Signaling Pathways
The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.
ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.
The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.
References:
[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.
Products for Signaling Pathways
- Proteases(1086)
- Apoptosis(645)
- Chromatin/Epigenetics(344)
- Metabolism(720)
- MAPK Signaling(99)
- Tyrosine Kinase(275)
- DNA Damage/DNA Repair(480)
- PI3K/Akt/mTOR Signaling(128)
- Microbiology & Virology(887)
- Cell Cycle/Checkpoint(295)
- Ubiquitination/ Proteasome(155)
- JAK/STAT Signaling(66)
- TGF-β / Smad Signaling(35)
- Angiogenesis(81)
- GPCR/G protein(552)
- Stem Cell(87)
- Membrane Transporter/Ion Channel(465)
- Cancer Biology(211)
- Endocrinology and Hormones(222)
- Neuroscience(898)
- Obesity, Appetite Control & Diabetes(108)
- Other Signal Transduction(31)
- Immunology/Inflammation(1135)
- Cardiovascular(280)
- Vitamin D Related(13)
- PROTAC(135)
- Ox Stress Reagents(138)
- Others(1262)
- Antiparasitics(40)
- Toxins(28)
- Cat.No. Product Name Information
-
GC68479
MMRi62
-
GC68478
Bictegravir sodium
-
GC68477
Stepronin
-
GC68476
(S)-Nicardipine
-
GC68475
(R)-Nicardipine
-
GC68474
Pivanex
-
GC68473
Methyl carnosate
-
GC68471
Nifurpirinol
-
GC68470
SPD304 dihydrochloride
-
GC68469
CID1231538
-
GC68468
MPO-IN-3
-
GC68465
SDH-IN-1
-
GC68464
ALDH1A3-IN-1
-
GC68463
ULK1-IN-2
-
GC68462
ALDH1A3-IN-2
-
GC68461
TrxR-IN-5
-
GC68460
PDE4B-IN-3
-
GC68459
NHS-SS-Ac
-
GC68458
HS-243
-
GC68457
Mab Aspartate Decarboxylase-IN-1
-
GC68455
CP681301
-
GC68453
ITMN 4077
-
GC68452
2,4,6-Triiodophenol
-
GC68451
SRI-37330
-
GC68450
Hsp90-IN-17 hydrochloride
-
GC68449
CA inhibitor 1
-
GC68448
AOH1160
-
GC68447
GSK143 dihydrochloride
-
GC68446
NRX-103094
-
GC68445
SCD1 inhibitor-3
-
GC68444
SBI-993
-
GC68443
T3Inh-1
-
GC68442
L-Glutamine-15N-1
-
GC68441
SRI-37330 hydrochloride
-
GC68440
EGFR-IN-69
-
GC68439
GNE-064
-
GC68438
AMPA receptor modulator-3
-
GC68437
Vimentin-IN-1
-
GC68436
L82-G17
-
GC68435
Clazosentan
-
GC68433
OTS447
-
GC68432
DB-3-291
-
GC68431
NJH-2-030
-
GC68430
Selatinib
-
GC68429
GNE-490
-
GC68428
Rimantadine-d4 hydrochloride
-
GC68427
GSK1521498 free base
-
GC68426
17a-Hydroxypregnenolone-d3
-
GC68425
Ranolazine-d3
-
GC68424
Fingolimod-d4 hydrochloride
-
GC68423
Indomethacin-d4 Methyl Ester
-
GC68422
Choline-d4 chloride
-
GC68421
L-Aspartic acid-13C4,15N
-
GC68420
Propionylpromazine-d6 hydrochloride
-
GC68419
Prasugrel-d3
-
GC68418
Clenbuterol-d9
-
GC68417
Homovanillic acid-d5
-
GC68416
RAD51-IN-3
-
GC68415
Glycolic acid-d2
-
GC68414
(Rac)-Atropine-d3
-
GC68413
CYH33
-
GC68412
NAMPT inhibitor-linker 1
-
GC68411
RORγt Inverse agonist 10
-
GC68410
(S)-Mirtazapine-d3
-
GC68409
Cetirizine D8
-
GC68408
(R)-Praziquantel-d11
-
GC68407
Phenylethanolamine A-d3
-
GC68405
Lys-CoA TFA
-
GC68404
Human PD-L1 inhibitor IV
-
GC68403
Dusquetide
-
GC68402
Danofloxacin-d3
-
GC68401
Lehmannine
-
GC68399
Isolindleyin
-
GC68397
Galicaftor
-
GC68396
Vepafestinib
-
GC68395
L-Isoleucine-d10
-
GC68390
α5β1 integrin agonist-1
-
GC68389
SJ995973
-
GC68388
XIAP degrader-1
-
GC68387
FGN849
-
GC68386
CD73-IN-5
-
GC68385
TNF-α-IN-6
-
GC68384
DL-Mevalonolactone-d7
-
GC68383
(R)-Preclamol
-
GC68382
L-Cysteine-1-13C
-
GC68381
L-Glutamine-1-13C
-
GC68380
Sarcosine-15N
-
GC68379
L-Arginine-13C6,15N4 hydrochloride
-
GC68378
GDC-4379
-
GC68377
OAB-14
-
GC68376
PROTAC AR-V7 degrader-1
-
GC68375
Cholic acid-13C
-
GC68374
5a-Pregnane-3,20-dione-d6
-
GC68373
BLK-IN-2
-
GC68371
Mutant p53 modulator-1
-
GC68370
Amatuximab
-
GC68369
Belantamab
-
GC68368
Magrolimab
-
GC68367
Ieramilimab
-
GC68366
Thiocolchicine-d3