Vijay Chudasama
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View article: Triggered “Capture-and-Release” Enables a High-Affinity Rebinding Strategy for Sensitivity Enhancement in Lateral Flow Assays
Triggered “Capture-and-Release” Enables a High-Affinity Rebinding Strategy for Sensitivity Enhancement in Lateral Flow Assays Open
Lateral flow assays (LFAs) are point-of-care devices that are known for their affordability, speed, and simplicity. However, LFA sensitivity is often limited by the need for fast associative rates between the assay components. This work pr…
View article: An Integrin-Targeting Peptide Enables Efficient Lysosomal Delivery of Antibody-Drug Conjugates
An Integrin-Targeting Peptide Enables Efficient Lysosomal Delivery of Antibody-Drug Conjugates Open
Antibody-drug conjugates (ADCs) are standard-of-care therapies for several types of cancer, with an expanding representation in clinical development pipelines. A key determinant of efficacy for most ADCs is their ability to internalize int…
View article: Triggered ‘capture-and-release’ enables a high-affinity re-binding strategy for sensitivity enhancement in lateral flow assays
Triggered ‘capture-and-release’ enables a high-affinity re-binding strategy for sensitivity enhancement in lateral flow assays Open
Lateral flow assays (LFAs) are point-of-care devices known for their affordability, speed, and simplicity. However, their sensitivity is often limited due to the need for fast associative rates between assay components. This work presents …
View article: Formation of mono- and dual-labelled antibody fragment conjugates <i>via</i> reversible site-selective disulfide modification and proximity induced lysine reactivity
Formation of mono- and dual-labelled antibody fragment conjugates <i>via</i> reversible site-selective disulfide modification and proximity induced lysine reactivity Open
Exploiting quantitative and reversible site-selective disulfide modification as a means for selective lysine functionalisation on clinically relevant antibody fragments.
View article: Bis-amino maleimides: a new class of dual hydrogen bond donor for anion binding and transport
Bis-amino maleimides: a new class of dual hydrogen bond donor for anion binding and transport Open
Bis-amino maleimides are a new class of hydrogen bond donor for anion binding and transport. This motif contains three handles for synthetic diversification, offering opportunities to tune the structure, properties and function.
View article: Mass spectrometric imaging and quantitative analysis of the <i>in vivo</i> biodistribution of trastuzumab using a rhodium(<scp>iii</scp>) sarcophagine complex
Mass spectrometric imaging and quantitative analysis of the <i>in vivo</i> biodistribution of trastuzumab using a rhodium(<span>iii</span>) sarcophagine complex Open
A new immunoconjugate, Rh-sar-PD-trastuzumab, enables in vivo mapping of antibody biodistribution, and tissue imaging of HER2 expression, using ICP-MS methods.
View article: Modular Semisynthetic Approach to Generate T Cell-Dependent Bispecific Constructs from Recombinant IgG1 Antibodies
Modular Semisynthetic Approach to Generate T Cell-Dependent Bispecific Constructs from Recombinant IgG1 Antibodies Open
Redirecting T cells to tumor cells by bispecific antibodies is an effective approach to treat cancer, and T cell-dependent bispecific antibodies (TDBAs) are an emerging class of potent immunotherapeutic agents. By simultaneously targeting …
View article: A Modular Semi-Synthetic Approach to Generate T cell-Dependent Bispecific Constructs from Recombinant IgG1 Antibodies
A Modular Semi-Synthetic Approach to Generate T cell-Dependent Bispecific Constructs from Recombinant IgG1 Antibodies Open
Redirecting T cells to tumor cells by bispecific antibodies is an effective approach to treat cancer and T cell-dependent bispecific antibodies (TDBAs) are an emerging class of potent immunotherapeutic agents. By simultaneously targeting a…
View article: Synthesis and Antibacterial Study of 1-(4-(4-Chlorophenyl) thiazol-2-yl)-4-(4-methoxy phenyl)-5, 6-bis(o-/m-/p-nitrophenyl amino)pyridin-2(1H)-One
Synthesis and Antibacterial Study of 1-(4-(4-Chlorophenyl) thiazol-2-yl)-4-(4-methoxy phenyl)-5, 6-bis(o-/m-/p-nitrophenyl amino)pyridin-2(1H)-One Open
Acetone dicarboxylic acid prepared from reaction of citric acid with conc. H2SO4 .-(4-chlorophenyl)thiazol-2-amine is prepared by reaction of Thiourea and I2 were triturated and reflux with p-chloroacetophenone.Now, 1-(4-(4-Chlorophenylthi…
