Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs View Full Text


Ontology type: schema:Chapter     


Chapter Info

DATE

2020-01-03

AUTHORS

Longyuan Gong , Danrui Cui , Xiufang Xiong , Yongchao Zhao

ABSTRACT

Cullin-RING ligases (CRLs), the largest family of E3 ubiquitin ligases, have become an attractive target for drug discovery, primarily due to their ability to regulate the degradation of numerous functionally and structurally diverse proteins, thereby controlling a myriad of biological processes. As the abnormal expressions of CRLs and their substrate proteins are associated with human diseases, elucidating their roles in these physiological and pathological processes will facilitate CRL-targeting drug development for the treatment of these diseases. Notably, these studies are also providing new concepts for the design of potential small-molecule therapeutics targeting CRLs and for the use of CRLs to degrade “undruggable” proteins. In this chapter, we systematically review the development of small molecules that target CRLs and especially emphasize the applications of CRLs in a chemical chimera for protein degradation, termed proteolysis-targeting chimeras (PROTACs). More... »

PAGES

317-347

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/978-981-15-1025-0_19

DOI

http://dx.doi.org/10.1007/978-981-15-1025-0_19

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1123790118

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/31898236


Indexing Status Check whether this publication has been indexed by Scopus and Web Of Science using the SN Indexing Status Tool
Incoming Citations Browse incoming citations for this publication using opencitations.net

JSON-LD is the canonical representation for SciGraph data.

TIP: You can open this SciGraph record using an external JSON-LD service: JSON-LD Playground Google SDTT

