List of signaling peptide/protein receptor modulators

This is a list of signaling peptide/protein receptor modulators

Adiponectin

AdipoR₁

• Agonists: Peptide: Adiponectin
• ADP-355
• ADP-399; Non-peptide: AdipoRon
• (–)-Arctigenin
• Arctiin
• Gramine
• Matairesinol

• Antagonists: Peptide: ADP-400

AdipoR₂

• Agonists: Peptide: Adiponectin
• ADP-355
• ADP-399; Non-peptide: AdipoRon
• Deoxyschizandrin
• Parthenolide
• Syringing
• Taxifoliol

• Antagonists: Peptide: ADP-400

Angiotensin

• See here instead.

Bradykinin

• Agonists: Bradykinin
• Kallidin

• Antagonists: FR-173657
• Icatibant
• LF22-0542

Calcitonin gene-related peptide receptor

• Agonists: Amylin
• CGRP
• Pramlintide

• Antagonists: Atogepant
• BI 44370 TA
• CGRP (8-37)
• MK-3207
• Olcegepant
• Rimegepant
• SB-268262
• Telcagepant
• Ubrogepant

• Antibodies: Eptinezumab
• Erenumab
• Fremanezumab
• Galcanezumab

Cholecystokinin

CCK_A

• Agonists: Cholecystokinin

• Antagonists: Amiglumide
• Asperlicin
• Devazepide
• Dexloxiglumide
• Lintitript
• Lorglumide
• Loxiglumide
• Pranazepide
• Proglumide
• Tarazepide
• Tomoglumide

CCK_B

• Agonists: Cholecystokinin
• CCK-4
• Gastrin
• Pentagastrin (CCK-5)

• Antagonists: Ceclazepide
• CI-988 (PD-134308)
• Itriglumide
• L-365,360
• Netazepide
• Proglumide
• Spiroglumide

Unsorted

• Antagonists: Nastorazepide

Corticotropin-releasing hormone receptor

CRF₁

• Agonists: Cortagine
• Corticorelin
• Corticotropin-releasing hormone
• Sauvagine
• Stressin I
• Urocortin

• Antagonists: Antalarmin
• Astressin-B
• CP-154,526
• Emicerfont
• Hypericin
• LWH-234
• NBI-27914
• NBI-74788
• Pexacerfont
• R-121919
• TS-041
• Verucerfont

CRF₂

• Agonists: Corticorelin
• Corticotropin-releasing hormone
• Sauvagine
• Urocortin

• Antagonists: Astressin-B

Cytokine

See here instead.

Endothelin

• Agonists: Endothelin 1
• Endothelin 2
• Endothelin 3
• IRL-1620
• Sarafotoxin

• Antagonists: A-192621
• ACT-132577
• Ambrisentan
• Aprocitentan
• Atrasentan
• Avosentan
• Bosentan
• BQ-123
• BQ-788
• Clazosentan
• Darusentan
• Edonentan
• Enrasentan
• Fandosentan
• Feloprentan
• Macitentan
• Nebentan
• Sitaxentan
• Sparsentan
• Tezosentan
• Zibotentan

Galanin

GAL₁

• Agonists: Galanin
• Galanin (1-15)
• Galanin-like peptide
• Galmic
• Galnon
• NAX 810-2

• Antagonists: C7
• Dithiepine-1,1,4,4-tetroxide
• Galantide (M15)
• M32
• M35
• M40
• SCH-202596

GAL₂

• Agonists: Galanin
• Galanin (1-15)
• Galanin (2-11)
• Galanin-like peptide
• Galmic
• Galnon
• J18
• NAX 810-2

• Antagonists: C7
• Galantide (M15)
• M32
• M35
• M40
• M871

GAL₃

• Agonists: Galanin
• Galanin (1-15)
• Galmic
• Galnon

• Antagonists: C7
• Galantide (M15)
• GalR3ant
• HT-2157
• M32
• M35
• M40
• SNAP-37889
• SNAP-398299

Ghrelin/GHS

• See here instead.

GH

• See here instead.

GHRH

• See here instead.

GLP

GLP-1

• Agonists: Albiglutide
• Beinaglutide
• Dulaglutide
• Efpeglenatide
• Exenatide
• GLP-1
• Langlenatide
• Liraglutide
• Lixisenatide
• Oxyntomodulin
• Pegapamodutide
• Semaglutide
• Taspoglutide

GLP-2

• Agonists: Apraglutide
• Elsiglutide
• Glepaglutide
• GLP-2
• Teduglutide

Others

• Propeptides: Preproglucagon
• Proglucagon

Glucagon

• Agonists: Dasiglucagon
• Glucagon
• Oxyntomodulin

• Antagonists: Adomeglivant
• L-168,049
• LGD-6972

• Propeptides: Preproglucagon
• Proglucagon

GnRH

• See here instead.

Gonadotropin

• See here instead.

Growth factor

• See here instead.

