Target General Infomation
Target ID
T17163
Former ID
TTDR00238
Target Name
Leptin receptor
Gene Name
LEPR
Synonyms
HuB219; LEP-R; OB receptor; OB-R; LEPR
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Cachexia [ICD9: 799.4; ICD10: R64]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Diabetes; Hypertriglyceridemia [ICD9: 250, 272.1, 272.6; ICD10: E08-E13, E78.1, E78.2, E78.3, E88.1]
Obesity [ICD9: 278; ICD10: E66]
Function
Receptor for obesity factor (leptin). On ligand binding, mediates signaling through JAK2/STAT3. Involved in the regulation of fat metabolism and, in a hematopoietic pathway, required for normal lymphopoiesis. May play a role in reproduction. Can also mediate the ERK/FOS signaling pathway (By similarity).
BioChemical Class
Cytokine receptor
UniProt ID
Sequence
MICQKFCVVLLHWEFIYVITAFNLSYPITPWRFKLSCMPPNSTYDYFLLPAGLSKNTSNS
NGHYETAVEPKFNSSGTHFSNLSKTTFHCCFRSEQDRNCSLCADNIEGKTFVSTVNSLVF
QQIDANWNIQCWLKGDLKLFICYVESLFKNLFRNYNYKVHLLYVLPEVLEDSPLVPQKGS
FQMVHCNCSVHECCECLVPVPTAKLNDTLLMCLKITSGGVIFQSPLMSVQPINMVKPDPP
LGLHMEITDDGNLKISWSSPPLVPFPLQYQVKYSENSTTVIREADKIVSATSLLVDSILP
GSSYEVQVRGKRLDGPGIWSDWSTPRVFTTQDVIYFPPKILTSVGSNVSFHCIYKKENKI
VPSKEIVWWMNLAEKIPQSQYDVVSDHVSKVTFFNLNETKPRGKFTYDAVYCCNEHECHH
RYAELYVIDVNINISCETDGYLTKMTCRWSTSTIQSLAESTLQLRYHRSSLYCSDIPSIH
PISEPKDCYLQSDGFYECIFQPIFLLSGYTMWIRINHSLGSLDSPPTCVLPDSVVKPLPP
SSVKAEITINIGLLKISWEKPVFPENNLQFQIRYGLSGKEVQWKMYEVYDAKSKSVSLPV
PDLCAVYAVQVRCKRLDGLGYWSNWSNPAYTVVMDIKVPMRGPEFWRIINGDTMKKEKNV
TLLWKPLMKNDSLCSVQRYVINHHTSCNGTWSEDVGNHTKFTFLWTEQAHTVTVLAINSI
GASVANFNLTFSWPMSKVNIVQSLSAYPLNSSCVIVSWILSPSDYKLMYFIIEWKNLNED
GEIKWLRISSSVKKYYIHDHFIPIEKYQFSLYPIFMEGVGKPKIINSFTQDDIEKHQSDA
GLYVIVPVIISSSILLLGTLLISHQRMKKLFWEDVPNPKNCSWAQGLNFQKPETFEHLFI
KHTASVTCGPLLLEPETISEDISVDTSWKNKDEMMPTTVVSLLSTTDLEKGSVCISDQFN
SVNFSEAEGTEVTYEDESQRQPFVKYATLISNSKPSETGEEQGLINSSVTKCFSSKNSPL
KDSFSNSSWEIEAQAFFILSDQHPNIISPHLTFSEGLDELLKLEGNFPEENNDKKSIYYL
GVTSIKKRESGVLLTDKSRVSCPFPAPCLFTDIRVLQDSCSHFVENNINLGTSSKKTFAS
YMPQFQTCSTQTHKIMENKMCDLTV
Drugs and Mode of Action
Drug(s) Metreleptin Drug Info Approved Diabetes; Hypertriglyceridemia [542357], [550293]
Second-generation leptin Drug Info Terminated Obesity [547353]
Modulator AMPE4L Drug Info [543464]
AMPPL Drug Info [543464]
AMPSL Drug Info [543464]
ANG-2004 Drug Info [543464]
Leptin Drug Info [543464]
Metreleptin Drug Info [533123]
PEGylated leptin Drug Info [543464]
Second-generation leptin Drug Info [544044]
Antagonist BL-5040 Drug Info [543464]
PEG-LPA-2 Drug Info [543464]
Agonist EDP-21 Drug Info [543464]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cytokine-cytokine receptor interaction
Neuroactive ligand-receptor interaction
AMPK signaling pathway
Jak-STAT signaling pathway
Adipocytokine signaling pathway
Non-alcoholic fatty liver disease (NAFLD)
Pathway Interaction Database Signaling events mediated by PTP1B
WikiPathways Leptin signaling pathway
AMPK Signaling
References
Ref 542357(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7333).
Ref 547353Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015436)
Ref 550293US FDA approves orphan drug MYALEPT? (metreleptin for injection)
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 543464(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1712).
Ref 544044Effects of Exogenous Leptin on Satiety and Satiation in Patients with Lipodystrophy and Leptin Insufficiency. J Clin Endocrinol Metab. 2004 September; 89(9): 4258-4263.

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