View article: An Albumin-Holliday Junction Biomolecular Modular Design for Programmable Multifunctionality and Prolonged Circulation
An Albumin-Holliday Junction Biomolecular Modular Design for Programmable Multifunctionality and Prolonged Circulation Open
Combinatorial properties such as long-circulation and site- and cell-specific engagement need to be built into the design of advanced drug delivery systems to maximize drug payload efficacy. This work introduces a four-stranded oligonucleo…
View article: Macrocyclic Dual‐Locked “Turn‐On” Drug for Selective and Traceless Release in Cancer Cells
Macrocyclic Dual‐Locked “Turn‐On” Drug for Selective and Traceless Release in Cancer Cells Open
Drug safety and efficacy due to premature release into the bloodstream and poor biodistribution remains a problem despite seminal advances in this area. To circumvent these limitations, we report drug cyclization based on dynamic covalent …
View article: Site-directed conjugation of single-stranded DNA to affinity proteins: quantifying the importance of conjugation strategy
Site-directed conjugation of single-stranded DNA to affinity proteins: quantifying the importance of conjugation strategy Open
Site-selective conjugation of ssDNA to affinity proteins grants improved target binding and lower non-specific binding.
View article: Chemo- and regio-selective differential modification of native cysteines on an antibody <i>via</i> the use of dehydroalanine forming reagents
Chemo- and regio-selective differential modification of native cysteines on an antibody <i>via</i> the use of dehydroalanine forming reagents Open
Use of dehydroalanine-forming reagents to enable the first example of differentially modifying the native solvent accessible cysteines on an antibody.
View article: Multivalent nanobody engineering for enhanced physisorption and functional display on gold nanoparticles
Multivalent nanobody engineering for enhanced physisorption and functional display on gold nanoparticles Open
Engineered multivalent nanobodies improve gold nanoparticle bioconjugate stability and improve sensitivity of nanobody-based lateral flow assay.
View article: The Nitrile Bis-Thiol Bioconjugation Reaction
The Nitrile Bis-Thiol Bioconjugation Reaction Open
Electron-poor aryl nitriles are promising reagents for bioconjugation due to their high electrophilicity and selectivity for reaction with thiols, albeit generally in a reversible manner. A transient species has previously been observed in…
View article: Rapid Access to Potent Bispecific T Cell Engagers Using Biogenic Tyrosine Click Chemistry
Rapid Access to Potent Bispecific T Cell Engagers Using Biogenic Tyrosine Click Chemistry Open
Bispecific antibodies as T cell engagers designed to display binding capabilities to both tumor-associated antigens and antigens on T cells are considered promising agents in the fight against cancer. Even though chemical strategies to dev…
View article: CCDC 2296018: Experimental Crystal Structure Determination
CCDC 2296018: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Hydrogel Cross-Linking via Thiol-Reactive Pyridazinediones
Hydrogel Cross-Linking via Thiol-Reactive Pyridazinediones Open
Thiol-reactive Michael acceptors are commonly used for the formation of chemically cross-linked hydrogels. In this paper, we address the drawbacks of many Michael acceptors by introducing pyridazinediones as new cross-linking agents. Throu…
View article: Dual-Locked Macrocyclic “Turn-On” Drug for Selective and Traceless Release in Cancer Cells
Dual-Locked Macrocyclic “Turn-On” Drug for Selective and Traceless Release in Cancer Cells Open
Drug safety and efficacy due to premature drug release in the bloodstream and poor biodistribution remain challenging issues despite seminal advances in the field. To circumvent these limitations, we report a directed-macrocylization as a …
View article: Site-directed Conjugation of Single-Stranded DNA to Affinity Proteins: Quantifying the Importance of Conjugation Strategy
Site-directed Conjugation of Single-Stranded DNA to Affinity Proteins: Quantifying the Importance of Conjugation Strategy Open
Affinity protein–oligonucleotide conjugates are increasingly being explored as diagnostic and therapeutic tools. Despite growing interest, these probes are typically constructed using outdated, non-selective chemistries, and little has bee…
View article: Site-directed Conjugation of Single-Stranded DNA to Affinity Proteins: Quantifying the Importance of Conjugation Strategy
Site-directed Conjugation of Single-Stranded DNA to Affinity Proteins: Quantifying the Importance of Conjugation Strategy Open
Affinity protein–oligonucleotide conjugates are increasingly being explored as diagnostic and therapeutic tools. Despite growing interest, these probes are typically constructed using outdated, non-selective chemistries, and little has bee…
View article: The Nitrile Bis-Thiol Bioconjugation Reaction
The Nitrile Bis-Thiol Bioconjugation Reaction Open
Electron-poor aryl nitriles are promising reagents for bioconjugation, due to their high electrophilicity and selectivity for reaction with thiols, albeit generally in a reversible manner. A transient species has previously been observed i…
View article: Trifunctional Dibromomaleimide Reagents Built Around A Lysine Scaffold Deliver Site‐selective Dual‐modality Antibody Conjugation
Trifunctional Dibromomaleimide Reagents Built Around A Lysine Scaffold Deliver Site‐selective Dual‐modality Antibody Conjugation Open
We describe the synthesis and application of a selection of trifunctional reagents for the dual‐modality modification of native, solvent accessible disulfide bonds in trastuzumab. The reagents were developed from the dibromomaleimide (DBM)…
View article: Chemical generation of checkpoint inhibitory T cell engagers for the treatment of cancer
Chemical generation of checkpoint inhibitory T cell engagers for the treatment of cancer Open
Bispecific T cell engagers (BiTEs), a subset of bispecific antibodies (bsAbs), can promote a targeted cancer cell’s death by bringing it close to a cytotoxic T cell. Checkpoint inhibitory T cell engagers (CiTEs) comprise a BiTE core with a…
View article: Chemical generation of checkpoint inhibitory T cell engagers (CiTEs) for the treatment of cancer
Chemical generation of checkpoint inhibitory T cell engagers (CiTEs) for the treatment of cancer Open
Bispecific antibodies (bsAbs) provide enticing therapeutic opportunities in the area of immunotherapy, especially in the field of immuno-oncology. These constructs can bind two separate antigenic epitopes and thus provide access to unique …
View article: Recent advances in N- and C-terminus cysteine protein bioconjugation
Recent advances in N- and C-terminus cysteine protein bioconjugation Open
Advances in the site-specific chemical modification of proteins, also referred to as protein bioconjugation, have proved instrumental in revolutionary approaches to designing new protein-based therapeutics. Of the sites available for prote…
View article: A Light‐Induced Decarboxylative‐Elimination of Substituted Maleimides as a Strategy Towards Triggered Photorelease
A Light‐Induced Decarboxylative‐Elimination of Substituted Maleimides as a Strategy Towards Triggered Photorelease Open
Herein we report on photodecarboxylations of various substituted maleimides, resulting in an elimination reaction. Furthermore, we establish facile wavelength tunability through modulation of the maleimide double bond substituents. We envi…
View article: Hydrogel crosslinking via thiol-reactive pyridazinediones
Hydrogel crosslinking via thiol-reactive pyridazinediones Open
Thiol-reactive Michael acceptors are commonly used for the formation of chemically crosslinked hydrogels. In this paper, we address the drawbacks of many Michael acceptors by introducing pyridazinediones as new crosslinking agents. Through…
View article: Modular Synthesis of Semiconducting Graft Copolymers to Achieve “Clickable” Fluorescent Nanoparticles with Long Circulation and Specific Cancer Targeting
Modular Synthesis of Semiconducting Graft Copolymers to Achieve “Clickable” Fluorescent Nanoparticles with Long Circulation and Specific Cancer Targeting Open
Semiconducting polymer nanoparticles (SPNs) are explored for applications in cancer theranostics because of their high absorption coefficients, photostability, and biocompatibility. However, SPNs are susceptible to aggregation and protein …
View article: Modular Chemical Construction of IgG-like Mono- and Bispecific Synthetic Antibodies (SynAbs)
Modular Chemical Construction of IgG-like Mono- and Bispecific Synthetic Antibodies (SynAbs) Open
In recent years there has been rising interest in the field of protein-protein conjugation, especially related to bispecific antibodies (bsAbs) and their therapeutic applications. These constructs contain two paratopes capable of binding t…