Insulin

• Agonists: Chaetochromin (4548-G05)
• Insulin-like growth factor 1
• Insulin-like growth factor 2
• Insulin
• Insulin aspart
• Insulin degludec
• Insulin detemir
• Insulin glargine
• Insulin glulisine
• Insulin lispro
• Mecasermin
• Mecasermin rinfabate

• Antagonists: BMS-754807
• S661
• S961

• Kinase inhibitors: Linsitinib

• Antibodies: Xentuzumab (against IGF-1 and IGF-2)

Kisspeptin

• Agonists: Kisspeptin
• Kisspeptin-10

• Antagonists: Kisspeptin-234

Leptin

• Agonists: Leptin
• Metreleptin

Melanin-concentrating hormone receptor

MCH₁

• Agonists: Melanin-concentrating hormone

• Antagonists: ATC-0065
• ATC-0175
• GW-803430
• NGD-4715
• SNAP-7941
• SNAP-94847

MCH₂

• Agonists: Melanin-concentrating hormone

Melanocortin

• See here instead.

mTOR

• Activators: beta-Hydroxy beta-methylbutyric acid
• Hydroxynorketamine
• Leucine
• NV-5138

• Inhibitors: Rapalogs: Everolimus
• Ridaforolimus
• Sirolimus (Rapamycin)
• Temsirolimus
• Umirolimus
• Zotarolimus; ATP-competitive / indirect: Berberine
• Curcumin
• Dactolisib
• EF-24
• Epigallocatechin gallate
• HY-124798
• NV-5440
• Pterostilbene
• Quercetin
• Resveratrol
• Sapanisertib
• Torin-1
• WYE-687
• XL-388

Neuropeptide FF

• Agonists: Neuropeptide AF
• Neuropeptide FF
• Neuropeptide SF (RFRP-1)
• Neuropeptide VF (RFRP-3)

• Antagonists: BIBP-3226
• RF9

Neuropeptide S

• Agonists: Neuropeptide S

• Antagonists: ML-154
• SHA-68

Neuropeptide Y

Y₁

• Agonists: Neuropeptide Y
• Peptide YY

• Antagonists: BIBO-3304
• BIBP-3226
• BVD-10
• GR-231118
• PD-160170

Y₂

• Agonists: 2-Thiouridine 5'-triphosphate
• Neuropeptide Y
• Neuropeptide Y (13-36)
• Peptide YY
• Peptide YY (3-36)

• Antagonists: BIIE-0246
• JNJ-5207787
• SF-11

Y₄

• Agonists: GR-231118
• Neuropeptide Y
• Pancreatic polypeptide
• Peptide YY

• Antagonists: UR-AK49

Y₅

• Agonists: BWX-46
• Neuropeptide Y
• Peptide YY

• Antagonists: CGP-71683
• FMS-586
• L-152,804
• Lu AA-33810
• MK-0557
• NTNCB
• Velneperit (S-2367)

Neurotensin

NTS₁

• Agonists:
  • Neurotensin
  • Neuromedin N
• Antagonists:
  • Meclinertant
  • SR-142948

NTS₂

• Agonists:
  • Neurotensin
• Antagonists:
  • Levocabastine
  • SR-142948

Opioid

• See here instead.

Orexin

OX₁

• Agonists: Orexin (A, B)

• Antagonists: ACT-335827
• ACT-462206
• Almorexant
• Filorexant
• Lemborexant
• Nemorexant
• RTIOX-276
• SB-334867
• SB-408124
• SB-649868
• Suvorexant
• TCS-1102

OX₂

• Agonists: Orexin (A, B)
• SB-668875

• Antagonists: ACT-335827
• ACT-462206
• Almorexant
• EMPA
• Filorexant
• JNJ-10397049
• Lemborexant
• MK-1064
• SB-649868
• Seltorexant
• Suvorexant
• TCS-1102
• TCS-OX2-29

Oxytocin

• See here instead.

Prolactin

• Agonists: Growth hormone
• Human placental lactogen
• Placental growth hormone (growth hormone variant)
• Prolactin
• S179D-hPRL
• Somatotropin

• Antagonists: Δ1–9-G129R-hPRL
• Δ1–14-G129R-hPRL
• G120K-hGH
• G129R-hPRL

• Prolactin modulators: Prolactin inhibitors: D₂ receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D₂ receptor antagonists (e.g., domperidone, metoclopramide, risperidone)
• Estrogens (e.g., estradiol)
• Progestogens (e.g., progesterone)

PTH

• Agonists: Abaloparatide
• Parathyroid hormone
• Parathyroid hormone-related protein (PTHrP)
• Semparatide
• Teriparatide

Relaxin

• Agonists: Insulin-like factor 3
• Relaxin (1, 2, 3)
• Serelaxin

Somatostatin

• See here instead.

Tachykinin

• See here instead.

TRH

• Agonists: Azetirelin
• Fertirelin
• Montirelin
• Orotirelin
• Posatirelin
• Protirelin
• Rovatirelin
• Taltirelin
• TRH (TRF)

TSH

• Agonists: Thyrotropin alfa
• TSH (thyrotropin)

Vasopressin

• See here instead.

VIP/PACAP

VIPR₁

• Agonists: Peptide: Bay 55-9837
• LBT-3393
• PACAP
• VIP

VIPR₂

• Agonists: Peptide: LBT-3627
• PACAP
• VIP

PAC₁

• Agonists: PACAP
• PACAP (1-27)
• PACAP (1-38)

• Antagonists: PACAP (6-38)

Unsorted

• PHI
• PHM
• PHV

Others

• Endogenous: Adrenomedullin
• Apelin
• Asprosin
• Bombesin
• Calcitonin
• Carnosine
• CART
• CLIP
• DSIP
• Enteroglucagon
• Formyl peptide
• GALP
• GIP
• GRP
• Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin)
• Kininogens
• Motilin
• Natriuretic peptides (ANP, BNP, CNP, urodilatin)
• Nesfatin-1
• Neuromedin B
• Neuromedin N
• Neuromedin S
• Neuromedin U
• Obestatin
• Osteocalcin
• Resistin
• Secretin
• Thymopoietin
• Thymosins
• Thymulin
• Urotensin-II
• VGF

• Exogenous: Lifitegrast (LFA-1 antagonist)