl Med . 2016 Mar; 8(329):329ra32. PMID: 26962156
The widespread emergence of methicillin-resistant Staphylococcus aureus (MRSA) has dramatically eroded the efficacy of current β-lactam antibiotics and created an urgent need for new treatment options. We report an S....
10.
Cote B, Burch J, Asante-Appiah E, Bayly C, Bedard L, Blouin M, et al.
Bioorg Med Chem Lett . 2014 Jan; 24(3):917-22. PMID: 24412110
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile...