The “cyclopropyl fragment” is a versatile player that frequently appears in preclinical/clinical drug molecules
TT Talele - Journal of medicinal chemistry, 2016 - ACS Publications
Recently, there has been an increasing use of the cyclopropyl ring in drug development to
transition drug candidates from the preclinical to clinical stage. Important features of the …
transition drug candidates from the preclinical to clinical stage. Important features of the …
[HTML][HTML] Vascular endothelial dysfunction and pharmacological treatment
JB Su - World journal of cardiology, 2015 - ncbi.nlm.nih.gov
The endothelium exerts multiple actions involving regulation of vascular permeability and
tone, coagulation and fibrinolysis, inflammatory and immunological reactions and cell …
tone, coagulation and fibrinolysis, inflammatory and immunological reactions and cell …
International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences
LMF Leeb-Lundberg, F Marceau, W Müller-Esterl… - Pharmacological …, 2005 - ASPET
Kinins are proinflammatory peptides that mediate numerous vascular and pain responses to
tissue injury. Two pharmacologically distinct kinin receptor subtypes have been identified …
tissue injury. Two pharmacologically distinct kinin receptor subtypes have been identified …
Sensory and signaling mechanisms of bradykinin, eicosanoids, platelet-activating factor, and nitric oxide in peripheral nociceptors
Peripheral mediators can contribute to the development and maintenance of inflammatory
and neuropathic pain and its concomitants (hyperalgesia and allodynia) via two …
and neuropathic pain and its concomitants (hyperalgesia and allodynia) via two …
The kallikrein-kinin system: current and future pharmacological targets
ME Moreau, N Garbacki, G Molinaro… - Journal of …, 2005 - jstage.jst.go.jp
The kallikrein-kinin system is an endogenous metabolic cascade, triggering of which results
in the release of vasoactive kinins (bradykinin-related peptides). This complex system …
in the release of vasoactive kinins (bradykinin-related peptides). This complex system …
Kinin receptors in pain and inflammation
R Couture, M Harrisson, RM Vianna… - European journal of …, 2001 - Elsevier
Kinins are among the most potent autacoids involved in inflammatory, vascular and pain
processes. These short-lived peptides, including bradykinin, kallidin and T-kinin, are …
processes. These short-lived peptides, including bradykinin, kallidin and T-kinin, are …
Mutant G-protein-coupled receptors as a cause of human diseases
T Schöneberg, A Schulz, H Biebermann… - Pharmacology & …, 2004 - Elsevier
G-protein-coupled receptors (GPCR) are involved in directly and indirectly controlling an
extraordinary variety of physiological functions. Their key roles in cellular communication …
extraordinary variety of physiological functions. Their key roles in cellular communication …
Bradykinin receptor ligands: therapeutic perspectives
F Marceau, D Regoli - Nature reviews Drug discovery, 2004 - nature.com
Kinins, which are produced by the action of kallikrein enzymes, are blood-derived local-
acting peptides that have broad effects mediated by two related G-protein-coupled receptors …
acting peptides that have broad effects mediated by two related G-protein-coupled receptors …
Nonallergic angioedema: role of bradykinin
M Bas, V Adams, T Suvorava, T Niehues… - Allergy, 2007 - Wiley Online Library
Angioedema is an underestimated clinical problem. Many cases are nonallergic reactions,
eg bradykinin‐induced angioedema caused by genetic defects and angiotensin‐converting …
eg bradykinin‐induced angioedema caused by genetic defects and angiotensin‐converting …
Kinins in pain and inflammation
In 1949, Rocha e Silva and collaborators reported the existence of a new relaxing
substance, liberated in plasma by the action of the snake venom of Bothrops jararaca or by …
substance, liberated in plasma by the action of the snake venom of Bothrops jararaca or by …