Receptor-mediated delivery of CRISPR-Cas9 endonuclease for cell-type-specific gene editing
CRISPR-Cas RNA-guided endonucleases hold great promise for disrupting or correcting
genomic sequences through site-specific DNA cleavage and repair. However, the lack of …
genomic sequences through site-specific DNA cleavage and repair. However, the lack of …
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo [3.2. 1] octane class of sodium-dependent glucose cotransporter 2 inhibitors
V Mascitti, TS Maurer, RP Robinson… - Journal of medicinal …, 2011 - ACS Publications
Compound 4 (PF-04971729) belongs to a new class of potent and selective sodium-dependent
glucose cotransporter 2 inhibitors incorporating a unique dioxa-bicyclo[3.2.1]octane (…
glucose cotransporter 2 inhibitors incorporating a unique dioxa-bicyclo[3.2.1]octane (…
Application of fundamental organometallic chemistry to the development of a gold‐catalyzed synthesis of sulfinate derivatives
…, NP Mankad, RG Bergman, V Mascitti… - Angewandte Chemie …, 2014 - Wiley Online Library
The development of a gold(I)‐catalyzed sulfination of aryl boronic acids is described. This
transformation proceeds through an unprecedented mechanism which exploits the reactivity of …
transformation proceeds through an unprecedented mechanism which exploits the reactivity of …
Palladium‐Catalyzed Synthesis of (Hetero) Aryl Alkyl Sulfones from (Hetero) Aryl Boronic Acids, Unactivated Alkyl Halides, and Potassium Metabisulfite
A Shavnya, KD Hesp, V Mascitti… - Angewandte Chemie …, 2015 - Wiley Online Library
A palladium‐catalyzed one‐step synthesis of (hetero)aryl alkyl sulfones from (hetero)arylboronic
acids, potassium metabisulfite, and unactivated or activated alkylhalides is described. …
acids, potassium metabisulfite, and unactivated or activated alkylhalides is described. …
Total synthesis of (±)-pentacycloanammoxic acid
V Mascitti, EJ Corey - Journal of the American Chemical Society, 2004 - ACS Publications
The first total synthesis of (±)-pentacycloanammoxic acid/methyl ester (1), an unusual naturally
occurring fatty acid from Candidatus Brocadia anammoxidans, has been accomplished …
occurring fatty acid from Candidatus Brocadia anammoxidans, has been accomplished …
Enantioselective synthesis of pentacycloanammoxic acid
V Mascitti, EJ Corey - Journal of the American Chemical Society, 2006 - ACS Publications
A highly effective enantioselective synthesis of pentacycloanammoxic acid (1), an unusual
naturally occurring fatty acid from Candidatus Brocadia anammoxidans, has been …
naturally occurring fatty acid from Candidatus Brocadia anammoxidans, has been …
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects
Z Miao, G Nucci, N Amin, R Sharma, V Mascitti… - Drug Metabolism and …, 2013 - ASPET
The disposition of ertugliflozin (PF-04971729), an orally active selective inhibitor of the
sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [ 14 C]-…
sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [ 14 C]-…
Metabolism-guided drug design
AF Stepan, V Mascitti, K Beaumont, AS Kalgutkar - MedChemComm, 2013 - pubs.rsc.org
Preclinical drug metabolism studies play a key role in the lead identification and optimization
process in drug discovery. Characterization of the metabolic pathways of new chemical …
process in drug discovery. Characterization of the metabolic pathways of new chemical …
Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists
…, S Liras, PM Loria, V Mascitti… - Journal of medicinal …, 2015 - ACS Publications
Cyclic constraints are incorporated into an 11-residue analogue of the N-terminus of
glucagon-like peptide-1 (GLP-1) to investigate effects of structure on agonist activity. Cyclization …
glucagon-like peptide-1 (GLP-1) to investigate effects of structure on agonist activity. Cyclization …
Palladium-catalyzed sulfination of aryl and heteroaryl halides: direct access to sulfones and sulfonamides
A Shavnya, SB Coffey, AC Smith, V Mascitti - Organic letters, 2013 - ACS Publications
A novel palladium-catalyzed sulfination of aryl and heteroaryl halides is described. This
reaction operates under mild conditions and provides access to a wide range of aryl and …
reaction operates under mild conditions and provides access to a wide range of aryl and …