Santosh Keshipeddy
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View article: HMGB2 is a potential diagnostic marker and therapeutic target for liver fibrosis and cirrhosis
HMGB2 is a potential diagnostic marker and therapeutic target for liver fibrosis and cirrhosis Open
Background: High mobility group proteins 1 and 2 (HMGB1 and HMGB2) are 80% conserved in amino acid sequence. The function of HMGB1 in inflammation and fibrosis has been extensively characterized. However, an unaddressed central question is…
View article: Data from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound
Data from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound Open
AK3 compounds are mitotic arrest agents that induce high levels of γH2AX during mitosis and apoptosis following release from arrest. We synthesized a potent AK3 derivative, AK306, that induced arrest and apoptosis of the HCT116 colon cance…
View article: Data from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound
Data from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound Open
AK3 compounds are mitotic arrest agents that induce high levels of γH2AX during mitosis and apoptosis following release from arrest. We synthesized a potent AK3 derivative, AK306, that induced arrest and apoptosis of the HCT116 colon cance…
View article: Supplemental Material, Figures 1, 2 and 3 from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound
Supplemental Material, Figures 1, 2 and 3 from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound Open
S1: Results from AK306 testing on the NCI60 cancer cell line panel. Testing was done by the National Institutes of Health Developmental Therapeutics Program. S2: AK3-BODIPY arrests YAMC cells in mitosis at 600 and 800 nM. YAMCs were treate…
View article: Supplemental Material, Figures 1, 2 and 3 from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound
Supplemental Material, Figures 1, 2 and 3 from Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound Open
S1: Results from AK306 testing on the NCI60 cancer cell line panel. Testing was done by the National Institutes of Health Developmental Therapeutics Program. S2: AK3-BODIPY arrests YAMC cells in mitosis at 600 and 800 nM. YAMCs were treate…
View article: Chiral evasion and stereospecific antifolate resistance in Staphylococcus aureus
Chiral evasion and stereospecific antifolate resistance in Staphylococcus aureus Open
Antimicrobial resistance presents a significant health care crisis. The mutation F98Y in Staphylococcus aureus dihydrofolate reductase (SaDHFR) confers resistance to the clinically important antifolate trimethoprim (TMP). Propargyl-linked …
View article: Amide-Linked C4″-Saccharide Modification of KRN7000 Provides Potent Stimulation of Human Invariant NKT Cells and Anti-Tumor Immunity in a Humanized Mouse Model
Amide-Linked C4″-Saccharide Modification of KRN7000 Provides Potent Stimulation of Human Invariant NKT Cells and Anti-Tumor Immunity in a Humanized Mouse Model Open
Activation of invariant natural killer T (iNKT) cells by α-galactosylceramides (α-GalCers) stimulates strong immune responses and potent anti-tumor immunity. Numerous modifications of the glycolipid structure have been assessed to derive a…
View article: Chiral evasion and stereospecific antifolate resistance in<i>Staphylococcus aureus</i>
Chiral evasion and stereospecific antifolate resistance in<i>Staphylococcus aureus</i> Open
Antimicrobial resistance is a health care crisis. The resistance-conferring mutation F98Y in Staphylococcus aureus dihydrofolate reductase (SaDHFR) reduces effectiveness of antifolates, e.g., trimethoprim (TMP). Although propargyl-linked a…
View article: Post-Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules
Post-Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules Open
Many small molecule natural products with antibiotic and antiproliferative activity are adorned with a carbohydrate residue as part of their molecular structure. The carbohydrate moiety can act to mediate key interactions with the target, …
View article: Post Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules
Post Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules Open
Many small molecule natural products with are adorned with a carbohydrate as part of their molecular structure that acts to mediate key interactions with the target, attenuate physicochemical properties, or both. Facile incorporation of a …
View article: Post Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules
Post Glycosylation Diversification (PGD): An Approach for Assembling Collections of Glycosylated Small Molecules Open
Many small molecule natural products with are adorned with a carbohydrate as part of their molecular structure that acts to mediate key interactions with the target, attenuate physicochemical properties, or both. Facile incorporation of a …
View article: Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound
Spindle Assembly Disruption and Cancer Cell Apoptosis with a CLTC-Binding Compound Open
AK3 compounds are mitotic arrest agents that induce high levels of γH2AX during mitosis and apoptosis following release from arrest. We synthesized a potent AK3 derivative, AK306, that induced arrest and apoptosis of the HCT116 colon cance…
View article: High‐mobility‐group protein 2 regulated by microRNA‐127 and small heterodimer partner modulates pluripotency of mouse embryonic stem cells and liver tumor initiating cells
High‐mobility‐group protein 2 regulated by microRNA‐127 and small heterodimer partner modulates pluripotency of mouse embryonic stem cells and liver tumor initiating cells Open
High‐mobility‐group protein 2 (HMGB2) expression is up‐regulated in human liver cancer; however, little is known about its regulatory function. Here, we establish HMGB2 as a new modulator of the pluripotency of mouse embryonic stem cells. …
View article: Scaling Proteome-Wide Reactions of Activity-Based Probes
Scaling Proteome-Wide Reactions of Activity-Based Probes Open
Unified analysis of complex reactions of an activity-based probe with proteins in a proteome remains an unsolved challenge. We propose a power expression, rate = kobs[Probe]α, for scaling the progress of proteome-wide reactions and use the…
View article: Direct Substitution of Arylalkynyl Carbinols Provides Access to Diverse Terminal Acetylene Building Blocks
Direct Substitution of Arylalkynyl Carbinols Provides Access to Diverse Terminal Acetylene Building Blocks Open
To develop next generation antifolates for the treatment of trimethoprim-resistant bacteria, synthetic methods were needed to prepare a diverse array of 3-aryl-propynes with various substitutions at the propargyl position. A direct route w…
View article: Propargyl-Linked Antifolates Are Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis
Propargyl-Linked Antifolates Are Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis Open
Mycobacterium tuberculosis continues to cause widespread, life-threatening disease. In the last decade, this threat has grown dramatically as multi- and extensively-drug resistant (MDR and XDR) bacteria have spread globally and the number …
View article: Charged Propargyl-Linked Antifolates Reveal Mechanisms of Antifolate Resistance and Inhibit Trimethoprim-Resistant MRSA Strains Possessing Clinically Relevant Mutations
Charged Propargyl-Linked Antifolates Reveal Mechanisms of Antifolate Resistance and Inhibit Trimethoprim-Resistant MRSA Strains Possessing Clinically Relevant Mutations Open
Drug-resistant enzymes must balance catalytic function with inhibitor destabilization to provide a fitness advantage. This sensitive balance, often involving very subtle structural changes, must be achieved through a selection process invo…
View article: Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens
Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens Open
Although classical, negatively charged antifolates such as methotrexate possess high affinity for the dihydrofolate reductase (DHFR) enzyme, they are unable to penetrate the bacterial cell wall, rendering them poor antibacterial agents. He…
View article: Atypical natural killer T-cell receptor recognition of CD1d–lipid antigens
Atypical natural killer T-cell receptor recognition of CD1d–lipid antigens Open
Crucial to Natural Killer T (NKT) cell function is the interaction between their T-cell receptor (TCR) and CD1d-antigen complex. However, the diversity of the NKT cell repertoire and the ensuing interactions with CD1d-antigen remain unclea…
View article: Nonracemic Antifolates Stereoselectively Recruit Alternate Cofactors and Overcome Resistance in <i>S</i>. <i>aureus</i>
Nonracemic Antifolates Stereoselectively Recruit Alternate Cofactors and Overcome Resistance in <i>S</i>. <i>aureus</i> Open
While antifolates such as Bactrim (trimethoprim-sulfamethoxazole; TMP-SMX) continue to play an important role in treating community-acquired methicillin-resistant Staphylococcus aureus (CA-MRSA), resistance-conferring mutations, specifical…