[
  {
    "@context": "https://springernature.github.io/scigraph/jsonld/sgcontext.json", 
    "about": [
      {
        "id": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/11", 
        "inDefinedTermSet": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/", 
        "name": "Medical and Health Sciences", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Animals", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Cullin Proteins", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Disease", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Drug Design", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Drug Evaluation, Preclinical", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Humans", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Proteolysis", 
        "type": "DefinedTerm"
      }, 
      {
        "inDefinedTermSet": "https://www.nlm.nih.gov/mesh/", 
        "name": "Small Molecule Libraries", 
        "type": "DefinedTerm"
      }
    ], 
    "author": [
      {
        "affiliation": {
          "alternateName": "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China", 
          "id": "http://www.grid.ac/institutes/grid.13402.34", 
          "name": [
            "Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China", 
            "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Gong", 
        "givenName": "Longyuan", 
        "id": "sg:person.07553766144.18", 
        "sameAs": [
          "https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.07553766144.18"
        ], 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China", 
          "id": "http://www.grid.ac/institutes/grid.13402.34", 
          "name": [
            "Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China", 
            "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Cui", 
        "givenName": "Danrui", 
        "id": "sg:person.0732121253.08", 
        "sameAs": [
          "https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.0732121253.08"
        ], 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China", 
          "id": "http://www.grid.ac/institutes/grid.13402.34", 
          "name": [
            "Cancer Institute of the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China", 
            "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Xiong", 
        "givenName": "Xiufang", 
        "id": "sg:person.01110467571.75", 
        "sameAs": [
          "https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01110467571.75"
        ], 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China", 
          "id": "http://www.grid.ac/institutes/grid.13402.34", 
          "name": [
            "Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China", 
            "Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Zhao", 
        "givenName": "Yongchao", 
        "id": "sg:person.01304472406.33", 
        "sameAs": [
          "https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01304472406.33"
        ], 
        "type": "Person"
      }
    ], 
    "datePublished": "2020-01-03", 
    "datePublishedReg": "2020-01-03", 
    "description": "Cullin-RING ligases (CRLs), the largest family of E3 ubiquitin ligases, have become an attractive target for drug discovery, primarily due to their ability to regulate the degradation of numerous functionally and structurally diverse proteins, thereby controlling a myriad of biological processes. As the abnormal expressions of CRLs and their substrate proteins are associated with human diseases, elucidating their roles in these physiological and pathological processes will facilitate CRL-targeting drug development for the treatment of these diseases. Notably, these studies are also providing new concepts for the design of potential small-molecule therapeutics targeting CRLs and for the use of CRLs to degrade \u201cundruggable\u201d proteins. In this chapter, we systematically review the development of small molecules that target CRLs and especially emphasize the applications of CRLs in a chemical chimera for protein degradation, termed proteolysis-targeting chimeras (PROTACs).", 
    "editor": [
      {
        "familyName": "Sun", 
        "givenName": "Yi", 
        "type": "Person"
      }, 
      {
        "familyName": "Wei", 
        "givenName": "Wenyi", 
        "type": "Person"
      }, 
      {
        "familyName": "Jin", 
        "givenName": "Jianping", 
        "type": "Person"
      }
    ], 
    "genre": "chapter", 
    "id": "sg:pub.10.1007/978-981-15-1025-0_19", 
    "isAccessibleForFree": false, 
    "isPartOf": {
      "isbn": [
        "978-981-15-1024-3", 
        "978-981-15-1025-0"
      ], 
      "name": "Cullin-RING Ligases and Protein Neddylation", 
      "type": "Book"
    }, 
    "keywords": [
      "cullin-RING ligases", 
      "proteolysis-targeting chimeras", 
      "ubiquitin ligases", 
      "cullin-RING ubiquitin ligases", 
      "E3 ubiquitin ligases", 
      "potential small-molecule therapeutics", 
      "substrate proteins", 
      "diverse proteins", 
      "protein degradation", 
      "biological processes", 
      "small molecule therapeutics", 
      "ligases", 
      "human diseases", 
      "small molecules", 
      "large family", 
      "drug discovery", 
      "protein", 
      "attractive target", 
      "abnormal expression", 
      "pathological processes", 
      "chimeras", 
      "drug development", 
      "molecules", 
      "degradation", 
      "expression", 
      "family", 
      "discovery", 
      "therapeutics", 
      "target", 
      "applications", 
      "development", 
      "role", 
      "myriad", 
      "process", 
      "disease", 
      "ability", 
      "new concept", 
      "chapter", 
      "study", 
      "treatment", 
      "use", 
      "design", 
      "concept"
    ], 
    "name": "Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs", 
    "pagination": "317-347", 
    "productId": [
      {
        "name": "dimensions_id", 
        "type": "PropertyValue", 
        "value": [
          "pub.1123790118"
        ]
      }, 
      {
        "name": "doi", 
        "type": "PropertyValue", 
        "value": [
          "10.1007/978-981-15-1025-0_19"
        ]
      }, 
      {
        "name": "pubmed_id", 
        "type": "PropertyValue", 
        "value": [
          "31898236"
        ]
      }
    ], 
    "publisher": {
      "name": "Springer Nature", 
      "type": "Organisation"
    }, 
    "sameAs": [
      "https://doi.org/10.1007/978-981-15-1025-0_19", 
      "https://app.dimensions.ai/details/publication/pub.1123790118"
    ], 
    "sdDataset": "chapters", 
    "sdDatePublished": "2022-09-02T16:15", 
    "sdLicense": "https://scigraph.springernature.com/explorer/license/", 
    "sdPublisher": {
      "name": "Springer Nature - SN SciGraph project", 
      "type": "Organization"
    }, 
    "sdSource": "s3://com-springernature-scigraph/baseset/20220902/entities/gbq_results/chapter/chapter_371.jsonl", 
    "type": "Chapter", 
    "url": "https://doi.org/10.1007/978-981-15-1025-0_19"
  }
]
 

Download the RDF metadata as:  json-ld nt turtle xml License info

HOW TO GET THIS DATA PROGRAMMATICALLY:

JSON-LD is a popular format for linked data which is fully compatible with JSON.

curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1007/978-981-15-1025-0_19'

N-Triples is a line-based linked data format ideal for batch operations.

curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1007/978-981-15-1025-0_19'

Turtle is a human-readable linked data format.

curl -H 'Accept: text/turtle' 'https://scigraph.springernature.com/pub.10.1007/978-981-15-1025-0_19'

RDF/XML is a standard XML format for linked data.

curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1007/978-981-15-1025-0_19'


 

This table displays all metadata directly associated to this object as RDF triples.

