Chalcone: A Privileged Structure in Medicinal Chemistry

Chemical Reviews, Год журнала: 2017, Номер 117(12), С. 7762 - 7810

Опубликована: Май 10, 2017

Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found many naturally occurring compounds. Many chalcone derivatives also prepared due to their convenient synthesis. These natural products and synthetic compounds shown numerous interesting biological activities with clinical potentials against various diseases. This review aims highlight the recent evidence of privileged chemistry. Multiple aspects will be summarized herein, including isolation novel derivatives, development new methodologies, evaluation properties, exploration mechanisms action well target identification. expected comprehensive, authoritative, critical community.

Язык: Английский

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Deuterium‐ and Tritium‐Labelled Compounds: Applications in the Life Sciences

Angewandte Chemie International Edition, Год журнала: 2017, Номер 57(7), С. 1758 - 1784

Опубликована: Авг. 17, 2017

Hydrogen isotopes are unique tools for identifying and understanding biological chemical processes. isotope labelling allows the traceless direct incorporation of an additional mass or radioactive tag into organic molecule with almost no changes in its structure, physical properties, activity. Using deuterium-labelled isotopologues to study mass-spectrometric patterns generated from mixtures biologically relevant molecules drastically simplifies analysis. Such methods now providing unprecedented levels insight a wide continuously growing range applications life sciences beyond. Tritium (3 H), particular, has seen increase utilization, especially pharmaceutical drug discovery. The efforts costs associated synthesis labelled compounds more than compensated by enhanced molecular sensitivity during analysis high reliability data obtained. In this Review, advances application hydrogen described.

Язык: Английский

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Bioorthogonal chemistry

Nature Reviews Methods Primers, Год журнала: 2021, Номер 1(1)

Опубликована: Апрель 15, 2021

Язык: Английский

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Chemical proteomics approaches for identifying the cellular targets of natural products

Natural Product Reports, Год журнала: 2016, Номер 33(5), С. 681 - 708

Опубликована: Янв. 1, 2016

This review focuses on chemical probes to identify the protein binding partners of natural products in living systems.

Язык: Английский

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Click Chemistry in Proteomic Investigations

Cell, Год журнала: 2020, Номер 180(4), С. 605 - 632

Опубликована: Фев. 1, 2020

Язык: Английский

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Advances in targeting ‘undruggable’ transcription factors with small molecules

Nature Reviews Drug Discovery, Год журнала: 2021, Номер 20(9), С. 669 - 688

Опубликована: Май 18, 2021

Язык: Английский

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The Life of Pi Star: Exploring the Exciting and Forbidden Worlds of the Benzophenone Photophore

Chemical Reviews, Год журнала: 2016, Номер 116(24), С. 15284 - 15398

Опубликована: Дек. 16, 2016

The widespread applications of benzophenone (BP) photochemistry in biological chemistry, bioorganic and material science have been prominent both academic industrial research. BP photophores unique photochemical properties: upon n−π* excitation at 365 nm, a biradicaloid triplet state is formed reversibly, which can abstract hydrogen atom from accessible C–H bonds; the radicals subsequently recombine, creating stable covalent C–C bond. This light-directed attachment process exploited many different ways: (i) binding/contact site mapping ligand (or protein)–protein interactions; (ii) identification molecular targets interactome mapping; (iii) proteome profiling; (iv) bioconjugation site-directed modification biopolymers; (v) surface grafting immobilization. also has practical advantages, including low reactivity toward water, stability ambient light, convenient nm. In addition, several BP-containing building blocks reagents are commercially available. this review, we explore "forbidden" (transitions) excitation-activated world photoinduced by touring colorful palette recent examples. exploration, will see pros cons using photophores, hope that novice expert photolabelers enjoy be inspired breadth depth possibilities.

Язык: Английский

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Achieving Controlled Biomolecule–Biomaterial Conjugation

Chemical Reviews, Год журнала: 2018, Номер 118(16), С. 7702 - 7743

Опубликована: Июль 24, 2018

The conjugation of biomolecules can impart materials with the bioactivity necessary to modulate specific cell behaviors. While biological roles particular polypeptide, oligonucleotide, and glycan structures have been extensively reviewed, along influence attachment on material structure function, key role played by strategy in determining activity is often overlooked. In this review, we focus chemistry biomolecule provide a comprehensive overview strategies for achieving controlled biomaterial functionalization. No universal method exists optimal attachment, here will discuss both relative advantages disadvantages each technique. doing so, highlight importance carefully considering impact suitability technique during design.

Язык: Английский

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Photocatalytic Modification of Amino Acids, Peptides, and Proteins

Chemistry - A European Journal, Год журнала: 2018, Номер 25(1), С. 26 - 42

Опубликована: Июль 31, 2018

Abstract In the last decade, visible‐light photoredox catalysis has emerged as a powerful strategy to enable novel transformations in organic synthesis. Owing mild reaction conditions (i.e., room temperature, use of visible light) and high functional‐group tolerance, could represent an ideal for chemoselective biomolecule modification. Indeed, recent trend is its application development methodologies amino acid Herein, up‐to‐date overview photocatalytic modification single acids, peptides, proteins provided. The advantages offered by suitability biocompatible are described. addition, brief consideration current limitations approaches, well future challenges be addressed, discussed.

Язык: Английский

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Target identification of natural medicine with chemical proteomics approach: probe synthesis, target fishing and protein identification

Signal Transduction and Targeted Therapy, Год журнала: 2020, Номер 5(1)

Опубликована: Май 21, 2020

Abstract Natural products are an important source of new drugs for the treatment various diseases. However, developing natural product-based medicines through random moiety modification is a lengthy and costly process, due in part to difficulties associated with comprehensively understanding mechanism action side effects. Identifying protein targets effective strategy, but most interact multiple targets, which complicate this process. In recent years, increasing number researchers have begun screen target proteins chemical proteomics approaches, can provide more comprehensive array active small molecules unbiased manner. Typically, experiments identification consist two key steps: (1) probe design synthesis (2) fishing identification. decades, five different types proteomic probes their respective methods been developed structures, variety approaches invented. Presently, we will classify these application scopes characteristics probes, methods, advantages disadvantages strategies.

Язык: Английский

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