6VHG

Crystal structure of phosphorylated RET tyrosine kinase domain complexed with a pyrazolo[1,5-a]pyrimidine inhibitor

Functional Information from GO Data

Chain	GOid	namespace	contents
A	0004672	molecular_function	protein kinase activity
A	0004713	molecular_function	protein tyrosine kinase activity
A	0005524	molecular_function	ATP binding
A	0006468	biological_process	protein phosphorylation

Functional Information from PDB Data

site_id	AC1
Number of Residues	17
Details	binding site for residue QX1 A 1101

Chain	Residue
A	LEU730
A	GLU805
A	ALA807
A	GLY810
A	ARG878
A	ASN879
A	LEU881
A	SER891
A	ASP892
A	GLY731
A	PHE735
A	VAL738
A	ALA756
A	LYS758
A	GLU775
A	ILE788
A	VAL804

---

site_id	AC2
Number of Residues	7
Details	binding site for residue SO4 A 1102

Chain	Residue
A	SER811
A	ARG813
A	GLY814
A	ARG878
A	HOH1217
A	HOH1219
A	HOH1252

---

site_id	AC3
Number of Residues	5
Details	binding site for residue SO4 A 1103

Chain	Residue
A	ARG817
A	ARG820
A	GLY949
A	ASN950
A	HOH1255

---

site_id	AC4
Number of Residues	4
Details	binding site for residue SO4 A 1104

Chain	Residue
A	PRO720
A	ARG721
A	LYS722
A	HOH1205

---

site_id	AC5
Number of Residues	7
Details	binding site for residue SO4 A 1105

Chain	Residue
A	ARG770
A	ARG873
A	ARG897
A	ARG908
A	SER909
A	HOH1201
A	HOH1212

---

site_id	AC6
Number of Residues	4
Details	binding site for residue CL A 1106

Chain	Residue
A	ARG897
A	ASP898
A	GLU901
A	HOH1273

---

site_id	AC7
Number of Residues	3
Details	binding site for residue CL A 1107

Chain	Residue
A	TYR809
A	GLU884
A	GLY885

---

site_id	AC8
Number of Residues	2
Details	binding site for residue ACT A 1108

Chain	Residue
A	LYS740
A	HOH1213

---

Functional Information from PROSITE/UniProt

site_id	PS00107
Number of Residues	29
Details	PROTEIN_KINASE_ATP Protein kinases ATP-binding region signature. LGEGEFGKVVkAtafhlkgragytt.....VAVK

Chain	Residue	Details
A	LEU730-LYS758

---

site_id	PS00109
Number of Residues	13
Details	PROTEIN_KINASE_TYR Tyrosine protein kinases specific active-site signature. LVHrDLAARNILV

Chain	Residue	Details
A	LEU870-VAL882

---

Functional Information from SwissProt/UniProt

site_id	SWS_FT_FI1
Number of Residues	1
Details	Active site: {"description":"Proton acceptor","evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PROSITE-ProRule","id":"PRU10028","evidenceCode":"ECO:0000255"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI2
Number of Residues	8
Details	Binding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000305"},{"source":"PDB","id":"4CKI","evidenceCode":"ECO:0007744"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI3
Number of Residues	1
Details	Binding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000305"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI4
Number of Residues	2
Details	Binding site: {"evidences":[{"source":"PubMed","id":"20117004","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"2X2M","evidenceCode":"ECO:0007744"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI5
Number of Residues	1
Details	Site: {"description":"Cleavage; by caspase-3","evidences":[{"source":"PubMed","id":"21357690","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI6
Number of Residues	1
Details	Site: {"description":"Breakpoint for translocation to form PCM1-RET; RET-CCDC6; RET-GOLGA5; RET-TRIM24 and RET-TRIM33 oncogenes","evidences":[{"source":"PubMed","id":"10439047","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"10980597","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"2406025","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"2734021","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI7
Number of Residues	2
Details	Modified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI8
Number of Residues	1
Details	Modified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"16928683","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI9
Number of Residues	1
Details	Modified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"16928683","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"20117004","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"28846099","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---

site_id	SWS_FT_FI10
Number of Residues	1
Details	Modified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"}]}

Chain

Residue

Details

---