167 TRIPLES      22 PREDICATES      74 URIs      68 LITERALS      16 BLANK NODES

Subject Predicate Object
1 sg:pub.10.1007/978-981-15-1025-0_19 schema:about N0f570cb0222f4b28a2ee69f1e6c03e21
2 N31394813870548f2bad39e3dc3c88c0c
3 N52954563f757433ca86d08e5f0cba3cd
4 Nc8354f50fb23423c8b14d2109e2172d8
5 Ncbbcf2a85fd9433eb4f14380dc03038f
6 Ne65734e1a3344bcc9e86cacaaa1b6189
7 Ne7e9a12aeaba4fc5bc05608a11341da6
8 Nec89c69985e14738a9c68689f9783759
9 anzsrc-for:11
10 schema:author N44d95ea2c4844c618afaf7fbbd360531
11 schema:datePublished 2020-01-03
12 schema:datePublishedReg 2020-01-03
13 schema:description Cullin-RING ligases (CRLs), the largest family of E3 ubiquitin ligases, have become an attractive target for drug discovery, primarily due to their ability to regulate the degradation of numerous functionally and structurally diverse proteins, thereby controlling a myriad of biological processes. As the abnormal expressions of CRLs and their substrate proteins are associated with human diseases, elucidating their roles in these physiological and pathological processes will facilitate CRL-targeting drug development for the treatment of these diseases. Notably, these studies are also providing new concepts for the design of potential small-molecule therapeutics targeting CRLs and for the use of CRLs to degrade “undruggable” proteins. In this chapter, we systematically review the development of small molecules that target CRLs and especially emphasize the applications of CRLs in a chemical chimera for protein degradation, termed proteolysis-targeting chimeras (PROTACs).
14 schema:editor N34e41d531883418d8ac1b843000564b2
15 schema:genre chapter
16 schema:isAccessibleForFree false
17 schema:isPartOf Ndc77f83f3ae94ca3bd04f005f9392208
18 schema:keywords E3 ubiquitin ligases
19 ability
20 abnormal expression
21 applications
22 attractive target
23 biological processes
24 chapter
25 chimeras
26 concept
27 cullin-RING ligases
28 cullin-RING ubiquitin ligases
29 degradation
30 design
31 development
32 discovery
33 disease
34 diverse proteins
35 drug development
36 drug discovery
37 expression
38 family
39 human diseases
40 large family
41 ligases
42 molecules
43 myriad
44 new concept
45 pathological processes
46 potential small-molecule therapeutics
47 process
48 protein
49 protein degradation
50 proteolysis-targeting chimeras
51 role
52 small molecule therapeutics
53 small molecules
54 study
55 substrate proteins
56 target
57 therapeutics
58 treatment
59 ubiquitin ligases
60 use
61 schema:name Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs
62 schema:pagination 317-347
63 schema:productId N1674e41ad5814007bdd13193ba5f607c
64 N28460df8b3334adb9711a4cb2a4ce04f
65 N4bebc1dc1ce94542ae95e76280f92469
66 schema:publisher N935b6b2845314e6f93e90d8234344dc8
67 schema:sameAs https://app.dimensions.ai/details/publication/pub.1123790118
68 https://doi.org/10.1007/978-981-15-1025-0_19
69 schema:sdDatePublished 2022-09-02T16:15
70 schema:sdLicense https://scigraph.springernature.com/explorer/license/
71 schema:sdPublisher Nb982729654484725ab7e3d148c995cb8
72 schema:url https://doi.org/10.1007/978-981-15-1025-0_19
73 sgo:license sg:explorer/license/
74 sgo:sdDataset chapters
75 rdf:type schema:Chapter
76 N0f570cb0222f4b28a2ee69f1e6c03e21 schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
77 schema:name Drug Design
78 rdf:type schema:DefinedTerm
79 N1674e41ad5814007bdd13193ba5f607c schema:name doi
80 schema:value 10.1007/978-981-15-1025-0_19
81 rdf:type schema:PropertyValue
82 N28460df8b3334adb9711a4cb2a4ce04f schema:name pubmed_id
83 schema:value 31898236
84 rdf:type schema:PropertyValue
85 N31394813870548f2bad39e3dc3c88c0c schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
86 schema:name Cullin Proteins
87 rdf:type schema:DefinedTerm
88 N34e41d531883418d8ac1b843000564b2 rdf:first N5391896b515044d0941348036f607c9f
89 rdf:rest N7d3113fbeb4b4c0995f6e597144b8d43
90 N37d3aa8bfdad434a9d5dff62ecfc0829 rdf:first sg:person.01110467571.75
