Nick A. Paras
University of California, San Francisco
Amine gas treatingStereocenterEnantioselective synthesisReactivity (chemistry)Medicinal chemistryCatalysisLewis acids and basesAlkylationOrganic chemistryNucleophileAqueous solutionChemistryStereospecificityAromaticityIndole testFriedel–Crafts reactionIn vivoCombinatorial chemistryHydroxylaminePrimary (chemistry)NeurodegenerationEne reactionIminiumSulfonateDiseaseAldehydeAlkylTolterodineOrganic chemicalsMetal saltsEnantiomeric excessSynthonAmino acidYield (chemistry)BiochemistryAldol reactionMedicineAddition reaction
23Publications
10H-index
1,030Citations
Publications 20
Newest
#1Ghahyun J. Kim (UCSF: University of California, San Francisco)H-Index: 2
#2Han Mo (McGovern Institute for Brain Research)H-Index: 1
Last. Longping Peng (SHU: Shanghai University)H-Index: 1
view all 21 authors...
Parkinson’s disease is caused by the slow death and deterioration of brain cells, in particular of the neurons that produce a chemical messenger known as dopamine. Certain drugs can mitigate the resulting drop in dopamine levels and help to manage symptoms, but they cause dangerous side-effects. There is no treatment that can slow down or halt the progress of the condition, which affects 0.3% of the population globally. Many factors, both genetic and environmental, contribute to the emergence of...
Source
#1Ghahyun J. Kim (UCSF: University of California, San Francisco)H-Index: 2
#2Han Mo (McGovern Institute for Brain Research)H-Index: 1
Last. Longping Peng (SHU: Shanghai University)H-Index: 1
view all 21 authors...
Source
#1Terrence-Thang H. Nguyen (UCSF: University of California, San Francisco)
#2Connor J. O’Brien (UCSF: University of California, San Francisco)H-Index: 1
Last. Jay Conrad (UCSF: University of California, San Francisco)H-Index: 2
view all 8 authors...
The development of a water-soluble iridium catalyst enables the trifluoromethylation of polar small molecules and peptides in DMSO solution or aqueous media. The reaction was optimized in a microtiter plate format under ambient air, using commercial Langlois reagent as a CF3 radical source, blue LEDs for excitation, and using DPBS as solvent to provide up to 60% CF3- peptide.
Source
#1Cedric Lozano (UCSF: University of California, San Francisco)
#2Cristian Ramirez (UCSF: University of California, San Francisco)
Last. Jay Conrad (UCSF: University of California, San Francisco)H-Index: 2
view all 7 authors...
In the literature, C-N coupling methods for the reaction of iodo-oxazole with 2-pyridinone were found to be low yielding. C-N coupling using silver benzoate additives with CuI catalysts and 4,7-dimethoxy-1,10-phenanthroline ligands has been developed to afford synthetically useful yields of the desired heterobicycle product. The reaction conditions are applied to the coupling of a range of iodo-heterocycles with 2-pyridinone. The coupling of a variety of NH-containing heterocycles with 4-iodo-ox...
Source
#1Daniel Wong (UCSF: University of California, San Francisco)H-Index: 15
#2Jay Conrad (UCSF: University of California, San Francisco)H-Index: 2
Last. Michael J. Keiser (UCSF: University of California, San Francisco)H-Index: 24
view all 12 authors...
In microscopy-based drug screens, fluorescent markers carry critical information on how compounds affect different biological processes. However, practical considerations may hinder the use of certain fluorescent markers. Here, we present a deep learning method for overcoming this limitation. We accurately generated predicted fluorescent signals from other related markers, and validated this new machine learning (ML) method on two biologically distinct datasets. We used the ML method to improve ...
Source
#1Yi LiH-Index: 9
#2Roy J. Vaz (UCSF: University of California, San Francisco)H-Index: 1
Last. Jay Conrad (UCSF: University of California, San Francisco)H-Index: 2
view all 6 authors...
The addition of electron deficient radicals to the C2 position of indoles has been described in the literature as opposed to electrophilic addition at the C3 position. Density functional theory calculations were used to understand the switch in regioselectivity from C3 to C2 for indole to undergo radical additions. Electron deficient radicals have a lower barrier for reaction at C2 and a lower energy radical intermediate that benefits from benzylic radical stabilization. Trifluoromethyl radical ...
Source
#1Jacob I. Ayers (UCSF: University of California, San Francisco)H-Index: 18
#2Nick A. Paras (UCSF: University of California, San Francisco)H-Index: 10
Last. Stanley B. Prusiner (UCSF: University of California, San Francisco)H-Index: 189
view all 3 authors...
Prions were initially discovered in studies of scrapie, a transmissible neurodegenerative disease (ND) of sheep and goats thought to be caused by slow viruses. Once scrapie was transmitted to rodents, it was discovered that the scrapie pathogen resisted inactivation by procedures that modify nucleic acids. Eventually, this novel pathogen proved to be a protein of 209 amino acids, which is encoded by a chromosomal gene. After the absence of a nucleic acid within the scrapie agent was established,...
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#1Jean-Marc M. Grandjean (UCSF: University of California, San Francisco)H-Index: 2
#2Alexander Y. Jiu (UCSF: University of California, San Francisco)H-Index: 2
Last. Nick A. Paras (UCSF: University of California, San Francisco)H-Index: 10
view all 20 authors...
Tau prions feature in the brains of patients suffering from Alzheimer’s disease and other tauopathies. For the development of therapeutics that target the replication of tau prions, a high-content, fluorescence-based cell assay was developed. Using this high-content phenotypic screen for nascent tau prion formation, a 4-piperazine isoquinoline compound (1) was identified as a hit with an EC50 value of 390 nM and 0.04 Kp,uu. Analogs were synthesized using a hypothesis-based approach to improve po...
Source
#1Sean Caenepeel (Amgen)H-Index: 21
#2Sean P. Brown (Amgen)H-Index: 16
Last. Paul E. Hughes (Amgen)H-Index: 32
view all 38 authors...
The prosurvival BCL2 family member MCL1 is frequently dysregulated in cancer. To overcome the significant challenges associated with inhibition of MCL1 protein–protein interactions, we rigorously applied small-molecule conformational restriction, which culminated in the discovery of AMG 176, the first selective MCL1 inhibitor to be studied in humans. We demonstrate that MCL1 inhibition induces a rapid and committed step toward apoptosis in subsets of hematologic cancer cell lines, tumor xenograf...
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#1Connor J. O’Brien (UCSF: University of California, San Francisco)H-Index: 1
#2Daniel G. Droege (UCSF: University of California, San Francisco)H-Index: 2
Last. Jay Conrad (UCSF: University of California, San Francisco)H-Index: 2
view all 7 authors...
The direct cyanomethylation of indoles at the 2- or 3-position was achieved via photoredox catalysis. The versatile nitrile synthon is introduced as a radical generated from bromoacetonitrile, a photocatalyst, and blue LED as a light source. The mechanism of the reaction is explored by determination of the Stern–Volmer quenching constants. By combining photophysical data and mass spectrometry to follow the catalyst decomposition, the catalyst ligands were tuned to enable synthetically useful yie...
Source
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