91 rdf:rest N6cd85517ca174ccf8cbc7edf433c8619
92 N40609b9ae3af44fc8e41fb16815a4700 schema:familyName Jin
93 schema:givenName Jianping
94 rdf:type schema:Person
95 N44d95ea2c4844c618afaf7fbbd360531 rdf:first sg:person.07553766144.18
96 rdf:rest Nd0253e4a764f40ae99e7031b59ddbb99
97 N4bebc1dc1ce94542ae95e76280f92469 schema:name dimensions_id
98 schema:value pub.1123790118
99 rdf:type schema:PropertyValue
100 N52954563f757433ca86d08e5f0cba3cd schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
101 schema:name Humans
102 rdf:type schema:DefinedTerm
103 N5391896b515044d0941348036f607c9f schema:familyName Sun
104 schema:givenName Yi
105 rdf:type schema:Person
106 N6cd85517ca174ccf8cbc7edf433c8619 rdf:first sg:person.01304472406.33
107 rdf:rest rdf:nil
108 N7d3113fbeb4b4c0995f6e597144b8d43 rdf:first Nc493d06cf57346b1a93242330a510904
109 rdf:rest Nefce32bcce1a4750b17ff40ae31e5bb1
110 N935b6b2845314e6f93e90d8234344dc8 schema:name Springer Nature
111 rdf:type schema:Organisation
112 Nb982729654484725ab7e3d148c995cb8 schema:name Springer Nature - SN SciGraph project
113 rdf:type schema:Organization
114 Nc493d06cf57346b1a93242330a510904 schema:familyName Wei
115 schema:givenName Wenyi
116 rdf:type schema:Person
117 Nc8354f50fb23423c8b14d2109e2172d8 schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
118 schema:name Animals
119 rdf:type schema:DefinedTerm
120 Ncbbcf2a85fd9433eb4f14380dc03038f schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
121 schema:name Drug Evaluation, Preclinical
122 rdf:type schema:DefinedTerm
123 Nd0253e4a764f40ae99e7031b59ddbb99 rdf:first sg:person.0732121253.08
124 rdf:rest N37d3aa8bfdad434a9d5dff62ecfc0829
125 Ndc77f83f3ae94ca3bd04f005f9392208 schema:isbn 978-981-15-1024-3
126 978-981-15-1025-0
127 schema:name Cullin-RING Ligases and Protein Neddylation
128 rdf:type schema:Book
129 Ne65734e1a3344bcc9e86cacaaa1b6189 schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
130 schema:name Proteolysis
131 rdf:type schema:DefinedTerm
132 Ne7e9a12aeaba4fc5bc05608a11341da6 schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
133 schema:name Small Molecule Libraries
134 rdf:type schema:DefinedTerm
135 Nec89c69985e14738a9c68689f9783759 schema:inDefinedTermSet https://www.nlm.nih.gov/mesh/
136 schema:name Disease
137 rdf:type schema:DefinedTerm
138 Nefce32bcce1a4750b17ff40ae31e5bb1 rdf:first N40609b9ae3af44fc8e41fb16815a4700
139 rdf:rest rdf:nil
140 anzsrc-for:11 schema:inDefinedTermSet anzsrc-for:
141 schema:name Medical and Health Sciences
142 rdf:type schema:DefinedTerm
143 sg:person.01110467571.75 schema:affiliation grid-institutes:grid.13402.34
144 schema:familyName Xiong
145 schema:givenName Xiufang
146 schema:sameAs https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01110467571.75
147 rdf:type schema:Person
148 sg:person.01304472406.33 schema:affiliation grid-institutes:grid.13402.34
149 schema:familyName Zhao
150 schema:givenName Yongchao
151 schema:sameAs https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01304472406.33
152 rdf:type schema:Person
153 sg:person.0732121253.08 schema:affiliation grid-institutes:grid.13402.34
154 schema:familyName Cui
155 schema:givenName Danrui
156 schema:sameAs https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.0732121253.08
157 rdf:type schema:Person
158 sg:person.07553766144.18 schema:affiliation grid-institutes:grid.13402.34
159 schema:familyName Gong
160 schema:givenName Longyuan
161 schema:sameAs https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.07553766144.18
162 rdf:type schema:Person
163 grid-institutes:grid.13402.34 schema:alternateName Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China
164 schema:name Cancer Institute of the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China
165 Institute of Translational Medicine, Zhejiang University School of Medicine, Hangzhou, China
166 Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China
167 rdf:type schema:Organization
 




Preview window. Press ESC to close (or click here)


...